Phytochemical Study and Evaluation of the Antioxidant Activity of Extracts of the Roots of Chrysopogon nigritanus

In this work, we were interested in a medicinal plant named Chrysopogon nigritanus, belonging to the Poaceae family. In order to carry out this study, we were interested first in the phytochemical screening test, after having carried out the extraction with two solvents (water and isopropanol), to characterize the different families of metabolites present in the extracts. Then, the assays of polyphenols and flavonoids were carried out in order to quantify the contents of these two compounds in each extract. Finally, the antioxidant activity of the extracts was evaluated by three methods: the CUPRAC method, the trapping of the 2,2-diphenyl-1-picryl-hydrazyl radical (DPPH•) and the trapping of the ABTS•+ radical-cation (2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid)). The best antioxidant activities were obtained with the ABTS•+ radical scavenging with IC50 of 0.13 mg/mL for the aqueous extract and 0.19 mg/mL for the isopropanol extract. Based on these first results, an in-depth study is underway for various biological tests and the isolation of bioactive molecules.

Expression of recombinant human interleukin-29-Fc fusion protein in HEK293F cells and analysis of its anti-tumor activity in vitro / 中国生物制品学杂志

@#Objective To express recombinant human interleukin-29-Fc(rhIL-29-Fc) fusion protein in human embryonic kidney 293-F(HEK293F) cells and analyze its anti-tumor activity in vitro.Methods The recombinant expression plasmid UCOE-IL-29-Fc was constructed and transiently transfected into HEK-293F cells.After expression and purification,rhIL-29-Fc fusion protein was obtained and identified by SDS-PAGE and Western blot;Female Japanese white rabbits were immunized with rhIL-29 and rhIL-29-Fc protein subcutaneously in the left ear respectively,2 rabbits in each group,0.5 mg per rabbit.Blood samples were collected from the vein of right ear,and the serum was separated.The half-life was measured by ELISA and the anti-proliferation effect of rhIL-29-Fc protein on human colon cancer HT-29,human colon cancer HCT-116,human Burkkit lymphoma Daudi,human non-small cell lung cancer NCI-H1975,human small cell lung cancer NCI-H209,human esophageal cancer EC109 and human pancreatic cancer PANC-1 cells in vitro was detected by CCK-8 assay,and the inhibitory concentration 50(IC_(50)) was calculated.Results The recombinant expression plasmid UCOE-IL-29-Fc was constructed correctly as identified by double digestion and sequencing.After transient transfection into HEK-293 cells for 6 d,the culture supernatant was harvested.The relative molecular mass of the purified rhIL-29-Fc fusion protein was consistent with the expectation.The protein showed a specific binding reaction with mouse anti-human IL-29 monoclonal antibody with a concentration of 1.5 mg/ml and a purity of 93%.RhIL-29-Fc protein had a half-life of 25 h and showed different inhibitory effects on the proliferation of 7 kinds of tumor cells,and the IC_(50) on different cells was also different.Conclusion The rhIL-29-Fc fusion protein was successfully expressed in HEK-293F cells,and the half-life of the fusion protein was 20 h longer than that of rhIL-29.According to the different anti-tumor proliferation activity in vitro and IC_(50) results on 7 kinds of tumor cells,it was found that the anti-tumor activity of rhIL-29-Fc fusion protein was higher than that of rhIL-29.This study laid a foundation of the development of IL-29 protein in the treatment of tumors.

The study of the biological activities of Ziziphora clinopodioides

Abstract The aim of the current study was to determine the chemical constituents of essential oil and to study the antibacterial and antioxidant activities of essential oil and the extracts obtained from the raw material of Ziziphora wild growing in the floras of Armenia and Artsakh cultivated in the hydroponic conditions. The essential oils were obtained by the method of hydro-distillation. The determination of the essential oil constituents were performed by the GC-MS method. Agar disk diffusion method was used to study the antimicrobial activity of essential oils. The antioxidant activity determination was carried out DPPH test by the spectrophotometric method, at the same time IC50 was determined. The highest values of the essential oils yield (1.25 ± 0.01%) and IC50 13.83±0.218(x10-5)g/l) were received for the plant cultivated in hydroponic conditions. For the first time in the above studied samples, by the method of GC-MS more than 70 components were revealed. The results of the study showed that essential oils of Ziziphora exhibit antimicrobial activity and the extracts revealed relatively expressed antioxidant activity. The study results show the future prospects of the use of Ziziphora not only as the source of flavonoids and essential oils, but also antimicrobial and antioxidant agents.

Discovery of a potent and dual-selective bisubstrate inhibitor for protein arginine methyltransferase 4/5

Protein arginine methyltransferases (PRMTs) have been implicated in the progression of many diseases. Understanding substrate recognition and specificity of individual PRMT would facilitate the discovery of selective inhibitors towards future drug discovery. Herein, we reported the design and synthesis of bisubstrate analogues for PRMTs that incorporate a

Simulation Analysis of Occupancy Rates of Baicalein， Quercetin and Galangin on Target Sites of Xanthine Oxidase / 中国实验方剂学杂志

Objective:To simulate the occupancy rates of baicalein， quercetin and galangin on the target sites of xanthine oxidase <italic>in vivo</italic>. Method:In this experiment， the half inhibitory concentration （IC₅₀） of febuxostat， baicalein， quercetin and galangin against xanthine oxidase were determined by <italic>in vitro</italic> enzymatic reaction. Binding free energy was predicted by molecular docking technology and their association rate constant （k_on） and dissociation rate constant （k_off） were determined by surface plasmon resonance technology. Based on measured binding kinetic parameters （k_on and k_off） and extracted pharmacokinetic data， the target occupancy model <italic>in vivo</italic> was established. Result:The IC₅₀values of febuxostat， baicalein， quercetin and galangin were 0.002 7， 1.63， 0.38， 1.59 µmol·L^-1， respectively. The IC₅₀ of febuxostat was very close to that reported in the literature. The predicted curve of target occupancy rate <italic>in vivo</italic> of febuxostat was consistent with its duration of clinical efficacy. When single intragastric administration of long-circulating liposomes of quercetin with dose of 100 mg·kg^-1 in rats， the time of target occupancy rate >70% <italic>in vivo</italic> lasted for about 3.9 h. When rats were orally administered baicalein and galangin with dose of 200 mg·kg^-1， the time of target occupancy rate >50% <italic>in vivo </italic>lasted for about 10 h and 1.7 h， respectively. Conclusion:The prediction model of xanthine oxidase target occupancy constructed by drug target binding kinetics and <italic>in vivo</italic> pharmacokinetic curves can effectively evaluate the <italic>in vivo</italic> inhibitory activity of compounds against the target.

Review on the In Vitro Cytotoxicity Assessment in Accordance to the International Organization for Standardization (ISO)

@#Cytotoxicity is a predominant biological evaluation applied to search for a suitable and non-toxic bioactive compound and to determine the biocompatibility of medical devices-related human body. The broad usage of cytotoxicity tests leads to a robust establishment of cytotoxicity assays with high sensitivity and prompt results. In vitro assays are always prioritized over in vivo due to the reproducible data, reduce numbers of animal used and easily accessible material. Compounds concentration that execute 50% of cell population is determined by calculating the IC50. According to ISO10993, cytotoxicity tests must be performed to determine the biocompatibility of medical devices that has contact with human body. This is crucial to ensure the safety of research and its clinical use. Under the recommendation of ISO10995-Part 5, three categories of tests have been documented; extract elution, direct contact and indirect contact test. Each category plays significant role depending on the nature of experiment and sample used.

Effect Of Combination Of Aqueous Leaf Extracts Of Psidium Guajava Linn And Moringa Oleifera Lam On Diabetes Mellitus

Objective: To determine the anti-diabetic activity of combined aqueous extracts (1:1mixture) of dry leaves of Psidium guajava linn and Moringa oleifera lam as well as to compare the anti-diabetic activity of these plants by in vitro methods. Methods: In vitro alpha amylase inhibitory assay was performed on porcine alpha amylase and the absorbance was measured at 540 nm using a microplate reader and glucose diffusion inhibitory assay using dialysis membrane. Acarbose was used as the standard in the above mentioned methods. Results: The mixture (1:1) of aqueous plant extracts (at a concentration of 100µg/ml) of Psidium guajava linn and Moringa oleifera lam exhibited 72.08333% inhibition with IC50 value of 10.9µg/ml. The leaf extracts of Psidium guajava (at a concentration 100µg/ml) exhibited 71.23288% of a α amylase inhibitory activity with an IC50 values 19.883µg/ml whereas the leaf extracts of Moringa oleifera (at a concentration of 100µg/ml) exhibited 70.58824% of α amylase inhibitory activity with an IC50 value of 27.974 µg/ml. The Acarbose (standard drug) at a concentration of 100µg/ml showed 72.09302% inhibitory effect on the α amylase activity with an IC50 value 8.9µg/ml. In glucose diffusion inhibition assay the mixture of plant extracts exhibited 76.57% inhibition at 150 min which produces more effects than the two plants. The aqueous extract of Psidium guajava leaves exhibited maximum glucose diffusion inhibition (75.32%) at 150 min as well as Moringa oleifera leaf extract showed the maximum inhibition of 73.70% at the same time interval. For acarbose the percentage was 82.74 at 150 min. The interpretation of the results was done by one-way anova method. Conclusion: The combined extract of the leaves of the 2 plants was found to be more effective than individual plant extracts against diabetes. On comparison of two plants Psidium guajava was found to be more active against diabetes than Moringa oleifera. Also the potentiation effect shown by the combination of extract may be due to synergistic effect of the phytochemical constituents. As the 1:1 mixture of the aqueous extract is found to be more active, the combination of the two plants can be used to formulate drugs for treating diabetes.

Exploration Of Bioactive Components Of Thunbergia Coccinea, Its Pharmacognostic, Antioxidant, Gcms And Antihyperglycemic Studies

Objective: An effort currently made to appraise the preliminary phytochemical, pharmacognostic criteria, antioxidant, GCMS and antihyperglycemic investigations of the Thunbergia coccinea leaves. Thunbergia coccinea (T. coccinea) is an ornamental plant considerably practiced by the tribes of forest areas of Assam (INDIA) as an analgesic, antipyretic, anti-inflammatory, antidote, hepatoprotective, antidiabetic and detoxificant substance. Methods: A comprehensive literature survey was conducted to recognize the ethnomedicinal value of T. coccinea, which is currently grown practically in all provinces. The physicochemical constants like moisture content, ash values especially total ash, insoluble acid ash, water-soluble ash and foreign organic matter were determined for the assessment of the drug. Pharmacognostic parameters like fluorescence examination and microscopic characters of the leaf were studied that would serve to verify for contamination. The extract secured by maceration was subjected to the phytochemical inquiry to determine the existence of substances and their antioxidant activity. The antihyperglycemic characteristic of alcoholic extract of the leaf was examined with the inhibition of α-amylase and α-glucosidase enzymes. Gas Chromatography-Mass Spectrometry (GCMS) studies of alcoholic extract of the plant leaf have undertaken to get an insight into the therapeutic properties of the molecules present based on online PASS prediction. Results: Various physicochemical, microscopic parameters studied gave a clear distinguishing and identifying features of T. coccinea leaf. Phytochemical screening gave an insight into the secondary metabolites existing in the plant leaf through picturizing its therapeutic properties against various ailments. Both extracts of T. coccinea leaf showed enhanced antioxidant activities. Nevertheless, the alcoholic leaf extract has shown significant antioxidant activity with an IC50 of 171.38±2.51 μg/ml and AQTC an IC50 value of 206.29±4.5 μg/ml respectively by DPPH method. Further, ACTC showed a better-reducing potential with an IC50 value of 105.74±0.61 μg/ml in comparison with AQTC IC50 value of 203.702±0.97 μg/ml by FRP method. The inhibition potentiality of α-amylase and α-glucosidase was found to be 71.66 % and 83.74 %, respectively at 500 µg/ml that rationally an adequate remedy in the treatment of type-2 diabetes. GCMS studies of the alcoholic extract unveiled the presence of different molecules like Glycerol, tris (trimethylsilyl) ether, 3,7,11,15-Tetramethyl-2-hexadecen-1-ol, Undecanoic acid, Ethyl ester, Phytol in comparison with NIST library, thereby giving its predicted therapeutic properties like sugar phosphatase inhibitor, antifungal, phobic disorders treatment, antiviral and so on. Conclusion: The selected plant had many proven therapeutic traits and, possibly, successively united on to the sort of potential therapeutic plants. Besides, isolation and discoveries will lead to the detection of certain novel compounds, which will be of potential medicinal value.

In vitro study on the antioxidant activity of methanolic leaf extract of Carica papaya

Background: Newer drug research worldwide is now focusing on medicinal plants for ensuring health and vitality due to the seemingly safer side effect profile and abundance of plants in nature, compared to synthetic drugs. Antioxidants are vital in preventing free radical induced tissue damage. The purpose of the present study is to evaluate the antioxidant activity of the methanolic extract of the leaves of Carica papaya using 1,1-diphenyl-2-picrylhydrazine (DPPH). Phytochemical tests proved the presence of bioactive ingredients in the extract.Methods: DPPH free radical assay, one of the most accurate methods for evaluating antioxidant activity, was used to evaluate the antioxidant activity of methanolic extract of leaves of C. papaya.Results: The methanolic leaf extract of C. papaya showed antioxidant property with free radical scavenging activity increasing with increase in concentration. The IC50 value of methanolic extract was 213.68 礸m/ml. Ascorbic acid was used as control.Conclusions: Oxidative stress has been linked to heart disease, cancer, immune deficiency. Antioxidants as suggested from various studies may reduce the risk of such diseases. The utility of C. papaya in the treatment of heart disease, cancer and immune deficiency will have to be proved by detailed evaluation of its pharmacological properties.

Effect of Paiteling on HeLa Cell Proliferation and Metastasis Ability and PI3K/Akt Signal Transduction Pathway / 中国实验方剂学杂志

Objective:To explore the effect of Paiteling on the proliferation，metastasis and invasion of HeLa cells and relevant proteins of phosphatidylinositol 3-kinase/protein kinase B (PI3K/Akt) signaling pathway. Method:① HeLa cells were divided into blank group and Paiteling concentration gradient groups (3.906，2.604，1.953，1.563，1.302，1.116，0.977 g·L-1). After drug intervention for 24 h，the cell morphological changes were observed under microscope. The cell viability was measured by thiazole blue (MTT) colorimetry，and the half inhibitory concentration (IC50) of Paiteling on HeLa cells was calculated. ② HeLa cells were divided into blank group，cisplatin group (0.01 g·L-1)，Paiteling high-dose group (2.974 g·L-1)，Paiteling medium-dose group (1.487 g·L-1) and Paiteling low-dose group (0.991 g·L-1). Cell proliferation and toxicity test (CCK-8) method was used to detect the effect of Paiteling on the proliferation ability of HeLa cells，scratch test was used to detect cell migration，and invasion test (Transwell) was used to detect changes in cell invasion ability. ③ Inhibitor LY294002 group (0.006 g·L-1) was added. Western blot (WB) was used to detect the expressions of Paiteling on PI3K，Akt，recombinant human B-cell lymphoma factor-xl (Bcl-xl)，and B-cell lymphoma/leukemia associated D protein (Bad). Result:① Compared with the blank group，microscopic observation showed that the number of cells in the treatment group was significantly reduced, and the cell morphology was incomplete. MTT experiments showed that Paiteling has a significantly inhibitory effect on HeLa cell proliferation (P<0.01). The IC50 of Paiteling on HeLa cells was calculated as 2.974 g·L-1. ② The CCK-8 experiment showed that compared with the blank group，all the drug-treated groups had an inhibitory effect on HeLa cell proliferation at 24，36，48 h (P<0.01), compared with the cisplatin group，middle and low-dose Paiteling groups showed a reduced inhibitory effect on HeLa cell proliferation at each time point (P<0.01). The scratch test showed that，compared with the blank group，each drug-added group could inhibit the migration ability of HeLa cells (P<0.01)，and the cell migration rate of the high-dose Paiteling group was lower than that of the cisplatin group (P<0.05). Transwell experiments showed that compared with the blank group，the number of membranes permeated by HeLa cells in each drug-treated group was decreased (P<0.01)，and the number of membranes permeated in the middle and low-dose Paiteling groups was increased compared with the cisplatin group (P<0.01). ③ Western blot showed that compared with the blank group，the expression levels of PI3K，Bcl-xl，and Akt in the high，medium，and low-dose Paiteling groups and the LY294002 group decreased (P<0.05，P<0.01)，while the expression of Bad increased (P<0.01). Compared with the high-dose Paiteling group，the PI3K，Akt，and Bcl-xl protein expressions were increased in the low-dose Paiteling group (P<0.01)，whereas Bad expression was decreased (P<0.01). Conclusion:Paiteling can inhibit HeLa cell proliferation，metastasis and invasion ability in a dose-dependent and time-dependent manner，which may be related to its effect on the expressions of PI3K/Akt signaling pathway-related proteins.

Compuestos fenólicos y actividad antioxidante de los extractos de la hoja de chirimoya (Annona cherimola Mill) / Phenolic compounds and antioxidant activity of extracts from chirimoya (Annona cherimola Mill) leaf / Compostos fenólicos e atividade antioxidante dos extratos da folha de cherimoya (Annona cherimola Mill)

Resumen Después de la cosecha del fruto chirimoya, los árboles liberan enormes cantidades de hojas, las cuales son quemadas por los agricultores. Este trabajo muestra que las hojas pueden ser usadas para nuestro beneficio como antioxidante. Se determinaron los compuestos fenólicos (CF) y la actividad antioxidante (AA) de los extractos de la hoja seca de Annona cherimola Mill en etanol al 70% v/v, agua a 80 °C, y agua subcrítica (AS) a 110, 120 y 130 °C, siguiendo un diseño factorial con el programa Minitab. Los CF se cuantificaron con la metodología de Folin Ciocalteu y la AA con el 2,2-difenil-1-picrilhidrazilo (DPPH) y con el poder antioxidante reductor del hierro (FRAP). Los resultados indicaron que el tipo de solvente y el tiempo de extracción presentaron un efecto significativo en el contenido de CF y AA de los extractos. Se concluyó que el extracto de hoja de chirimoya es un potencial antioxidante. El extracto de AS a 130 °C presentó el mayor contenido de CF (5,6 g EAG/100 g de hoja seca) y el extracto etanólico presentó mayor AA (0,86 mg equivalente trolox/mg extracto seco; IC50=0,020 mg de extracto seco/mL de extracto de hoja seca y FRAP de 1710,14 μmol equivalente trolox /g de hoja seca) y los extractos obtenidos con AS a menor temperatura presentaron mayores valores de AA.

Abstract After harvesting cherimoya fruit, the trees release huge amounts of leaves, which are burned by farmers. This work shows that the leaves can be used as a source of antioxidants. Total phenolic compounds (TPC) and antioxidant activity (AA) of extracts of the dry leaf of Annona cherimola Mill in 70% v/v ethanol, water at 80 °C, subcritical water (SW) at 110 °C, 120 °C and 130 °C were determined, following a factorial design with the Minitab program. The TPC was quantified with the Folin Ciocalteu methodology, and the AA with 2,2-diphenyl-1-picrilhidrazil (DPPH) and Ferric Reducing Antioxidant Power (FRAP). Results indicate that the type of solvent and the extraction time had a significant effect on the TPC and AA of the extracts. Extracts of cherimoya leaves were found to be a potential antioxidant. The extract of SW at 130 °C presented the highest content of TPC (5.6 g EAG/100 g dry leaves) and the ethanolic extract had the highest AA (0.86 mg trolox equivalent/mg dry extract, IC50 = 0.020 mg dry extract/mL extract of dry leaves and FRAP of 1710.14 μmol ET/g dry leaves) and the extracts obtained with SW at a lower temperature presented a higher AA value.

Resumo Depois da colheita da fruta Cherimoya, as árvores liberam grandes quantidades de folhas, que são queimadas pelos agricultores. Este trabalho mostra que as folhas podem ser usadas para nosso benefício como um antioxidante. Compostos fenólicos (FC) e a actividade antioxidante (AA) de extractos de folha seca Annona cherimola Mill em etanol a 70% v/v água a 80 °C, água subcrítica (AS) 110, 120, 130 °C, foram determinados seguindo um planejamento fatorial com o programa Minitab. Os FC foram quantificados com a metodologia Folin Ciocalteu; e a capacidade antioxidante (AA) com 2,2-difenil-1-picrilhidrazil (DPPH) e poder antioxidante redutor de ferro (FRAP). Os resultados indicaram que o tipo de solvente e o tempo de extração tiveram um efeito significativo no conteúdo deCFeAA dos extratos. Conclui-se que o extracto de folha de cherimoya é um potencial antioxidante, o extracto de AS 130 °C tinha o maior conteúdo de CF (5,6 g EAG/100 g folha seca) e o extracto etanólico mostraram maior AA (0,86 mg equivalente Trolox/mg extrato seco, IC50 = 0,020 mg extrato seco/mL extracto de folha seca e FRAP de 1710,14 μmol ET/g folha seca). Os extratos obtido com AS a uma temperatura mais baixa apresentaram um maior valor de AA.

Antiproliferative effects of Vanilla planifolia leaf extract against breast cancer MCF-7 cells

Background: Breast cancer is the most common cancer disease among females in India and worldwide. This needs a critical research for finding the drugs to treat breast cancer with less side effects. The aim of the present study is to reveal the anti-proliferative effects of vanilla extract against MCF-7 cells.Methods: To reveal anti proliferative effects of vanilla leaf extract, MTT assay, cell cycle analysis and DNA fragmentation assay was performed as per standard protocols.Results: MTT assay showed decrease in cell viability with increase of dose of extract and revealed IC50 value at 31.2µg/ml. DNA fragmentation was seen in extract treated cells.Conclusions: The results of the present study confirm the antiproliferative property of vanilla leaf extract in MCF-7 cells. This study results conclude vanilla leaf extract as an effective plant source medicament for treating breast cancer.

Antibacterial activity of the cream preparation from Theobroma cacao L. Pod Aqueous extract

Background and Objectives@#While Theobroma cacao L has long been utilized in the food, cosmetic, and pharmaceutical industries, it was also found to possess antibacterial activity. The beans comprise 10% of the fruit, while the remaining 90%, consisting of pods, is considered waste. It was reported that the pods possess antibacterial activity, and if utilized for this purpose, T. cacao pods will no longer be considered as waste. The aim of this study was to evaluate the antibacterial activity of the cream formulated from the aqueous extract of T. cacao L pods. @*Methods@#The milled T. cacao pods were extracted using distilled water at 4°C for 24 hours. The crude extract was subjected to liquid-liquid partitioning using hexane, ethyl acetate, and n-butanol. Phytochemical screening was performed to identify the constituents present in the extract and its fractions. The extract and its fractions were tested against Staphylococcus aureus, Staphylococcus epidermidis, and Pseudomonas aeruginosa. Determination of IC50 using 3,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) Reduction Assay was used to evaluate the antibacterial activity. The extract with the highest yield and the highest antibacterial activity were formulated into a cream. T. cacao cream was evaluated with quality control tests for creams and emulsions. Acute skin irritation test was performed on the T. cacao cream to assess skin irritability upon application on adult male albino rabbits.@*Results@#T. cacao crude extract and its fractions possessed antibacterial activity. Among the fractions tested, n-butanol fraction had the highest activity against S. aureus, S. epidermidis, and P. aeruginosa. There was a significant difference between the fractions tested on the three bacterial strains (p<0.05). Although n-butanol fraction had the highest activity, the actual yield obtained after extraction was 0.95%. Since T. cacao aqueous extract also exhibited good antibacterial activity, it was chosen for the formulation study. There was no significant difference between the IC50 of the T. cacao crude extract and the IC50 of T. cacao cream, hence formulating it into a cream did not affect the antibacterial activity of the extract. @*Conclusion@#T. cacao pod extract, as well as its fractions, possessed antibacterial activity against three bacterial strains. The T. cacao cream produced was a water-in-oil, non-irritant cream with antibacterial activity, and with acceptable physical attributes.

In vitro Cytotoxicity and Antiplasmodial Activity of Fractions from Anthocleista djalonensis A. Chev. Acetone Root Extract

Aim: Malariacaused by Plasmodium falciparumis one of the killer diseases in Africa today and the uncontrollable spread of drug resistance and limited drugs with therapeutic efficacy makes it necessary to discover agents against this deadly parasite.Traditionally Anthocleistadjalonensisroot extract is used in the treatment of Malaria in many parts of Africa and has demonstrated to be a source of antiplasmodial agents. Thisstudy aims at identifying possible antiplasmodial agents from chromatographic root fractions of Anthocleistadjalonensisof the Genatianceae family as well as to evaluate their cytotoxicity against HeLacells.Place and Duration of Study: The study was undertaken in the Department of Organic Chemistry, Rhodes University, Grahamstown, South Africa. The duration period was betweenMarch and July 2016 Methodology: The Anthocleistadjalonensisroots were collected from Arochukwu, Abia State, Nigeria. The acetone extract was obtained from successive maceration of the methanolcrude extract with hexane, ethyl acetate and acetone. Theconcentration (1-1000?g/mL range) of the chromatographic fractions from acetone root extract of Anthocleistadjalonensiswere tested for anti-malarial activity against Plasmodium falciparium(P.falciparum). Cytotoxicity against HeLa cells was also evaluated using Resazurin based assay.Results: The Five fractions obtained from the chromatographic fractionation of acetone extract labeledA1, A2, A3, A4, and A5 with percentage yield (13.02, 26.66, 24.70, 0.05 and 26.66% respectively) showed excellent anti-plasmodial activity. The anti-malarial bioassay test showed fractions A1, A2, A3, A4 and A5 with IC50value of 0.0360 ± 0.0100, 8.1299 ± 2.0358, 46.2482 ± 1.2720, 0.0151± 0.0010, and 9.8013 ± 0.8171 ?g/mL respectively. CC50 values of 44.2010 ± 8.6790, 50.0000 ± 5.6412, 71.6221 ± 2.9600, 36.7212 ± 5.8900 and 0.5132 ± 3.770 ?g mL–1were recorded for fractions A1, A2, A3, A4 and A5 respectively. Fractions were classified as marginally active (A3) showing SI of 1.540 ± 0.0091, partially active (A2 and A5)with SI 6.150 ± 0.0200 and 4.133 ± 0.015 and as active (A1, A4,)exhibiting SI of 1227.805 ± 8.210 and 2431.867 ± 1.589 respectively. A1 and A4 showed SI > 10 and IC50 < 10 ug/mL.Chloroquine, used as a reference anti-malarial drug, tested in parallel hadan IC50of 0.0125 ± 0.0001?M and was comparable with A1 and A4. Conclusion: The chromatographic fractions from acetone root extract of Anthocleistadjalonensisare potential sources for anti-malarial agents of lead compounds for the development of anti-plasmodial drugs.

The Antibacterial, Antioxidant and Phytochemical Composition of Combretum tanaense (J. Clark) Root Extracts

Aims: To evaluate the antibacterial, antioxidant and phytochemical composition of Combretum tanaense extracts. Study Design: Laboratory-experimental design was used in this study. Place and Duration of Study: Fresh roots of Combretum tanaense were obtained from Mount Kenya University botanical garden in Thika (Kiambu County-Kenya). The study was carried out between November 2017 and February 2018 at Mount Kenya University Biochemistry and Pharmacognosy laboratories. Methodology: Duplicate voucher specimens were prepared and deposited at the East Africa herbarium housed at the National Museums of Kenya and Mount Kenya University herbarium. Extraction of total extracts of C. tanaense roots was conducted according to standard procedures. Agar well diffusion and 2-2-diphenyl picryl hydrazyl (DPPH) assay methods were used to evaluate antibacterial and free radical scavenging activities of the extracts. All assays were performed in triplicate. Antibacterial data was presented as a mean zone of inhibition ± SEM while free radical scavenging activities were expressed regarding IC50. Phytochemical screening was carried out using standard procedures to ascertain the presence or absence of various phytochemical groups in the test plant. Results: The current study indicated that Combretum tanaense root extracts had antibacterial activities against the selected gram-positive and gram-negative bacterial strains. The highest activity was recorded against gram-negative bacteria (Haemophilus influenza) by exhibiting inhibition zones of 13.32±0.15 mm and 12.82±0.36 mm for methanol and water extracts respectively. Antioxidant activities for both methanol and water extracts were ten times higher compared to that of standard (L-ascorbic acid). The extracts were found to have saponins, phenols including tannins and glycosides. Conclusion: Extracts of Combretum tanaense have compounds that exhibit antibacterial and antioxidant activities. From the results obtained, the ability of the extracts to inhibit bacterial growth and scavenge for free radicals was due to the presence of phenolic compounds and will be attributed to the healing properties of this plant. This study recommends further studies including toxicity and isolation of active compounds for the development of products with pharmaceutical value.

In vitro study on antioxidant activity of methanolic leaf extract of Cassia fistula Linn.

Background: The use of medicinal plants for maintaining good health is getting attention worldwide. Antioxidants play an important role to protect damage caused by oxidative stress. In the present study methanolic extracts of Cassia fistula was determined using DPPH for its antioxidant activity. Phytochemical investigation confirmed the presence of bioactive ingredients in the extract.Methods: The antioxidant activity of methanolic extract of Cassia fistula was evaluated using DPPH free radical assay. DPPH (1,1-diphenyl-2-picrylhydrazyine) free radical analysis is one of the accurate and frequently employed method for evaluating antioxidant activity.Results: The methanolic extracts showed increase in radical scavenging activity as concentration increases. The IC50 values were calculated for the methanolic extract. Ascorbic acid was used as control. Cassia fistula exhibited IC 50 of 79.42µg/ml.Conclusions: Scientific evidence suggests that antioxidants reduce the risk for chronic diseases including cancer and heart disease and infectious diseases. Further evaluation of pharmacological activities of Cassia fistula may prove useful in treatment of cancer and heart diseases.

Dipole Moment, Solvation Energy, and Ovality Account for the Variations in the Biological Activity of HIV-1 Reverse Transcriptase Inhibitor Fragments

Objective: A computational approach was employed to determine the interaction of molecular descriptors and the biological activity of the different fragments of HIV-1 reverse transcriptase inhibitors (RTIs). Methods: Using multiple linear regression analysis and leave-one-out validation method, a quantitative structure activity relationship (QSAR) model was developed to relate the biological activity (log IC50) of the different fragment-sized compounds against HIV-1 RT(WT) DNA-dependent DNA polymerase and molecular descriptors of these compounds. Results: QSAR model identified dipole moment, solvation energy, and ovality of fragment-sized compounds to confer reverse transcriptase inhibitory action. A highly significant correlation with log P, molecular weight, polarizability, molecular energy, zero-point energy, constant volume heat capacity at 298 K, and entropy was identified to account for the variations in the potency of RTIs. An increase in ovality, log P, and molecular weight of the fragment-sized compound renders a more active reverse transcriptase inhibition. Conclusion: The quality of the established QSAR model has been validated and demonstrates its potential as a tool for computational design and synthesis of next generation RTIs.

Sensibilidad in vitro de Trichoconiella padwickii a diversos principios activos usados como fungicidas en el cultivo del arroz / In vitro susceptibility of Trichoconiella padwickii to various active ingredients used as fungicides in the cultivation of rice

El objetivo de este trabajo fue evaluar in vitro la sensibilidad micelial de Trichoconiella padwickii a diferentes principios activos por medio del cálculo de la concentración inhibitoria media (CI50). Para ello se realizaron siembras de discos de inóculo en agar poroto con distintas concentraciones (0,1; 1; 10; 30, 50; 100 y 1.000 mg/l) de diversos fungicidas. A los 7 días se midió el diámetro de crecimiento de la colonia (cm). Los datos obtenidos se ajustaron a modelos de regresión no lineal. La sensibilidad se clasificó utilizando la escala de Edgington. Los resultados obtenidos demuestran que el patógeno es muy sensible a los productos que actúan sobre la cadena respiratoria (quinone outside inhibitors QoI y succinate dehydrogenase inhibitors SDHI) y la membrana celular (multisitio), y moderadamente sensible a los que interfieren en la división celular (metil benzimidazol carbamatos MBC), en la síntesis de ácidos nucleicos (fenilamidas PA) y en la transducción de la señal osmótica (actividad multisitio). Este trabajo es el primer antecedente sobre la sensibilidad in vitro de T. padwickii a principios activos fungicidas.

The aim of this study was to evaluate in vitro the mycelial susceptibility of Trichoconiella padwickii to different active ingredients through average median concentration IC50 calculation. Inoculum disks were seeded on bean agar at different concentrations (0.1; 1; 10; 30, 50; 100 and 1000 mg/l) of various fungicides. After seven days the colony diameter was measured. The data obtained were fitted to nonlinear regression models. Susceptibility was classified using the scale proposed by Edgington. The results show that the pathogen is very sensitive to products that act on the respiratory chain (quinone outside inhibitors QoI and succinate dehydrogenase inhibitors SDHI) and cell membrane (multi-site contact activity), and moderately sensitive to those products interfering with cell division (methyl benzimidazole carbamates MBC), synthesis of nucleic acids (phenylamides PA) and osmotic signal transduction (multi-site contact activity). This work is the first record on the sensitivity of T. padwickii.

Study of CJ016 in treatment of lung cancer / 中国药理学通报

Aim Tostudythetherapeuticeffectof CJ016 on human lung cancer model and the mecha-nism.Methods Anexperimentalhumanlungadeno-carcinoma model of A549 was set up to investigate the anti-tumor effect of CJ016,while the effect of angio-genesis and apoptosis in tumor were detected.Results In vitro,the cell proliferation was inhibited signifi-cantly by CJ016,and the value of IC50 was 34. 22 nmol ·L-1 .In vivo,the tumor inhibition rate and T/C%value were 70. 08%and 27. 75%,respectively,at the dose of 20 mg·kg-1 .Meanwhile,CJ016 could reduce the expression of CD31 and promote the apoptosis of tumorcells.Conclusion CJ016caninhibitthegrowth of A549 cells,and the possible mechanism may be re-lated to the reduction of angiogenesis and inducing tumor cell apoptosis.

Relationship between CMPK1 protein and ADM caused multidrug resistance / 中国药理学通报

Aim To assay the possible targets of adriamycin (ADM), screening ADM resistance related proteins.Methods The drug sensitivity of the cells was analyzed by IC50 assay;RT-PCR assay was used to detect the expression of genes in the cells;CMPK1 protein expression was tested by Western blot assay;the expression of CMPK1 in the cells was decreased by siRNA of CMPK1.Results Data from IC50 assay showed the sensitivity of cells transfected with CMPK1 was increased most(IC50 HEK293-CMPK /IC50 HEK293-Control=0.15, P<0.01), and the expression of CMPK1 protein in ADM resistant breast cells (MCF7/ADM) was lower than that in parent MCF7 cells (P<0.05).When the expression level of CMPK1 was decreased by CMPK1 siRNA, the sensitivity of MCF7 cells to ADM decreased (IC50 MCF7-siCMPK1/IC50MCF7-Control=3.6, P< 0.01), and the sensitivity of MCF7 cells to paclitaxel and gemcitabine also decreased.Conclusions CMPK1 was related to the multidrug resistance of cells, and the expression of CMPK1 was positively related to the sensitivity to drugs, which provides the possibility of CMPK1 as a target in the treatment of multidrug resistance.