Anti-HIV-1 Activities of Hemslecins A and B

目的:研究从药用植物金佛山雪胆分离的雪胆素A和雪胆素B两个三萜类化合物的体外抗HIV活性.方法:应用合胞体抑制实验、p24抗原产生的抑制实验、慢性感染细胞和正常细胞间的细胞融合抑制实验等技术检测化合物的体外抗HIV-l活性;利用HIV-l逆转录酶、蛋白酶抑制实验,NCp7锌离子逐出实验探讨化合物的作用机制.结果:雪胆素A和雪胆素B在体外有较好的抑制HIV-l活性,其活性主要表现为:(1)抑制HIV-l诱导合胞体形成,EC50值分别为3.09 μg·mL-1和2.53μg·mL-1;(2)抑制HIV- 急性感染的C8106细胞p24抗原产生,EC50值分别为3.97μg·mL-1和18.90μg·mL-1;(3)抑制HIV-1 慢性感染H9与正常C8166细胞间融合,EC50分别为1.76μg·mL-1和11.95μg·mL-1.雪胆素A和雪胆素B对HIV-l逆转录酶、蛋白酶、NCp7锌离子逐出均没有抑制作用.雪胆素A对HIV-1整合酶有微弱的结合活性,而雪胆素B对HIV-1整合酶没有结合活性.在共培养实验中,雪胆素A和雪胆素B预处理C8166细胞组比未经预处理细胞组能够更有效的抑制HIV-l活性.结论:化合物雪胆素A和雪胆素B体外有较好的抗HIV-1活性,可能主要作用于HIV-1病毒进入细胞阶段.

Indole and carbazole alkaloids from Glycosmis montana with weak anti-HIV and cytotoxic activities

A diprenylated indole, (E)-3-(3-hydroxymethyl-2-butenyl)-7-(3-methyl-2-butenyl)-1H-indole (1), and six known carbazole alkaloids were isolated from the twigs and leaves of Glycosmis montana Pierre (Rutaceae). Their structures were determined on the basis of analysis of spectral evidence including 1D and 2D NMR and MS. The alkaloids (1-3) exhibited weak to moderate take in vitro inhibitory activity against HIV replication in C8166 cells, and they (as well as carbalexine A and B) had cytotoxic activity against the human leukaemia cell line CCRF-CEM. (c) 2005 Elsevier Ltd. All rights reserved.

Anti-HIV-1 activities of extracts from the medicinal plant Rhus chinensis

Rhus chinensis, a species used in folk medicine by Chinese native people, the anti-HIV-1 activities of the petroleum ether, ethyl acetate, butanol and aqueous extract of Rhus chinensis, named as RC-1, RC-2, RC-3 and RC-4, respectively, was evaluated. The

Rubriflordilactones A and B, two novel bisnortriterpenoids from Schisandra rubriflora and their biological activities

Rubriflordilactones A (1) and B (2), two novel highly unsaturated rearranged bisnortriterpenoids possessing a biosynthetically modified aromatic D-ring, were isolated from the leaves and stems of Schisandra rubriflora. Their structures were established on

Synthesis and anti-HIV-1 activities of novel podophyllotoxin derivatives

In order to explore the range of biological activities of the podophyllotoxin compound class, a novel series of derivatives of podophyllotoxin, which were conjugates containing stavudine and different structural podophyllotoxin analogues, were designed, s

Anti-HIV-1 activities of compounds isolated from the medicinal plant Rhus chinensis

Aim of the study: Previously, we reported that the petroleum ether fraction, RC-1, and EtOAc fraction, RC-2, of the medicinal plant Rhus chinensis showed potent anti-HIV-1 activities. To address anti-HIV-1 constituents of RC-1 and RC-2, 17 compounds were

Synthesis of Zidovudine Derivatives with Anti-HIV-1 and Antibacterial Activities

Twelve novel zidovudine derivatives were prepared by modifying 5 '-hydroxyl group of sugar moiety (1-8) and 5-methyl group of thymidine nucleus (9-12) and characterized spectrally. The compounds were evaluated for anti-HIV-1, antitubercular and antibacter

Anti-HIV Activities of the Compounds Isolated from Polygonum cuspidatum and Polygonum multiflorum

The 70% EtOH extract of Polygonum cuspidatum showed inhibitory action against HIV-1-induced syncytium formation at non-cytotoxic concentrations in vitro with a 50% effective concentration (EC50) of 13.94 +/- 3.41 mu g/mL. Through bioactivity-guided fractionation, 20 phenolic compounds, including eight stilbenoids, were isolated from the roots of Polygonum cuspidatum, and their anti-HIV-1 activities were evaluated. Results showed that compounds 1, 13, 14, and 16 demonstrated fairly strong antiviral activity against HIV-1-induced cytopathic effects in C8166 lymphocytes at non-cytotoxic concentrations, with EC50 values of 4.37 +/- 1.96 mu g/mL, 19.97 +/- 5.09, 14.4 +/- 1.34 mu g/mL, and 11.29 +/- 6.26 mu g/mL and therapeutic index (TI) values of 8.12, > 10.02, > 13.89, and > 17.71, respectively. Other compounds showed either weak or no effects. Compound 6 also showed weak inhibition (153.42 +/- 19.25 mu g/mL); however, it possesses very good water solubility and showed almost no cytotoxicity (> 2000 mu g/mL), therefore achieving a fairly good TI (13.04). The activities of the two compounds (3 and 18) from Polygonum multiflorum were also assayed. The relationship between molecular structures and their bioactivities was also discussed.

Dibenzocyclooctadiene Lignans from Schisandra wilsoniana and Their Anti-HIV-1 Activities

Twelve new dibenzocyclooctadiene lignans, marlignans A-L (1-12), together with 16 known compounds, were isolated from the leaves and stems of Schisandra wilsoniana. The structures of 1-12 were elucidated by spectroscopic methods including 1D- and 2D-NMR techniques. Compounds 1-12 were evaluated for their anti-HIV activities, of which compounds 3, 6, 8, and 12 showed modest activities with therapeutic index values of 13.2, 15.6, 17.6, and 16.4, respectively.

Dibenzocyclooctadiene Lignans from Schisandra lancifolia and Their Anti-human Immunodeficiency Virus-1 Activities

Three new dibenzocyclooctadiene lignans, schilancifolignans A-C (1-3), together with thirteen known ones, were isolated from the leaves and stems of Schisandru lancifolia. The structures of 1-3 were elucidated by spectroscopic methods, including extensive 1D- and 2D-NMR techniques. Compounds 1-3 were tested for their anti-human immunodeficiency virus-1 activities and showed weak bioactivities.

Dibenzocyclooctadiene lignans from the fruits of Schisandra wilsoniana and their anti-HIV-1 activities

Three new dibenzocyclooctadiene lignans, wilsonilignans A-C (1-3), together with nine known ones, were isolated from the fruits of Schisandra wilsoniana. The structures of 1-3 were elucidated by spectroscopic methods including extensive 1D and 2D NMR techniques. Compounds 1-3 were also evaluated for their anti-HIV-1 activities and showed bioactivity with EC50 values of 3.26, 6.18, and 2.87g/ml, respectively.

EEG activities in the orbitofrontal cortex and dorsolateral prefrontal cortex during the development of morphine dependence, tolerance and withdrawal in rhesus monkeys

Investigating the activities of the prefrontal cortex (PFC) in the process of addiction is valuable for understanding the neural mechanism underlying the impairments of the PFC after drug abuse. However, limited data are obtained from primate animals and few studies analyze Electroencephalogram (EEG) in the gamma band, which plays an important role in cognitive functions. In addition, it is yet unclear whether drug abuse affects the orbitofrontal cortex (OFC) and dorsolateral PFC (DLPFC) - the two most important subregions of the PFC - in similar ways or not. The aim of this study is to address these issues. We recorded EEG in the OFC and DLPFC in three rhesus monkeys. All animals received a course of saline (NaCl 0.9%, 2 ml) injection (5 days) followed by 10 days of morphine injection (every 12 h), and then a further series of saline injection (7 days). A main finding in the present study was that morphine decreased EEG power in all frequency bands in a short period after injection in both the OFC and DLPFC in monkeys. And gamma power decreased not just in short period after morphine injection but lasted to 12 h after injection. Moreover, we found that although the changes in EEG activities in the OFC and DLPFC at 30-35 min after injection were similar, the DLPFC was more sensitive to the effect of morphine than the OFC. (c) 2005 Elsevier B.V. All rights reserved.

Effects of human activities on migratory waterbirds at Lashihai Lake, China

Surveys on migratory waterbirds and their habitats at Lashihai Lake, China, were conducted from October 1999 to April 2000. Five fixed points, representing different degrees of habitat disturbance and quality, were selected around the lake. We used counts (n = 30) to compare diversity and abundance of waterbirds at each point and evaluate the effects of habitat disturbance. The distribution of waterbirds was affected by disturbance, with snore than one-third of the total species and nearly half of the total individuals occurring at the least disturbed point. Species richness was weakly and abundance was strongly correlated to habitat disturbance, but not to habitat quality. Habitat destruction and use of canoes were prominent at the lake. Naxi ethnic fishermen (n = 37) were interviewed. They caught 570 waterbirds between October 1999 and March 2000 in fishing nets. An estimation of the total number of waterbirds been trapped on the lake is 6164. Diving species were most susceptible. Conservation measures that should implement immediately include the cessation of habitat destruction, better plan for the development of tourism, a reduction in the number of canoes and zoning of the non-fishing area. (C) 2002 Elsevier Science Ltd. All rights reserved.

Effect of Pyrethrins and Rosemary on the ATPase Activities of Rat Cerebral Synaptosome

除虫菊酯越来越广泛地被应用于农业和家庭昆虫防治,主要通过作用于膜结合蛋白而对动物起神经毒性.迷迭香因其抗氧化功能而被应用于很多商业化的除虫菊酯产品中.本实验以大鼠大脑突触体ATP酶为研究对象,对除虫菊酯和迷迭香的药理学进行了研究.用Percoll梯度离心法分离突触体,通过检测无机磷的量来测定总ATP酶和Mg2+-ATP酶活性.结果表明,除虫菊酯在浓度为10 μmol/L时总ATP酶和Mg2+-ATP酶分别降低到对照的80.3%和46.9%.迷迭香在浓度为0.3～30 μmol/L时几乎不影响ATP酶活性,当浓度上升到3 000 μmol/L时,总ATP酶活性降低到66.8%,而Mg2+-ATP酶活性降低到54.5%. 10 μmol/L 除虫菊酯和30 μmol/L迷迭香混合物引起总ATP酶和Mg2+-ATP酶分别降低到72.9%和33.4%.结论: 1) 除虫菊酯能抑制大鼠大脑ATP酶活性; 2) 迷迭香只在高浓度下才对ATP酶有抑制作用; 3) 迷迭香能增强除虫菊酯对ATP酶的抑制作用.图3参19

In vitro activities of small peptides from snake venom against clinical isolates of drug-resistant Mycobacterium tuberculosis

The recent re-emergence of tuberculosis, especially the multidrug-resistant cases, has highlighted the importance of screening effective novel drugs against Mycobacterium tuberculosis. In this study, the in vitro activities of small peptides isolated from snake venom were investigated against multidrug-resistant M. tuberculosis. Minimum inhibitory concentrations (MICs) were determined by the Bactec TB-460 radiometric method. A small peptide with the amino acid sequence ECYRKSDIVTCEPWQKFCYREVTFFPNHPVYLSGCASECTETNSKWCCTTDKCNRARGG (designated as vgf-1) from Naja atra (isolated from Yunnan province of China) venom had in vitro activity against clinically isolated multidrug-resistant strains of M. tuberculosis. The MIC was 8.5 mg/l. The antimycobacterial domain of this 60aa peptide is under investigation. (C) 2003 Elsevier Science B.V. and the International Society of Chemotherapy. All rights reserved.