Assessment of genotoxicity and cytotoxicity of standardized aqueous extract from leaves of Erythroxylum cuneatum in human HepG2 and WRL68 cells line

Objective:To investigate the cytotoxicity and the genotoxicity of standardized aqueous of dry leaves of Erythroxylum cuneatum(E.cuneatum)in human HepG2 and WRL68 cells.Methods:The cytoloxicity of E.cuneatum extract was evaluated by both MTS and LDH assays.Genotoxicity study on E.cuneatum extract was assessed by the single cell gel electrophoresis(comet assay).The protective effect of E.cuneatum against menadione-induced cytotoxicity was also investigated.Results:Results from this study showed that E.cuneatum extract exhibited cytotoxic activities towards the cells with IC_(50)value of(125±12)and(125±14)μg/mL for HepG2and WRL68 cells respectively,after 72 h incubation period as determined by MTS assay.LDH leakage was detected at(251±19)and(199.5±12.0)μg/mL for HepG2 and WRL68 respectively.Genotoxicity study results showed that treatment with E.cuneatum up to 1 mg/mL did not cause obvious DNA damage in WRL68 and HepG2 cells.Addition of E.cunaetum did not show significant protection towards menadione in WRL68 and HepG2 Cells.Conclusions:E.cuneatum standardized aqueous extract might be developed in onler to establish new pharmacological possibilities for its application.

Hepatoprotective effect of leaves of Erythroxylum monogynum Roxb.on paracetamol induced toxicity

Objective:To investigate the hepatoprotective activity of methanolic extract of leaves of Erythroxylum monogynum(E.monogynum)on paracetamol induced toxicity.Methods:Methanolic extract of leaves of E.monogynum was given in doses of 100 mg/kg,200 mg/kg and 400 mg/kg for 7 d and toxicity was induced by paracetamol(2 mg/kg)on Day 8.Silymarin(50 mg/kg)was used as reference standard.After 24 h of toxicity induction blood samples were collected from retro-orbital plexsus and analyzed for serum parameters like serum glutamic pyruvic transaminase,serum glutamic oxaloacetate transaminse,alkaline phosphatase and total bilirubin.Livers isolated were studied for histopathological changes.Results:Phytochemical analysis of methanolic extract of E.monogynum leaves showed the presence of carbohydrates,flavonoids,phenols and saponins.Prior administration of this extract restored the elevated levels serum markers as compared to toxic group which is also confirmed by the histopathological changes observed.Conclusions:The present study showed that methanolic extract of leaves of E.monogynum possess hepatoprotective action against paracetamol induced hepatotoxicity.

Advances in chemistry and bioactivity of the genus Erythroxylum

Erythroxylum P.Browne is the largest and most representative genus of Erythroxylaceae family.It contains approxi-mately 230 species that are mainly distributed in tropical and subtropical regions.Some species in this genus,such as E.monogynum and E.coca,have been used as folk medicines in India or South America for a long history.It is well known that Erythroxylum plants are rich in tropane alkaloids,and the representative member cocaine shows remarka-ble activity in human central nervous system.However,many other types of active compounds have also been found in Erythroxylum along with the broadening and deepening of phytochemical research.To date,a total of 383 com-pounds from Erythroxylum have been reported,among which only 186 tropane alkaloids have been reviewed in 2010.In this review,we summarized all remained 197 compounds characterized from 53 Erythroxylum species from 1960 to 2021,which include diterpenes,triterpenes,alkaloids,flavonoids,and other derivates,providing a comprehensive overview of phytoconstituents profile of Erythroxylum plants.In addition,the biological activities of representative phytochemicals and crude extracts were also highlighted.

Protein Tyrosine Phosphatase 1B Inhibitory Potential in Erythroxylum monogynum Leaf Extracts

Insulin and Leptin resistance are the hallmarks for the development of type 2 diabetes mellitus (T2DM) and obesity. Both of these conditions are associated with increased activity and idiom of Protein Tyrosine Phosphatase 1B (PTP 1B). Therefore, inhibition of PTP 1B activity or down-regulation of its expression has become a striking area of therapeutics development in order to ameliorate the phenomenon of Insulin and Leptin resistance. Lack of awareness and late diagnosis makes diabetes difficult to manage. PTP 1B inhibitory activity by Erythroxylum monogynum plant extracts in the cytosolic supernatant of goat skeletal muscle and the liver was estimated. Erythroxylum monogynum plant extraction was done in hydroalcoholic solution (water–ethanol 20:80 (v/v)) and Methanol. The Polyphenols and protein content were identified in the hydroalcoholic and methanolic extracts. The greatest PTP 1B inhibitory activity in goat liver and skeletal muscle was found in the hydroalcoholic extract. Erythroxylum monogynum is a potent natural source of PTP 1B inhibition and may become cost-effective therapeutics in correcting metabolic disturbances of T2DM, obesity and cardiovascular disorders.

基于HPLC-Q-TOF-MS技术的柳叶鼠李化学成分分析

目的建立HPLC-Q-TOF-MS方法快速分析柳叶鼠李的化学成分。方法采用BEH C_(18)色谱柱(2.1 mm×100 mm,1.7μm),以0.1%甲酸水溶液和乙腈为流动相进行梯度洗脱,流速为0.3 mL·min^(-1)。扫描方式采用正、负离子Full-dd MS^(2)模式。通过在线mz Cloud及Chemspider数据库和自建标准库mz Vault进行分析,结合相关文献检索以及质谱裂解规律分析柳叶鼠李中的化学成分。结果共鉴定出138个化合物,主要是黄酮类和有机酸类。结论对柳叶鼠李中的化学成分进行了快速的分析,可为柳叶鼠李的质量控制和药效物质基础研究提供参考。

柳叶鼠李播种育苗初探

本文对柳叶鼠李(Rhamnus erythroxylum)的种子进行了萌发试验,种子未经处理和经过浸种24 h处理,采用人工气候箱和温室穴盘播种2种方式,试验结果表明,经过处理的种子发芽率明显高于未经处理的种子发芽率,且柳叶鼠李种子无休眠,当年采种即可播种,发芽率可达60%,温室内播种可为大田育苗奠定基础,为柳叶鼠李大量播种繁殖提供科学依据。

Double-blind evaluation of homeopathy on cocaine craving：a randomized controlled pilot study

Background： Brazil is among the nations with the greatest rates of annual cocaine usage. Pharmacological treatment of cocaine addiction is still limited, opening space for nonconventional interventions.Homeopathic Q-potencies of opium and Erythroxylum coca have been tested in the integrative treatment of cocaine craving among homeless addicts, but this setting had not proven feasible, due to insufficient recruitment.Objective： This study investigates the effectiveness and tolerability of homeopathic Q-potencies of opium and E. coca in the integrative treatment of cocaine craving in a community-based psychosocial rehabilitation setting.Design, setting, participants, and interventions： A randomized, double-blind, placebo-controlled, parallelgroup, eight-week pilot trial was performed at the Psychosocial Attention Center for Alcohol and Other Drugs（CAPS-AD）, Sao Carlos/SP, Brazil. Eligible subjects included CAPS-AD patients between 18 and 65 years of age, with an International Classification of Diseases-10 diagnosis of cocaine dependence（F14.2）. The patients were randomly assigned to two treatment groups： psychosocial rehabilitation plus homeopathic Q-potencies of opium and E. coca（homeopathy group）, and psychosocial rehabilitation plus indistinguishable placebo（placebo group）.Main outcome measures： The main outcome measure was the percentage of cocaine-using days. Secondary measures were the Minnesota Cocaine Craving Scale and 12-Item Short-Form Health Survey scores.Adverse events were reported in both groups.Results： The study population comprised 54 patients who attended at least one post-baseline assessment,out of the 104 subjects initially enrolled. The mean percentage of cocaine-using days in the homeopathy group was 18.1%（standard deviation（SD）： 22.3%）, compared to 29.8%（SD： 30.6%） in the placebo group（P 〈0.01）. Analysis of the Minnesota Cocaine Craving Scale scores showed no between-group differences in the intensity of cravings, but results significantly favored homeopathy over placebo in the proportion of weeks without craving episodes and the patients＇ appraisal of treatment efficacy for reduction of cravings. Analysis of 12-Item Short-Form Health Survey scores found no significant differences. Few adverse events were reported： 0.57 adverse events/patient in the homeopathy group compared to 0.69 adverse events/patient in the placebo group（P = 0.41）.Conclusions： A psychosocial rehabilitation setting improved recruitment but was not sufficient to decrease dropout frequency among Brazilian cocaine treatment seekers. Psychosocial rehabilitation plus homeopathic Q-potencies of opium and E. coca were more effective than psychosocial rehabilitation alone in reducing cocaine cravings. Due to high dropout rate and risk of bias, further research is required to confirm our findings, with specific focus on strategies to increase patient retention.