Pharmacognosy and Phytochemistry

Eighteen strawberry genotypes were evaluated for their phenolic content and antioxidant capacity using several methods. High antioxidant capacity was found for `Harmonie', `Saint-Jean d'Orléans', and `Saint-Laurent d'Orléans', which were reported to have better shelf life than `Kent'. `Harmonie', `Saint-Jean d'Orléans', `Orléans', and some advanced selections had higher hydroxycinnamic acids, benzoic acids, and flavonols than `Kent'. The significant variation in antioxidant capacity and total phenolic compounds clearly shows the potential value of certain new cultivars and advanced lines as parents in a breeding program. The future plan is to examine individual antioxidant and their role in disease resistance and extension of shelf life and to use selected genotypes as parents to developed new lines.

Chrysin has been shown to exert several beneficial pharmacological activities. Chrysin has anti-cancer, anti-viral, anti-diabetic, neuroprotective, cardioprotective, hepatoprotective, and renoprotective as well as gastrointestinal, respiratory , reproductive, ocular, and skin protective effects through modulating signaling pathway involved in apoptosis, oxidative stress, and inflammation. In the current review, we discussed the emerging cellular and molecular mechanisms underlying therapeutic indications of chrysin in various cancers. Online databases comprising Scopus, PubMed, Embase, ProQuest, Science Direct, Web of Science, and the search engine Google Scholar were searched for available and eligible research articles. The search was conducted by using MeSH terms and keywords in title, abstract, and keywords. In conclusion, experimental studies indicated that chrysin could ameliorate cancers of the breast, gastroin-testinal tract, liver and hepatocytes, bladder, male and female reproductive systems, choroid, respiratory tract, thyroid, skin, eye, brain, blood cells, leukemia, osteoblast, and lymph. However, more studies are needed to enhance the bio-availability of chrysin and evaluate this agent in clinical trial studies.

Hydrosol beverages in Persian nutrition culture and ethnomedicine are the side products of essential oil industry that are used as delicious drinks or safe remedies. To investigate indications and chemical composition of hydrosol beverages for hyperlipidemia and cardiovascular conditions, Fars province was selected as the field of study. Ethnomedical data were gathered by questionnaires. The constituents of hydrosols were extracted with liquid/liquid extraction and analyzed by gas chromatography-mass spectrometry. Statistical analysis were used to cluster their constituents and find the relevance of their composition. A literature survey was also performed on plants used to prepare them. Thymol was the major or second major component of these beverages, except for wormwood and olive leaf hydrosols. Based on clustering methods, although some similarities could be found, composition of barberry, will fumitory, dill, and aloe hydrosols have more differences than others. These studies may help in developing some functional beverages or new therapeutics.

As Allium cepa is one of the most important condiment plants grown and consumed all over the world, various therapeutic and pharmacological effects of A. cepa were reviewed. Onion (Allium cepa) is a high dietary fiber-rich perennial herb that is placed under the family Amaryllidaceae. It contains high concentration of folic acid, vitamin B6, magnesium, calcium, potassium, and phosphorus as well as vitamins and minerals. It is widely used as an antimicrobial agent, but it showed anticancer, antidiabetic, antioxidant, antiplatelet, antihypertensive, and antidepressant effects and neuroprotective, anti-inflammatory, and antiparasitic effects and so on. It is said to have beneficial effects on the digestive, circulatory, and respiratory systems, as well as on the immune system. is review article was devoted to discussing many health benefits and traditional uses of onions in pharmacological perspectives, as well as the safety/toxicological profile. If more detailed research on this perennial herb is conducted, it will open the door to an infinite number of possibilities.

Ginkgo biloba is an ancient plant species that is thought to provide a variety of health benefits to living organisms and contains plenty of bioactive components, making it a chemically diversified plant. G. biloba has been shown to have a variety of medicinal and pharmacological properties, including anticancer, antidementia, antidiabetic, antiobesity, antilipidemic, antimicrobial, antioxidant, antilipid peroxidation, antiplatelet, anti-inflammatory, hepatoprotective, antidepressant, antiaging, immunomod-ulatory, antihypertensive, and neuroprotective effects and is frequently used to treat neurological, cardiovascular, and respiratory diseases, such as tardive dyskinesia. erefore, this review described the therapeutic applications of G. biloba. In addition to describing the therapeutic potential, this review also evaluates the chemical constituents, toxicity, adverse effect, synergistic effect, and the clinical studies of this plant which have been utilized for therapeutic benefits but have demonstrated other consequences.

Fungal diseases represent an increasing threat to human health worldwide which in some cases might be associated with substantial morbidity and mortality. However, only few antifungal drugs are currently available for the treatment of life-threatening fungal infections. Furthermore, plant diseases caused by fungal pathogens represent a worldwide economic problem for the agriculture industry. The marine environment continues to provide structurally diverse and biologically active secondary metabolites, several of which have inspired the development of new classes of therapeutic agents. Among these secondary metabolites, several compounds with noteworthy antifungal activities have been isolated from marine microorganisms, invertebrates, and algae. During the last fifteen years, around 65% of marine natural products possessing antifungal activities have been isolated from sponges and bacteria. This review gives an overview of natural products from diverse marine organisms that have shown in vitro and/or in vivo potential as antifungal agents, with their mechanism of action whenever applicable. The natural products literature is covered from January 2000 until June 2015, and we are reporting the chemical structures together with their biological activities, as well as the isolation source.

Cancer is one of the most extreme medical conditions in both developing and developed countries around the world, causing millions of deaths each year. Chemotherapy and/or radiotherapy are key for treatment approaches, but both have numerous adverse health effects. Furthermore, the resistance of cancerous cells to anticancer medication leads to treatment failure. The rising burden of cancer overall requires novel efficacious treatment modalities. Natural medications offer feasible alternative options against malignancy in contrast to western medication. Furanocoumarins' defensive and restorative impacts have been observed in leukemia, glioma, breast, lung, renal, liver, colon, cervical, ovarian, and prostate malignancies. Experimental findings have shown that furanocoumarins activate multiple signaling pathways, leading to apoptosis, autophagy, antioxidant, antimetastatic, and cell cycle arrest in malignant cells. Additionally, furanocoumarins have been shown to have chemo preventive and chemotherapeutic synergistic potential when used in combination with other anticancer drugs. Here, we address different pathways which are activated by furanocoumarins and their therapeutic efficacy in various tumors. Ideally, this review will trigger interest in furanocoumarins and their potential efficacy and safety as a cancer lessening agents.

Alzheimer's disease (AD) is a neurodegenerative condition mostly communal in people of advanced years accompanying various dysfunctionalities especially cognitive impairments. A number of cellular damages, such as amyloid-beta aggregation, tau protein hyperphosphorylation, some neurotransmitter imbalances, apoptosis, oxidative stress, and inflammatory responses are responsible for AD incidence. As a reason for inadequate efficacy, side effects, and pharmacokinetic problems of conventional drugs used for AD, the discovery of novel therapeutic agents with multi-targeted potential is desirable. Protective properties of phytochemicals combat numerous diseases and their vast acceptance and demand in human beings encouraged scientists to assess their effective activities. Zingiber officinale, gingerol, shogaol, and borneol were evaluated against memory impairments. Online databases including; Web of Science, Scopus, Embase, Pubmed, ProQuest, ScienceDirect, and Cochrane Library were searched until 3 February 2020. In vitro, in vivo, and clinical studies are included after screening their eligibility. Mostly interventive mechanisms such as; oxidative stress, neuroinflammation, and apoptosis are described. Correlation between the pathogenesis of AD and signaling pathways is explicated. Results and scores of cognition measurements are clarified due to in vivo studies and clinical trials. Some traditional aspects of consuming ginger in AD are also mentioned in the present review. In accumulation ginger and its components possess great potency for improving and abrogating memory dysfunctions but conducting further studies to evaluate their pharmacological and pharmaceutical aspects is required.

About 12% of world population is affected by different forms of urolithiasis of which the recurrence rate in female is 47-60% and in male is 70-80%. Standard therapeutic agents (allopurinol, citrate, cystone and thiazide diuretics) are used to prevent and treat urolithiasis but these are not universally-effective due to common kidney stone relapse and other side effects. Surgical treatment causes long-term renal damage, hypertension and stone recurrence. Polyphenols, the plant-derived bioactive molecules, have showed protection against cancers, car-diovascular diseases, diabetes, osteoporosis and neurodegenerative diseases, among a number of other ailments. The role of these phytochemicals in urolithiasis management is emerging. Hence, the present review discusses peer-reviewed published literature till date on this aspect and highlights that polyphenols could effectively inhibit the formation of calcium oxalate urinary stones (most common renal stone), correlating with their an-tioxidant, anti-inflammatory, diuretic and angiotensin-converting enzyme (ACE) inhibition. Further, we have proposed the prospects and challenges in developing the plant polyphenols into drugs against kidney stone prevention. This review might be a stepping stone for further investigation into the clinical implications of the polyphenols in urolithiasis remediation.

Phosphodiesterase inhibitors (PDEIs) are a class of drugs that are widely used because of their various pharmacological properties including cardiotonic, vasodilator, smooth muscle relaxant, antidepressant, antithrombotic, bronchodilator, antiinflammatory and enhancer of cognitive function. In the recent years, interest in drugs of plant origin has been progressively increased. Some pharmacologically active substances that come from plants demonstrate PDEI activity. They mainly belong to alkaloids, flavonoids, and saponins. In this review, studies on herbal PDEI were reviewed and their possible therapeutic applications were discussed. Screening plants for PDE inhibitory activity may help to develop standardized phytotherapeutic products or find new sources for new lead structures with PDEI pharmacological activity. The studies discussed in this paper are mainly in vitro and for more reasonable and conclusive results, it is required to conduct in vivo and finally human and clinical tests.Copyright 2009 Elsevier Ltd. All rights reserved.

Thymoquinone is a monoterpenoid compound which derives from volatile and fixed oil of Nigella sativa (Ranunculaceae). This phytochemical compound has several biological effects including; antioxidant, antibacterial, antineoplastic, nephroprotective, hepatoprotective, gastroprotective, neuroprotective, anti-nociceptive, and anti-inflammatory activities. Thymoquinone shows pharmacological activities including anti-hepatocellular carcinoma, nephroprotection, neuroprotection, retina protection, gastroprotection, cardioprotection, anti-allergy, reproductive system protection, bladder protection, and respiratory protection. It was found that these beneficial effects are mostly related to modulation of the Nrf2 signaling pathway by blockage of Keap1, stimulating the expression of the Nrf2 gene, and inducing the nuclear translocation of Nrf2. In the present review, the therapeutic effects of thymoquinone are overviewed through the Nrf2 signaling pathway.

Many researches have been undergone to hasten the natural wound healing process. In this study, several Hi-biscus species (leaves) were extracted with petroleum ether, methanol, and their mucilage was separated. All the tested species extracts were assessed for their viability percentage using the water-soluble tetrazolium. H.syriacus was the plant of choice to be incorporated in a new drug delivery system and evaluated for its wound healing activity. H.syriacus petroleum ether extract (PEE) showed a high percentage of palmitic and oleic acids while its mucilage demonstrated high glucosamine and galacturonic acid. It was selected to be formulated and pharmaceutically evaluated into three different composite sponges using chitosan in various ratios. Fourier-transformed infrared spectroscopy investigated the chemical interaction between the utilized sponges' ingredients. Morphological characteristics were evaluated using scanning electron microscopy. H.syriacus composite sponge of mucilage: chitosan (1:5) was loaded with three different concentrations of PEE. Medicated formulations were assessed in rat model of excision wound model. The wound healing ability was clearly proved by the clinical acceleration, histopathological examination, and modulation of correlated inflammatory parameters as tumor necrosis factor in addition to vascular endothelial growth factor suggesting a promising valuable candidate that supports the management of excision wounds using single-dose preparation.

Molecular mechanism behind the therapeutic potential of pigeon pea over the human diseases such as rheumatoid arthritis, breast cancer, type II diabetes, malaria, measles and sickle cell disease were revealed through docking of GC–MS identified phyto-compound ligands with candidate disease proteins. Of the 242 ligands, three dimensional structures of 47 compounds had to be drawn using ChemSketch and the remaining structures were retrieved from PubChem and docked with the active sites of candidate proteins. The molecules identified through docking were further subjected to ADMET analysis and promising drug candidates were identified for each disease. This paper presents a precise account of the chemoprofile of pigeon pea leaves, stems and seeds, interaction of these molecules with target proteins and suggests 26 highly potential molecules which are drug candidates for multiple human diseases. Pigeon pea seeds are especially proven as invaluable source for therapeutic molecules.

Members of the genus Lathyrus are used as food and in traditional drug formulations. In order to find new sources of biologically-active compounds, chemical and biological profiles of two Lathyrus species (L. czeczottianus and L. nissolia) were investigated. Chemical profiles were evaluated by HPLC-ESI-MSn, as well as by their total phenolic and flavonoid contents. In addition, antioxidant, enzyme inhibitory, and cytotoxic effects were also investigated. Antioxidant properties were tested by using different assays (DPPH, ABTS, CUPRAC, FRAP, phosphomolybdenum, and metal chelation). Cholinesterases (AChE and BChE), tyrosinase, α-amylase and α-glucosidase were used to evaluate enzyme inhibitory effects. Moreover, vitexin (apigenin-8-C-glucoside) and 5-O-caffeoylquininic acid were further subjected to molecular docking experiments to provide insights about their interactions at molecular level with the tested enzymes. In vitro cytotoxic effects were examined against human embryonic kidney cells (HEK293) by using iCELLigence real time cell analysis system. Generally, L. czeczottianus exhibited stronger antioxidant properties than L. nissolia. However, L. nissolia had remarkable enzyme inhibitory effects against cholinesterase, amylase and glucosidase. HPLC-ESI-MSn analysis revealed that flavonoids were major components in these extracts. On the basis of these results, Lathyrus extracts were rich in biologically active components; thus, these species could be utilized to design new phytopharmaceutical and nutraceutical formulations.

Background: The world pandemic COVID-19 caused by SARS-CoV-2 is currently claiming thousands of lives. Flavonoids abundantly present in the fruits and vegetables, especially quercetin, are shown to have antiviral activities. Main text: This paper reviews the capability of the plant flavonoid quercetin to fight the novel coronavirus and the possibility for drug development based on this. The mode of action explaining the known pathways through which this molecule succeeds in the antiviral activity, action of quercetin on SARS-CoV-2 main protease 3CL pro , antiviral activities of its derivatives on human viruses, effect of combination of zinc co-factor along with quercetin in the COVID-19 treatment, and the regulation of miRNA genes involved in the viral pathogenesis are discussed. Proof for this concept is provided following the virtual screening using ten key enzymes of SARS-CoV-2 and assessing their interactions. Active residues in the 3D structures have been predicted using CASTp and were docked against quercetin. Key proteins 3CL pro , spike glycoprotein/ human ACE2-BOAT1 complex, RNA-dependent RNA polymerase, main peptidase, spike glycoprotein, RNA replicase, RNA binding protein, papain-like protease, SARS papain-like protease/ deubiquitinase, and complex of main peptidase with an additional Ala at the N-terminus of each protomer, have shown the binding energies ranging between − 6.71 and − 3.37 kcal/ Mol, showing that quercetin is a potential drug candidate inhibiting multiple SARS-CoV-2 enzymes. Conclusion: The antiviral properties of flavonoid and the molecular mechanisms involved are reviewed. Further, proof for this concept is given by docking of key proteins from SARS-CoV-2 with quercetin.

Hematologic malignancies account for a substantial percentage of cancers worldwide, and the heterogeneity
and biological characteristics of leukemias and lymphomas present unique therapeutic challenges. Although treatment
options exist for most of these diseases, many types remain incurable and the emergence of drug resistance is pervasive.
Thus, novel treatment approaches are essential to improve outcome. Nearly half of the agents used in cancer therapy todayare either natural products or derivatives of natural products. The enormous chemical diversity in nature, coupled with millennia of biological selection, has generated a vast and underexplored reservoir of unique chemical structures with
biologic activity. This review will describe the investigation and application of natural products derived from higher
plants in the treatment of leukemia and lymphoma and the rationale behind these efforts. In addition to the approved vinca
alkaloids and the epipodophyllotoxin derivatives, a number of other plant compounds have shown promise in clinical
trials and in preclinical investigations. In particular, we will focus on the discovery and biological evaluation of the plantderived
agent silvestrol, which shows potential for additional development as a new therapeutic agent for B-cell
malignancies including chronic lymphocytic leukemia.

Aromatic herbal remedies, hydrosols, and essential oils are widely used for women's hormonal health. Scientific investigation of their major constituents may prevent unwanted infertility cases, fetal abnormalities, and drug-herb interactions. It also may lead to development of new medications. A list of 265 volatile molecules (mainly monoterpenes and sesquiterpenes) were prepared from a literature survey in Scopus and PubMed (2000-2019) on hydrosols and essential oils that are used for women's hormonal and reproductive health conditions. The PDB (protein data bank) files of the receptors (136 native PDB files) that involve with oxytocin, progesterone, estrogen, prolactin, acetyl choline, androgen, dopamine, human chorionic gonadotropin, luteinizing hormone, follicle-stimulating hormone, aromatase, and HER2 receptors were downloaded from Protein Data Bank. An in silico study using AutoDock 4.2 and Vina in parallel mode was performed to investigate possible interactions of the ligands with the receptors. Drug likeliness was investigated for the most active molecules using DruLiTo software. Aristola-1(10),8-diene, bergapten (5-methoxypsoralen), a-bergamotene, bicyclogermacrene, a-bisabolol oxide A, a-bisabolone oxide, p-cymen-8-ol, 10-epi elemol, a-elemol, b-eudesmol, 7-epi-b-eudesmol, ficusin, b-humulene, methyl jasmonate, nerolidol, pinocarvone, (þ)-spathulenol, and thujone had better interactions with some androgen, aromatase, estrogen, progesterone, HER2, AChR, and/or dopamine receptors. Most of these molecules had an acceptable drug likeliness except for a-bergamotene, bicyclogermacrene, b-humulene, and aristola-1(10),8-diene. Some volatile natural molecules can be considered as lead compound for drug development to treat hormonal conditions.

Propolis is a natural product with a plethora of biological effects, utilized by traditional medicine since antiquity. However, its application as a pharmaceutical is hindered by its variable composition and difficult standardization. CAPE has been shown to be a major component of propolis, with a large contribution to its pharmacological effects, among which the anti-inflammatory, antioxidant and antineoplastic have been attracting most attention. The current review article aims to present the cornerstone pharmacological studies of CAPE throughout the years, following its discovery, which confirmed its primary importance among propolis constituents and opened the path to its intensive research as a potential pharmaceutical. We present the diversity of drug delivery systems of CAPE, which have been developed to improve its efficacy in in vitro and in vivo disease models and discuss their primary promises and weaknesses. The increased interest in recent years over more practical approaches of CAPE research such as its pharmaceutical formulation comes to show that it has a potential to become commercialized as a pharmaceutical.

The biological activities of 4 medicinal plants (Acokanthera oppositifolia, Plantago lanceolata, Artemisia vulgaris and Conyza canadensis) were investigated. These plant extracts were subjected to screening for their possible effects as analgesic, and anti-inflammatory agents. The plant materials (only leaves were used in this study) were used in 4 solvents (acetone, ethyl acetate, chloroform and hexane). Plantago lanceolata hexane leaf extract inhibited cyclooxygenase-2 (COX-2) activity with an IC50 value of 0.41 µg/mL. Quercetin, positive control in this study inhibited COX-2 with a recorded IC50 = 8.39 µg/mL. However, the COX-1 inhibition by same extract indicated an IC50 of 68.99 µg/mL compared to the positive control (quercetin), whose activity was represented with an IC50 value of 4.6 µg/mL. The lipoxygenase assay indicated that Plantago lanceolata hexane extract and Acokanthera oppositifolia acetone extract were the most active samples with an IC50 of 4.75 µg/mL and 7.73 µg/mL. Plantago lanceolata hexane extract was the most active in all enzyme inhibitions, revealing the great potential it presents as a source of new anti-oxidative, analgesic and anti-inflammatory drugs, with less adverse effects.

Extended release formulation of Tramadol Hydrochloride based on osmotic technology was developed and evaluated. Target release profile was selected and different variables were optimized to achieve it. Formulation variables such as osmotic agent, plasticizer and coating thickness of semi-permeable membrane were found to markedly affect drug release. Tramadol hydrochloride release was directly proportional to the level of osmogent and plasticizer but inversely proportional to the level of coating thickness of semi-permeable membrane. Drug release from developed formulation was independent of pH and agitation intensity but dependent on osmotic pressure of release media. The optimized formulation was compared with marketed product CONTRAMAL SR and accelerated stability study was also carried out for 6 months.

Ethnopharmacological relevance: Neurological diseases are rising all around the world. In a developing country such as Togo, although plant-based medicines are the only means, still very little is known regarding the nature and efficiency of medicinal plants used by indigenous people to manage central nervous system (CNS) disorders. Aim of the study: This study, an ethnobotanical survey, aimed to report plant species used in traditional medicine (TM) for the management of various CNS disorders in Togo. Materials and methods: 52 traditional actors (TA) including 33 traditional healers (TH) and 19 medicinal plant sellers (MPS) were interviewed, using a questionnaire mentioning informants' general data and uses of medicinal plants. Results: The present study reports 44 medicinal plant species distributed into 26 families, mentioning scientific and common local names, plant organs used, preparation method, root of administration and putative applications. Conclusion: It appears that there is a real knowledge on medicinal plants used for traditional treatment of CNS disorders in Togo and that the local flora abounds of potentially neuroactive plants which could be useful for the discovery of antipsychotic or neuroprotective molecules.

Background: Diabetes mellitus is a metabolic disorder of glucose metabolism and management of blood glucose level is the hallmark in the treatment of this disease. The present study investigated chemical composition, in vitro antioxidant and antidiabetic activity of different fractions of 80% methanol Piper guineense leaves extract. Materials and methods: The crude methanolic extract of P. guineense was obtained following 80% methanol cold extraction and was successively partitioned with dichloromethane (DCM), ethyl acetate (EtOAc), n-butanol (nBuOH) and aqueous solvents to give four fractions. The chemical composition of the fractions from P. guineense was determined using gas chromatography coupled with mass spectrometry (GC-MS) and their potentials as antioxidant and anti-diabetes were evaluated. Results: The percentage yields were 3.16, 2.22, 0.68 and 0.66% (w/w) in n-butanol, DCM, aqueous and ethyl acetate fractions of P. guineense methanolic extract, respectively. The GC-MS analyses identified a total of 71 and 34 phytochemicals in n-butanol and ethyl acetate fractions respectively. Tributyl acetylcitrate (10.95%) and phytol (9.11%) were the major components in the n-butanol fraction while ethyl piperonyl cyanoacetate (27.35%) and phytol (15.17%) were the major constituents in the ethyl acetate fraction. Ethyl acetate fraction had the highest ferric reducing antioxidant power with a value of 53.96 ± 0.40 mgAAE/g while n-butanol fraction possessed highest total antioxidant power (9.98 ± 0.15) followed by aqueous fraction (9.72 ± 0.02). The ethyl acetate and n-butanol fractions with IC 50 value of 0.24 ± 0.07 and 0.83 ± 0.15 μg/mL respectively elicited significant inhibitory activities against α-glucosidase while only n-butanol fraction (IC 50 = 0.33 ± 0.09 μg/ml) exhibited appreciable inhibition against α-amylase activity. However, none of the four fractions showed significant inhibitory activity towards dipeptidyl-peptidase-IV. Conclusion: n-butanol and ethyl acetate fractions of 80% methanol P. guineense leaves extract can be a potential source of bioactive compounds of pharmacological importance in the management of diabetes.

Multiple studies have been recorded on the synthesis and design of multi-aim anti-Alzheimer molecules. Using dual butyrylcholinesterase/acetylcholinesterase inhibitor molecules has attracted more interest in the therapy for Alzheimer's disease. In this study, a tannic acid compound showed excellent inhibitory effects against acetylcholine esterase (AChE), α-glycosidase, α-amylase, and butyrylcho-linesterase (BChE). IC 50 values of tannic acid obtained 11.9 nM against α-glycosidase and 3.3 nM against α-amylase, respectively. In contrast, K i values were found of 50.96 ± 2.18 µM against AChE and 53.17 ± 4.47 µM against BChE. α-Glycosidase inhibitor compounds can be utilized as a novel group of antidiabetic drugs. By competitively decreasing glycosidase activity, these inhibitor molecules help to hamper the fast breakdown of sugar molecules and thereby control the blood sugar level. K E Y W O R D S anticholinergics, antidiabetic, enzyme inhibition, metabolic enzymes, tannic acid

Background: Rhus trilobata Nutt. (Anacardiaceae) (RHTR) is a plant of Mexico that is traditionally used as an alternative treatment for several types of cancer. However, the phytochemical composition and potential toxicity of this plant have not been evaluated to support its therapeutic use. Therefore, this study aimed to evaluate the biological activity of RHTR against colorectal adenocarcinoma cells, determine its possible acute toxicity, and analyze its phytochemical composition. Methods: The traditional preparation was performed by decoction of stems in distilled water (aqueous extract, AE), and flavonoids were concentrated with C 18-cartridges and ethyl acetate (flavonoid fraction, FF). The biological activity was evaluated by MTT viability curves and the TUNEL assay in colorectal adenocarcinoma (CACO-2), ovarian epithelium (CHO-K1) and lung/bronchus epithelium (BEAS-2B) cells. The toxicological effect was determined in female BALB/c mice after 24 h and 14 days of intraperitoneal administration of 200 mg/kg AE and FF, respectively. Later, the animals were sacrificed for histopathological observation of organs and sera obtained by retro-orbital bleeding for biochemical marker analysis. Finally, the phytochemical characterization of AE and FF was conducted by UPLC-MS E . Results: In the MTT assays, AE and FF at 5 and 18 μg/mL decreased the viability of CACO-2 cells compared with cells treated with vehicle or normal cells (p ≤ 0.05, ANOVA), with changes in cell morphology and the induction of apoptosis. Anatomical and histological analysis of organs did not reveal important pathological lesions at the time of assessment. Additionally, biochemical markers remained normal and showed no differences from those of the control group after 24 h and 14 days of treatment (p ≤ 0.05, ANOVA). Finally, UPLC-MSE analysis revealed 173 compounds in AE-RHTR, primarily flavonoids, fatty acids and phenolic acids. The most abundant compounds in AE and FF were quercetin and myricetin derivates (glycosides), methyl gallate, epigallocatechin-3-cinnamate, β-PGG, fisetin and margaric acid, which might be related to the anticancer properties of RHTR. Conclusion: RHTR exhibits biological activity against cancer cells and does not present adverse toxicological effects during its in vivo administration, supporting its traditional use.

There have been no reports published on the rare Echinops taeckholmiana growing wildly in Egypt. So, this study aimed to preserve it through method optimization of in vitro seed germination, besides callus formation from induced seedlings. Chemical profiling using gas chromatography-mass spectrometry (GC-MS) analysis of the n-hexane fraction afforded 29 identified components, mainly fatty acids esters, sesquiterpenes, triterpenes, one thiophene, and bis(2-ethylhexyl) phthalate. Ultra-performance liquid chromatography-electron spray ionization/tandem mass spectrometry (UPLC-ESI/MS-MS) analysis of total alcoholic root and induced calli extracts resulted in 68 metabolites. Taraxeryl acetate, β-sitosterol, stigmasterol-3β-D-glucoside, and 1,1,1-kestopentaose were identified from the defatted root extract, which inhibited α-amylase (IC 50 54.6 μg/mL) and α-glucosidase (60.4 μg/mL) enzymes compared with acarbose (IC 50 values of 30.57 and 34.71 μg/mL, respectively). Moreover, it showed moderate activity against HepG2 (IC 50 31.1 ± 1.4 μg/mL) and no activity against M-NFS-60 cell lines compared to cisplatin (IC 50 3.25 ± 1.4 and 8.37 ± 0.25, respectively).

ABSTRACT
Echium amoenum Fisch. and Mey. (Boraginaceae) is a plant which is used widely in Iranian folk medicine, especially for anxiety and depression. In
this study, published scientifc reports about the composition and pharmacological properties of this plant were reviewed. The electronic databases
including Google Scholar, PubMed, ScienceDirect, Scopus, Web of Science, and Scientifc Information Database were searched from 1970 to May
2016 and the data were summarized.Effcacy of E. amoenum (especially petals of E. amoenum) was studied in different in vitro, in vivo, and clinical
evaluations. Furthermore, some chemical compounds such as rosmarinic acid, echimidine, and cyanogenic glycosides were isolated from E. amoenum
petals. According to the results, E. amoenum showed various biological activities such as antimicrobial, antiviral, antioxidant, antidiabetic, analgesic,
immunomodulatory, and anxiolytic effects. Clinical studies on E. amoenum showed effectiveness of this plant in depression and anxiety disorders.
More clinical trials are recommended for evaluating different benefcial effects of this plant in human models and synthesis of new drugs from the active
ingredients of this plant in the future.
Key words: Biological activities, clinical, depression, chemical compound, Echium amoenum, in vivo, in vitro

Pachycereus marginatus (DC.) Britton & Rose and Ibervillea sonorae (S. Watson) Greene have been used in the Mexican traditional medicine for the treatment of various diseases, including cancer. The present study aims to investigate the cytotoxic activity of these plants against a murine lym-phoma. Soxhlet extraction of dried and powdered plant material was performed with methanol. Also, a further partitioning of these methanolic extracts with hexane and ethyl acetate was achieved. The in vitro cytotoxic activity against the murine lymphoma L5178Y-R cell line was assessed via the colorimetric MTT assay. The methanol extract from P. marginatus exhibited high cytotoxic activity (up to 94%) at concentrations ranging from 3.9 to 500 µg/mL; however, hexane and ethyl acetate partitions from this methanolic extract showed lower but significant (p < 0.05) concentration-dependent cytotoxicity (hexane partition up to 94% at 500 µg/mL; ethyl acetate partition up to 94% at 65.5 µg/mL). The methanolic extract and partitions derived from I. sonorae also showed significant (p < 0.05) and concentration-dependent cytotoxicity against L5178Y-R cells at concentrations ranging from 7.81 to 500 µg/mL (methanolic extract up to 63% at 500 µg/mL; hexane partition up to 76% at 250 µg/mL; ethyl acetate partition up to 73% at 500 µg/mL). These results demonstrate that the methanol extracts and partitions from P. marginatus and I. sonorae possess significant cytotoxic activity against the murine lymphoma L5178Y-R and validate the ethnobotanical use of these plants for the treatment of diseases consistent with cancer sympto-matology. Previous scientific reports describe the isolation of isoquinoline alkaloids of P. margi-R. Quintanilla-Licea et al. 1522 natus as well as cucurbitacins from I. sonorae, phytochemicals that could be responsible for their observed cytotoxic activity in this research. The direct extraction with methanol of medicinal plants allows extracting of both high and low-polarity compounds, contrary to the simple extraction with water that only allows obtaining compounds of high polarity. The subsequent partition of the methanol extract with a solvent of low polarity (hexane) and another of medium polarity (ethyl acetate) allows making a preliminary fractionation of the bioactive molecules present in the plant that will facilitate the bioguided chromatographic isolation of the pure compounds responsible for the biological activity of the plant.

High-performance liquid chromatography-diode array detection-electrospray ionization multi-stage mass spectrometry (HPLC-DAD-ESI-MSn) is considered to be a very valuable tool for the characterization of compounds found in trace amounts in natural matrices, as their previous isolation and clean-up steps can be avoided. Micro-scale separation increases the potential of this analytical technique, allowing the determination of compounds in reduced samples. Spodoptera littoralis represents a major challenge to Solanaceae plants, as it is one of the most deleterious pests. The S. littoralis/Lycopersicon esculentum system was studied for the first time concerning glycoalkaloids and phenolics. Using HPLC-DAD-ESI-MSn we were able to characterize 15 phenolic compounds in L. esculentum leaves. Nine of them are reported for the first time. Some differences were found between leaves of cerasiforme and 'Bull's heart' varieties. However, in the materials of S. littoralis (larvae, adults, exuviae and excrements) reared in both L. esculentum leaves no phenolics were identified. α-Tomatine was the main glycoalkaloid in the host plant. The glycoalkaloid composition of the different S. littoralis materials was distinct, with α-tomatine and dehydrotomatine being the main detected compounds in larvae and excrements. These results add knowledge to the ecological interaction in this insect/plant duo, for which it is hard to obtain considerable sample amounts. Copyright © 2011 John Wiley & Sons, Ltd.

Rutin is one of important bioflavonoids and biomarker that helps to increase the quality of the herbal product. It has a wide variety of pharmacological applications such as neuroinflammation, anti-hypercholesterolemic, neuroprotective, cardioprotective, wound healing, radioprotective, nephroprotective, hepatoprotective, antiplasmodial, antiarthritic, antiviral, antihypertensive, Antinociceptive, antimicrobial, gastroprotective, antiosteoporotic, anticancer, diuretic and anticonvulsant effect. The current review article helps to identify the current and future prospects of rutin. Most of the previous studies were more focus on their pharmacological activities and to understand their mechanism of action but less focus on its clinical trial, commercial potential and formulation development. This review article documents the pharmacological activities, standardization methods and formulation development over the last six years.

Putrescine N-methyltransferase (PMT) is a key enzyme of plant secondary metabolism at the start of the specific biosynthesis of nicotine, of tropane alkaloids, and of calystegines that are glycosidase inhibitors with nortropane structure. PMT is assumed to have developed from spermidine synthases (SPDS) participating in ubiquitous polyamine metabolism. In this study decisive differences between both enzyme families are elucidated. PMT sequences were known from four Solanaceae genera only, therefore additional eight PMT cDNA sequences were cloned from five Solanaceae and a Convolvulaceae. The encoded polypeptides displayed between 76% and 97% identity and typical amino acids different from plant spermidine synthase protein sequences. Heterologous expression of all enzymes proved catalytic activity exclusively as PMT and K cat values between 0.16 s−1 and 0.39 s−1. The active site of PMT was initially inferred from a protein structure of spermidine synthase obtained by protein crystallisation. Those amino acids of the active site that were continuously different between PMTs and SPDS were mutated in one of the PMT sequences with the idea of changing PMT activity into spermidine synthase. Mutagenesis of active site residues unexpectedly resulted in a complete loss of catalytic activity. A protein model of PMT was based on the crystal structure of SPDS and suggests that overall protein folds are comparable. The respective cosubstrates S-adenosylmethionine and decarboxylated S-adenosylmethionine, however, appear to bind differentially to the active sites of both enzymes, and the substrate putrescine adopts a different position.

Objective: The objective of this research was to isolate important secondary metabolites of Diospyros montana (Roxb.) leaves belonging to the family Ebenaceae. Methods: In this study, we investigated the chemical composition of a pentacyclic triterpenes fraction from the leaves of D. montana. Leaves were exhaustively extracted with ethanol and fractionated into petroleum ether, chloroform, and ethyl acetate extracts. The various fractions were further analyzed for phytochemical composition and HPTLC fingerprinting. The fractions were subjected to TLC and spectral analysis by IR, Mass, and 1 HNMR and 13 CNMR spectra to characterize isolated compounds. Results: The chemical examination of the leaves of D. montana (Roxb.) afforded the isolation of two compounds on column chromatography. These two compounds were confirmed by comparing their chemical and spectral data with that of published works of literature. Conclusion: The author could isolate a significant amount of Pentacyclic triterpenes: oleanolic acid and β-amyrin from the leaves of D. montana. Further preclinical studies may be extended to elucidate their mechanism.

Analysis of crude methanolic extracts of fresh khat (Cathaedulis) by liquid chromatography/mass spectrometry (LC/MS) revealed the presence of 62 cathedulin alkaloids (compared with 15 published structures). Many cathedulins generated doubly protonated molecules following electrospray ionisation and the ratio of doubly to singly protonated species could be manipulated by adjusting the electrospray capillary position and source conditions. By selecting the doubly protonated species for serial mass spectrometric analysis (MS/MS), it was possible to use an ion trap mass spectrometer to observe singly charged product ions at lower m/z values than ion trap MS/MS analysis of [M+H]+ would have allowed. These spectra were particularly valuable in elucidating the acylation patterns of cathedulins where MS/MS analysis of [M+H]+ resulted in loss of a large neutral species to yield a small singly charged fragment below the lower limit for ion trapping. Acylation patterns for most of the 62 cathedulins are proposed from mass spectrometric analysis, and the data obtained for a major unreported cathedulin of mass 1001 Da suggest that it belongs to a new group of cathedulins having a cathate dilactone bridge but not an evoninate bridge. Copyright © 2003 John Wiley & Sons, Ltd.

Economic development in southwest China and the increasing use of traditional Chinese medicine (TCM) worldwide have led to intensified collection of native medicinal plants. Fritillaria cirrhosa D. Don (Chuan Bei Mu), commonly used for the treatment of cough in TCM, is endemic to the Hengduan Mountain region of southwest China and is under increasing pressure from over-collection and decreasing suitable alpine habitat. The bioactive compounds in F. cirrhosa bulbs, isosteroidal alkaloids, are greatly influenced by environmental conditions and fluctuate in content and concentration with plant age and reproductive stage. Aiming at obtaining useful information for the sustainable management of wild F. cirrhosa populations, we evaluated how the phytochemical composition of F. cirrhosa bulbs varies at various stages of plant reproductive development. Using chemical methods and high performance liquid chromatography, two major bioactive alkaloids were extracted and analyzed from F. cirrhosa bulb samples collected throughout the Hengduan Mountain region. Plant reproductive stage was found to affect the concentration of bioactive alkaloids in F. cirrhosa bulbs. Bulb alkaloid concentration was highest during the early stages of fruit development and decreased significantly with fruit maturation. These results lend biochemical support to the practice of harvesting F. cirrhosa during the early stages of plant senescence (i.e., early fruit development).

Aconitum laciniatum is used in Bhutanese traditional medicine for treating various chronic infections and inflammatory conditions. We carried out in-depth isolation and characterization of the phytochemicals from the root component and determined the anti-inflammatory effects of the isolated compounds against chemically-induced colitis in mice. Five diterpenoid alkaloids - pseudaconitine, 14-veratroylpseudaconine, 14-O-acetylneoline, neoline, and senbusine A - were isolated from A. laciniatum for the first time. Two of the alkaloids were tested for anti-inflammatory properties in the TNBS-induced colitis model in mice. Various parameters were measured to assess pathology including weight loss, clinical and macroscopic scores, histological structure and IFN-γ production in the gut. Of the two alkaloids tested, 14-O-acetylneoline showed significant protection against different parameters of colitic inflammation. Compared to control mice that received TNBS alone, mice treated with 14-O-acetylneoline experienced significantly less weight loss and had significantly lower clinical scores, macroscopic pathology and grades of histological inflammation. Moreover, colonic IFN-γ mRNA levels were significantly reduced in mice that received 14-O-acetylneoline compared to control mice that received TNBS alone. This alkaloid is now considered a novel anti-colitis drug lead compound.

High dietary intake of fruits and vegetables rich in phytochemicals, particularly those with antioxidant activity, has been linked to reduced risks of many chronic diseases including cancer and cardiovascular diseases. Value-added foods and nutraceuticals containing such bioactive phytochemicals have been popular and made available in the market. Many factors affect the phytochemical concentration in fruits including farming practices, environmental factors and microclimate including the production methods, fruit maturity, and pre- and post-harvest handling of the fruits, but the genetic factor probably has the greatest effect on the biosynthesis of antioxidant secondary metabolites. A large variation of antioxidant concentrations exists within apple, strawberry, and raspberry cultivars and breeding lines, and it is possible to use this as a marker to develop new lines. The increase and/or decrease in phytochemical can both be useful in designing fruits: elevated concentration of antioxidants could extend the shelf life and reduce the incidence of diseases; and modulation of specific antioxidants can be use as a tool to change the specific quality characteristics of a fruit. Several examples like new raspberries and strawberries rich in phytochemical and post-cut non-browning apples low in certain antioxidants will be presented and discussed.

Perilla frutescens, perilla is a functional food, spice and medicinal herb and ornamental plant in the family of Lamiaceae. Thus, macro-morphological characteristics, phenolic acids, antioxidants of twelve accessions of P. frutescens grown under open field were studied. High polymorphism was found among the perilla accessions and macroscopic features of perilla genotypes showed variable results. Perilla can be classified into two clearly phenotypes green and purple, within these two other colours were appeared. A good level of biomass production was recorded for JTD3, 203P, PS2, 203P respectively. Principal component analysis was performed to cluster phenolic acids. GB phenotype exhibited the major content of polyphenols, followed by JTD3 then J1. Regarding antioxidant capacity, JTD3 showed the highest value followed by 203P and GB respectively. The HPLC analysis showed that the most abundant phenolic acids were ellagic acid which is accumulated in a higher percentage in NP606, 588P and JTD3 cultivars respectively, followed by salicylic acid and gallic acid. This is the first report of cultivation of various Perilla varieties under open field environmental conditions, not only to increase productivity but also to improve the quality. Therefore, the present study results confirm the importance of the Perilla species for human consumption, therapeutic and ornamental purposes.

The present investigation deals with the nutritional, phytochemical, antioxidant and antibacterial activity of dried fruit of fig (Ficus carica) commonly known as &quot; Anjir &quot; in India. The nutritional profiling of the dried fig fruit indicates that it is a good source of carbohydrates and minerals like strontium, calcium, magnesium, phosphorus and iron. It has average protein and dietary fiber content with very low amount of fat. Phytochemistry of the fruit revealed the presence of total phenolics, flavonoids, alkaloids and saponins and other secondary metabolites that contribute to its high antioxidant activity which was evident from ABTS and FRAP assays. Volatile components of fig fruit were identified through GC-MS and showed the presence of vitamin E, β-amyrin, stigmasterol, campesterol, oleic acid, isoamyl laurate and ϒ tocopherols majorly. The extract was also screened for antibacterial activity and showed zone of inhibition against Proteus mirabilis and Bacillus subti...

Boerhaavia diffusa is one of the renowned medicinal plants used to treat large number of human ailments as mentioned in Ayurveda, Charaka Samhita, and Sushrita Samhita. The Plant in whole or its peculiar parts (Aerial parts and Roots) have a numerous medicinal properties and are used by endemic and tribal people in India and Unani medicine in Arab countries to show Anti-bacterial, Anti-nociceptive, hepato-protective, hypo-glycemic, anti-proliferative, anti-estrogenic, anti-inflammatory, anti-convulsant, anti-stress and anti-metastatic activities and also in treatment of stress, dyspepsia, abdominal pain, inflammation, jaundice. Various phytochemical, pharmacological, experimental and clinical investigations are done on Boerhaavia diffusa by many scientist, researchers etc., to clearly understand the ancient Ayurvedic, Endemic and tribal usage of Boerhaavia diffusa. This paper includes the evidence-based overview of pharmacological and phytochemical properties of the aerial parts and the roots of Boerhaavia diffusa, which may be helpful to establish a standard natural drug for further research.