Cytotoxic activity and phytochemical standardization of Lunasia amara Blanco wood extract

Objective: To evaluate the cytotoxic activity of wood extracts of Lunasia amara Blanco(L. amara) and to perform further phytochemical standardization.Methods: The wood extracts of L. amara were assessed for cytotoxic activity by in vitro tetrazolium bromide(MTT) method against two human cancer cell lines, cervical cancer cells(He La) and breast cancer cells(T47D). Thin layer chromatography, Dragendorf,acetic anhydride-sulfuric acid and ferric chloride were used to detect alkaloids, steroids and polyphenols, respectively. Furthermore, quantitative determination of total alkaloid by ultra fast liquid chromatography-photodiode array detection using lunacrine as a marker compound was performed as well.Results: The ethyl acetate extract exhibited higher cell-growth inhibition than methanol and n-hexane extracts on He La and T47 D cancer line cells with the IC50 of 71.15 and79.04 mg/m L, respectively. Total alkaloid in ethyl acetate extract was counted as(10.46 ± 0.28)%(w/w), while lunacrine determined by ultra fast liquid chromatographyphotodiode array detection method was found to be(3.55 ± 0.26)%(w/w).Conclusions: The high total alkaloid and lunacrine concentration on the extract confirm the potential cytotoxic property of ethyl acetate wood extract of L. amara.

Phytochemical Analysis,Estimation of Quercetin,and in Vitro Anti-Diabetic Potential of Stevia Leaves Samples Procured from Two Geographical Origins

The current study used RP-HPLC to compare phytochemicals and estimate the bioactive constituents found in Stevia rebaudiana Bert.(SRB)leaves collected from two different geographical sources.SRB leaves were collected from Bangalore,Karnataka,India,and Reduit,Mauritius.Extracts were prepared using ethanol and aqueous solvents.Proximate analysis was used to evaluate moisture content,ash values,crude fibers,and extractive values.Following that,preliminary phytochemical screening was done on both ethanol leaves extracts,and subsequently total flavonoid content was determined.In addition,TLC chromatograms and RP-HPLC studies were performed on both plant extracts to determine the presence of flavonoid components in both leaves extracts,followed by in vitro anti-diabetic activity was performed with alpha amylase and alpha glucosidase enzymes against Acarbose as standard.Results revealed that both the extracts from two different geographical sources varied significantly with the yield,content of chemicals,and presence of quercetin(flavonoid)content when estimated through the RP-HPLC standardized method.Glycosides,flavonoids,proteins,steroids,saponins,terpenoids,and phenols were found in various concentrations during phytochemical screening.Among both zones,the ethanol leaves extract of SRB taken from Mauritius had a greater content of phytochemicals and a higher yield than other extracts due to the soil nature.The Mauritius sample had greater total flavonoid levels as well as more quercetin(0.92±0.011)than the other extracts.Following that,ethanol extract inhibited enzymes(alpha amylase,alpha glucosidases)more than aqueous extract,and this inhibition was dose dependent.Among them,the Mauritius ethanol sample showed higher anti-diabetic efficacy than the Indian sample,but this difference was not significant.Overall,SRB ethanol leaves extracts outperformed other leaves extracts in terms of yield,phytoconstituents,and total flavonoids.Overall,both SRB samples had high quercetin levels and possessed anti-diabetic potential,but they were greater in the Mauritius sample,demonstrating that plant traits are influenced by geographic location.

Antiviral activity of the dichloromethane extracts from Artocarpus heterophyllus leaves against hepatitis C virus

Objective: To determine anti-viral activities of three Artocarpus species: Artocarpus altilis, Artocarpus camansi, and Artocarpus heterophyllus(A. heterophyllus) against Hepatitis C Virus(HCV).Methods: Antiviral activities of the crude extracts were examined by cell culture method using Huh7it-1 cells and HCV genotype 2a strain JFH1. The mode of action for anti-HCV activities was determined by time-of-addition experiments. The effect on HCV RNA replication and HCV accumulation in cells were analyzed by quantitative reverse transcription-PCR and western blotting, respectively.Results: The dichloromethane(DCM) extract of A. heterophyllus exhibited strong antiHCV activity with an inhibitory concentration(IC_(50)) value of(1.5 ± 0.6) mg/mL without obvious toxicity. The DCM extracts from Artocarpus altilis and Artocarpus camansi showed moderate anti-HCV activities with IC_(50) values being(6.5 ± 0.3) mg/mL and(9.7 ± 1.1) mg/mL, respectively. A time-of-addition studies showed that DCM extract from A. heterophyllus inhibited viral entry process though a direct virucidal activity and targeting host cells. HCV RNA replication and HCV protein expression were slightly reduced by the DCM treatment at high concentration.Conclusions: The DCM extract from A. heterophyllus is a good candidate to develop an antiviral agent to prevent HCV grant reinfection following liver transplantation.

Plants used in traditional medicine for treatment of malaria by Tetunethnic people in West Timor Indonesia

To document the medicinal plants used for the treatment of malaria by the Tetun ethnic people in West Timor–Indonesia. Methods: The ethnobotany and anthropology methods were used in the field surveys. Ninety four informants from 29 villages of 15 sub-districts in Belu and Malaka were interviewed since April to December 2017. Medicinal plants specimen were collected from the field and identified according to taxonomic methods. Results: Ninety six medicinal plants species belong to 41 families were found to be used by the Tetun ethnic people in their traditional medicine for the treatment of malaria. These plants have been used in various formulas for drinking, massage, bath, inhalation or cataplasm. Strychnos ligustrina, Calotropis gigantea, Cleome rutidosperma, Physalis angulata, Alstonia spectabilis, Carica papaya, Melia azedarach, Alstonia scholaris, Jatropha curcas, Garuga floribunda, and Tamarindus indicawere the most cited plants. Conclusions: The documented plants are valuable sources for the future development of new drugs and strategies to support malaria eliminating programs that are culturally acceptable in these areas.

Ethnobotany,phytochemistry and pharmacological potential of Vitex negundo L.(five-leaved chaste tree):An updated review

In the past two decades,a shift in paradigm has been observed in the development of new drugs from the plants for the treatment of diseases.Many scientists are focusing on the evidence based use of medicinal plants to develop pharmacotherapy for various human ailments.An important medicinal plant that has caught the attention of researchers all over the globe is Vitex negundo Linn.This plant is commonly used in various traditional systems of medicine like Ayurveda,Chinese,Siddha and Unani to treat various diseases and has been the subject of extensive research studies lately.Its roots and leaves are widely used in various disorders and illnesses such as skin eczema,ringworm,liver disorders,spleen enlargement,rheumatic pain,gout,abscess,backache etc.Seeds are also used as folklore medicine in bronchitis,eye disorders,female reproductive disorders,cold,dropsy,malarial fever and as demulcent.The current article is an effort to compile an updated review to disseminate knowledge and information among the scientific fraternity covering the progress made in the pharmacology and phytochemistry of this useful medicinal plant.This review on a very important traditional medicine,Vitex negundo L.can serve as a reference to the scientific community for their future research on this plant.

Isolation and Characterization of Phytoconstituents from the Stems of Ichnocarpus frutescens

AIM: To study the chemical constituents of the stem part of Ichnocarpus frutescens. METHODS: The ethanolic extract of Ichnocarpus frutescens was used for the isolation of chemical constituents with the help of silica gel G and Sephadex column chromatography and their structures were elucidated on the basis of spectral data and chemical methods. RESULTS: Five compounds were isolated and identified as n-butyl oleate (1), n-octyl tetracontane (2), tetratriacontadiene (3), n-nonadecanyl benzoate (4), and benzocosanyl arachidate (5). CONCLUSION: Compound 5 is new; and compounds 1-4 are isolated from genus Ichnocarpus frutescens for the first time.

药用植物抗肝毒性的最新研究进展(英文)

肝脏损害是由于微循环障碍、肝细胞变性坏死而引起的肝功能异常,它影响到几乎每个年龄段人群肝脏细胞的重要生物活性,而常规用药来抑制肝脏损害是远远不够的。而且,由于对抗疗法所用药物往往具有肝毒性,反而加剧了肝脏功能的紊乱。为了寻找安全有效的替代药物,人们逐渐把目光转向了具有保肝作用的药用植物,并对其进行系统性的方法学研究和药用原理评估。药用植物治疗肝病具有悠久的历史,最早可追溯到公元前2100年的中国夏朝和古印度吠陀时期,但是能证明那个时期药用植物有效治疗肝病的证据却很难寻觅。本文旨在系统性地概述现今在临床治疗和实验研究中最常用以及最有效的保肝类药用植物。

毛萼厚壳树植物成分对关节炎TNF-α靶点的预测

目的类风湿性关节炎(RA)是一种涉及主要关节滑膜衬里的自身免疫性疾病。目前的治疗方法有明显的副作用。我们的研究通过计算机模拟来评估毛萼厚壳树植物成分对肿瘤坏死因子-α(TNF-α)的靶向作用。方法利用AutoDock Vina进行分子对接实验,以研究毛萼厚壳树植物成分与TNF-α(PDB ID:2AZ5)晶体结构的结合模式;随后,研究相互作用的氨基酸残基及其对活性成分抑制潜力的影响;进一步使用SwissADME和pkCSM进行药代动力学分析和毒性筛选。结果对接实验结果表明,与标准药物沙利度胺(−7.4 kcal/mol)相比,羽扇豆醇(−9.4 kcal/mol)和α-香树脂醇(−9.4 kcal/mol)对TNF-α的亲和力最强。其活性化学成分与保守的催化残基具有更好的相互作用,从而抑制或阻断RA中的TNF-α相关信号通路。此外,根据ADMET研究,这些植物化学物质的药代动力学和毒性参数均在可接受的范围内。结论植物成分靶向TNF-α的结合潜力显示出良好的结果。尽管如此,本研究鼓励毛萼厚壳树的传统应用,并为药物开发和临床治疗提供了重要的信息。

Enhancement of gut permeation of amoxicillin with Nigella sativa seed extract and its phytochemical screening

The seeds of Nigella sativa Linn.(Ranunculaceae), commonly known as Black cumin, are predominantly used as carminative, antispasmodic, and stimulant. The main objective of the present study was to evaluate the effect of N. sativa seed extract on the permeation of co-infused amoxicillin across the gut wall. The methanolic extract of N. sativa improved intestinal permeability of amoxicillin in in-vitro experiments in a dose-dependent manner. Two new glycosides, decanyl nigelloic acid diglucoside [n-decanyl-3-aldehydic-4-methoxy-5-hydroxy benzoate-5-β-D-glucofuranosyl(2→1)-β-D-glucopyranosyl-(2→1)-β-D-glucopyranoside]] and nigelabdienoyl triglucoside [homo-labd-5, 9(11)-dien-16-onyl-β-D-glucopyranosyl(2→1)-β-D-glucopyranosyl(2→1)-β-D-glucopyranoside], along with seven known fatty acid glycerides/esters, were isolated from the gut permeation enhancing extract. The structures of these new glycosides were elucidated by detailed spectroscopic analyses.

薄层色谱法提取和鉴定海州常山桐树叶中的化学标记物赤桐甾醇十六烷基酯(英文)

目的:赤桐甾醇十六烷基酯(clerosterol palmityl ester,CPE)是一种从海州常山桐(Clerodendrum phlomidis)树叶中提取的特殊的赤桐甾醇衍生物。鉴于这种物质的特殊性,本研究以CPE作为化学标志物,采用一种新的薄层色谱法鉴定海州常山桐树叶。方法:CPE的分离和量化采用薄层色谱法,流动相石油醚(60～80℃)与乙酸乙酯的体积比为95∶5(Rf0.64),硅胶60F254薄板层析检测。茴香醛浓硫酸试剂显色后使用光密度仪检测样品在527nm处的吸光度。结果:CPE在浓度范围100～500ng/孔的校正曲线呈线性分布。通过系统适用性检测,这种鉴定方法被证实具有很好的准确性和可重复性,特异性强并且具有较高的成本效益。结论:这种薄层色谱法能够有效地量化CPE的含量从而鉴定海州常山桐树叶及其衍生物。

Comparative phytochemical,thin layer chromatographic profiling and antioxidant activity of extracts from some Indian herbal drugs

Natural antioxidants play a significant role to prevent cell breaking and regenerate cells.Three plants native to India named dwarf morning-glory(Evolvulus alsinoides),Indian banyan(Ficus bengalensis)and chicory(Chicorium intybus)are used as medicine in India traditionally to treat diseases.The aim of this study is to evaluate and compare the antioxidant activity as well as to compare phytochemical profiles of the aqueous extracts of the selected three plants.The dried plant powder was extracted with ethanol individually by using the Soxhlet method for eight hours and the solvent was evaporated under reduced pressure.Similarly,the air-dried powder was ex-tracted with water,and the water was evaporated.The thin layer chromatography(TLC)profile of the extracts was determined by using TLC densitometer and the antioxidant activity was deter-mined by the conventional 2,2-diphenyl-1-picrylhydrazyl(DPPH)method.The TLC profile shows that there are no similarities of retention factor(R f)values among the plant extracts which means all three plants contain different chemical compounds.The antioxidant activities of the aqueous extracts at different concentrations show different antioxidant activities.Percentage inhibition is dose dependent,as doses are increasing then percentage inhibition is also increasing for all three plant extracts.Among the selected plants,the highest activity was found in C.intybus and the lowest was in E.alsinoides.The order of the antioxidant activity among the selected plants was C.intybus<F.bengalensis<E.alsinoides.Based on the TLC profile and antioxidant activities,the highest activity of the selected plant species was evaluated.

靶向TNF-α的植物抗炎先导化合物的计算机模拟筛选

目的通过计算机模拟进行分子对接,研究多种植物中的抗炎成分对肿瘤坏死因子α(TNF-α,一种参与炎症疾病的介质)的抑制作用。方法基于先前的研究,我们使用AutoDock Vina软件对不同药用植物的抗炎植物成分进行计算机模拟评估,以了解它们与TNF-α的结合模式(PDB ID:6OP0)。分子对接模拟分析中,网格箱(25×25×25)Å中心设为[-12.817×(-1.618)×19.009]Å,网格间距为0.375Å。此外,使用Discovery Studio Client 2020程序评估与靶标和配体氨基酸相关的二维和三维(2D和3D)氢键间的相互作用,并根据里宾斯基类药五规则和SwissADME数据库预测其理化性质,以支撑分子对接模拟结果。结果我们从选取的药用植物中筛选出200多种植物化合物与抗TNF-α蛋白结合,结合评分在-12.3至-2.5 kcal/mol范围内。其中,大黄素、芦荟大黄素、水黄皮籽素、紫花青素、附根含希米拉因、鞣花酸、欧前胡素、α-生育酚和八降葫芦素A表现出良好的结合亲和力,分别为-10.6、-10.0、-10.5、-10.1、-11.2、-10.3、-10.1、-10.1和-10.0 kcal/mol。此外,这些成分的吸收、分布、代谢、排泄及毒性(ADMET)特征参数均在正常范围内。结论根据初步研究结果,我们认为本研究选取的植物成分可以通过抑制TNF-α靶标成为良好的抗炎候选物。可以将这些化合物作为治疗炎症的新成分进行进一步优化和验证,以开发更加有效、安全的抗炎药物。

Evaluation of antiplasmodial properties in 15 selected traditional medicinal plants from India

Objective:The objective of this study was to evaluate the in vitro antiplasmodial properties against malaria parasite in 15 plants mentioned in Indian traditional medicine texts.Methods:In vitro antiplasmodial activity of methanolic extracts obtained from Indian traditional medicinal plants was evaluated on Plasmodium falciparum of FCK2 and INDO strains using schizont maturation inhibition assay and parasite lactate dehydrogenase inhibition assay.Results:Methanolic extracts of Adhatoda zeylanica,Embelia ribes,Piper nigrum and Plumbago zeylanica exhibited more than 50%inhibition in both the stains in schizont maturation inhibition assay.Methanolic extracts of seven medicinal plants exhibited antiplasmodial activity at half maximal inhibitory concentration(IC50)<100 mg/m L,and methanolic extracts of five medicinal plants exhibited antiplasmodial activity at IC50<50 mg/m L in P.falciparum lactate dehydrogenase(PfLDH)inhibition assay.A.zeylanica,E.ribes and P.nigrum exhibited promising antiplasmodial activity in PfLDH inhibition assay.A.zeylanica and E.ribes exhibited improved activity against resistant in comparison to sensitive strain.Conclusion:A.zeylanica and E.ribes were the most promising extracts from this study and deserve further investigation of their antiplasmodial properties.

Fatty acids of Pleurotus florida mushroom:Potential molecules for blood glucose control

In Vitro-In Vivo antidiabetic effect of Pleurotus florida mycelia was evaluated using enzymes,yeast cell and in streptozotocin induced type 2 diabetic(T2D)animal model.P.florida mycelia was prepared by submerged fermentation process.The fungal biomass was organically extracted using mixture of ethanol and water.Highest extractives yield of 14.3%w/w was obtained in hydroalcoholic solvent with dielectric constant-δvalue of 78.2(EX78).P.florida mycelia extract(EX 78)shows higher antioxidant power with 86.87%free radical scavenging activity and with 75.29 reducing power.In-vitroα-amylase inhibition,α-glucosidase inhibition and glucose uptake activity of EX 78 shows higher effectiveness.The P.florida mycelia extract(EX 78)is also found to be effective in controlling of blood glucose and insulin level in streptozotocin-nicotinamide induced T2D animals.The blood glucose was reduced to 216±6.21 mg/dl from 357±0.34 mg/dl and the insulin level was increased to 0.423±0.006 ng per mL from 0.164±0.03 ng/mL in P.florida treated animals.The higher fatty acids,C20-eicosane;C24-tetracosane and C30-squalene present in P.florida mycelium extract was found to be effective in inhibiting human intestinalα-glucosidase and pancreaticα-amylase.The P.florida mushroom is found to be effective in controlling high blood glucose elevated liver and cardiac enzymes.Consumption of this mushroom is suitable for controlling blood glucose level in person with hyperglycaemia.

Antimicrobial metabolites from marine microorganisms

Marine ecological niches have recently been described as "particularly promising" sources for search of new antimicrobials to combat antibiotic-resistant strains of pathogenic microorganisms. Marine organisms are excellent sources for many industrial products, but they are partly explored. Over 30 000 compounds have been isolated from marine sources. Bacteria, fungi, and cyanobacteria obtained from various marine sources secret several industrially useful bioactive compounds, possessing antibacterial, antifungal, and antimycobacterial activities. Sustainable cultivation methods for promising marine organisms and biotechnological processes for selected compounds can be developed, along with the establishment of biosensors for monitoring the target compounds. The semisynthetic modifications of marine-based bioactive compounds produce their new derivatives, structural analogs and mimetics that could serve as novel lead compounds against resistant pathogens. The present review focuses on promising antimicrobial compounds isolated from marine microbes from 1991-2013.