环烯醚萜类化合物近年研究进展

目的 介绍环烯醚萜类化合物研究概况和近年研究进展。方法 以近年来国内外发表的文献为依据,从结构分类、半合成及生物活性方面综述环烯醚萜类化合物近年研究进展。结果 环烯醚萜类化合物具有多种生物活性。结论 环烯醚萜是一类很有研究价值的化合物。     

雷公藤属醋酸乙酯部位化学成分及药理作用研究进展

雷公藤属植物化学成分复杂,具有广泛的药理作用。现在已经从雷公藤属醋酸乙酯提取部位分离得到多种化学成分,主要为二萜类、三萜类、倍半萜类、生物碱类及其他化合物;药理研究表明其具有抗炎、免疫抑制、抗血小板聚集作用和杀虫活性。对雷公藤属醋酸乙酯部位化学成分及药理作用研究进展进行综述,为后续研究提供理论依据。     

雷公藤中的新倍半萜类化合物

本文介绍日本学者对雷公藤属植物倍半萜类化学成分的研究概况。从日本产雷公藤叶中分离出11个新的倍半萜类化合物,从中国东北雷公藤(黑蔓)中分离出一个新的倍半萜类生物碱。     

八角属植物萜类成分及其药理活性研究进展

目的 为深入研究八角属植物萜类成分和开发其药理活性提供参考。方法 总结2011年至2021年全球八角属植物中萜类成分的新化合物和药理活性研究进展。结果 八角属植物主要含有挥发油、萜类、黄酮类、木脂素、有机酸等化学成分。其中,萜类新化合物有80多个,以结构复杂、类型繁多的倍半萜类为主,具有抗柯萨奇病毒B3型、抗乙型肝炎病毒、抗菌、抗氧化、抗炎、营养神经、抑制细胞毒性等多种药理活性。结论 倍半萜类化合物为八角属植物萜类成分的主要成分,其抗病毒、营养神经、抗炎、抑制细胞毒性、抗菌、抗氧化等药理活性有待开发。     

药用植物细胞悬浮培养体系生物转化的研究进展

细胞悬浮培养体系生物转化获得目标产物已成为获取天然活性产物的重要途径。利用不同药用植物的细胞悬浮培养体系及不同的反应类型对先导活性化合物进行生物转化,可以获得新的活性化合物或提高活性化合物的产率。本文综述了近年来药用植物细胞悬浮培养体系类型及生物转化的新进展,并对活性成分的结构修饰与资源利用进行探讨。     

GC-MS分析白鲜皮的挥发油成分

目的研究白鲜皮挥发油的化学成分。方法用水蒸气蒸馏法提取白鲜皮挥发油并用气相色谱-质谱技术分析。结果从白鲜皮挥发油中分离鉴定了31个组分,占总峰面积含量的86.17%。结论白鲜皮挥发油主要由倍半萜类化合物和长链脂肪酸成分构成,而倍半萜类化合物是其主要活性成分。     

中国吉林栽培西洋参挥发油成分的新近研究

本文用气相色谱-质谱-计算机联用装置分离分析了吉林栽培西洋参挥发油中的化学成分及相对含量,鉴定出37种化合物。其中倍半萜类化合物有26种,约占总挥发油的75%,为西洋参挥发油中的主要成分。同时探讨了倍半萜类及皂甙的可能生合成途径。     

亚菊属植物挥发油的化学成分及其生物活性研究进展

目的综述国内外关于亚菊属植物挥发油化学成分及其生物活性的研究进展,为亚菊属植物药用价值的进一步开发和利用提供参考。方法查阅相关文献,对亚菊属植物挥发油的现有研究进行归纳总结。结果亚菊属植物挥发油化学成分主要为单萜、倍半萜类化合物,具有抑菌、杀虫等功效。结论亚菊属植物具有较高的药用价值,但部分亚菊属植物未有报道,药理作用机制尚不明确,后续应进一步加强有关研究。     

泽泻属植物化学成分与药理活性

综述了泽泻属植物中的四环三萜类、倍半萜类、二萜类及其他化合物,总结了泽泻属植物提取物与部分单体的药理活性。     

款冬花的化学成分

从款冬花（Tussilago farfara L.0中分离得到四个倍半萜类化合物和两个苯二甲酸酯类化合物，经光谱分析确定其中两个倍半萜类化合物为新结构，命名为款冬花酮（tussilagonone,1)和新款冬花内酯（neotussilagolactone,2）。由血小板活化因子（PAF）引起的血小板聚集实验结果表明，两个新化合物均有较强的抑制PAF活性。     

Cytochrome P450 polymorphism--molecular, metabolic, and pharmacogenetic aspects. III. Influence of CYP genetic polymorphism on population differentiation of drug metabolism phenotype

In the human genome 684 alleles of CYP genes, and additionally 30 complete CYP pseudogenes, have been identified. So far 388 isoforms of 58 human CYP isoenzymes have been described at the phenotypic level. The molecular forms of many CYP isoenzymes responsible for drug biotransformation show a differentiated degree of specific catalytic activity - from increased, through normal and decreased to various extent, to trace or even absent. Depending on the homo- or heterozygous genotype, a broad palette of phenotypic forms may be present, differentiated in respect to biotransformation dynamics of specific drugs. The progress of molecular biology with particular consideration of genotyping and DNA microarray technologies has created a basis for the dynamic progress of pharmacogenetics, allowing fast and sensitive determination of the individual pharmacogenetic profile, encompassing a large set of CYP alleles extended by allelic variants of genes encoding other enzymes participating in drug metabolism. The possibility to evaluate the pharmacogenetic profile of patients together with the increasing knowledge about the mechanisms of inhibition, repression and also induction of enzymes participating in biotransformation of xenobiotics and endogenous compounds create increasing possibilities of elaborating optimal individualized pharmacotherapeutic strategies.     

地胆草的化学成分和药理作用研究进展

地胆草 Elephantopus scaber Linn.为菊科地胆草属植物,产于美洲、亚洲、非洲等地区及我国的南方诸省,具有清热解毒、消肿利尿之功效,用于治疗感冒、胃肠炎、扁桃体炎、咽喉炎、结膜炎、肾炎水肿、疖肿等。地胆草含有倍半萜、三萜、黄酮等成分,近年来从中发现的倍半萜内酯类成分因具有强大抗肿瘤活性而备受关注。为了更好的发掘、利用地胆草资源,该文综述了其化学成分和药理作用研究进展。     

南蛇藤属植物化学成分及活性研究进展

南蛇藤属植物在我国分布广泛，近年来从中分得了多种β-二氢沉香呋喃型倍半萜和friedlane等型三萜，其中一些具有昆虫拒食、抗肿瘤和细胞毒活性。本文综述了近10年来从南蛇藤属植物中分得的化学成分及其活性的研究进展。     

Expression of cytochrome p450 and other biotransformation genes in fetal and adult human nasal mucosa.

Despite recent progress in the identification and characterization of numerous nasal biotransformation enzymes in laboratory animals, the expression of biotransformation genes in human nasal mucosa remains difficult to study. Given the potential role of nasal biotransformation enzymes in the metabolism of airborne chemicals, including fragrance compounds and therapeutic agents, as well as the potential interspecies differences between laboratory animals and humans, it would be highly desirable to identify those biotransformation genes that are expressed in human nasal mucosa. In this study, a global gene expression analysis was performed to compare biotransformation enzymes expressed in human fetal and adult nasal mucosa to those expressed in liver. The identities of a list of biotransformation genes with apparently nasal mucosa-selective expression were subsequently confirmed by RNA-polymerase chain reaction (PCR) and DNA sequencing of the PCR products. Further quantitative RNA-PCR experiments indicated that, in the fetus, aldehyde dehydrogenase 6 (ALDH6), CYP1B1, CYP2F1, CYP4B1, and UDP glucuronosyltransferase 2A1 are expressed preferentially in the nasal mucosa and that ALDH7, flavin-containing monooxygenase 1, and glutathione S-transferase P1 are at least as abundant in the nasal mucosa as in the liver. The nasal mucosal expression of CYP2E1 was also detected. These findings provide a basis for further explorations of the metabolic capacity of the human nasal mucosa for xenobiotic compounds.     

Phytochemistry and bioactivities of sesquiterpenoids from the Artemisia species

The genus Artemisia is one of the largest and most widely distributed genera of the family Compositae. One type of the mainly active metabolites found in the Artemisia plants is sesquiterpenoids with extensive biological activities, including anti-inflammatory, immunomodulatory, anti-tumour, antimalarial, antinociceptive, antimicrobial and other activities. In this review, wecomprehensively summarized the progressconcerning the phytochemistry and biological activities of sesquiterpenoids obtained from the Artemisiaspecies from 2010 to July 2016. Furthermore,several future research perspectives and development of sesquiterpenoids as potential therapeutic agents were discussed as well.     

Acanthella属海绵化学成分及生物活性的研究进展

目的对Acanthella属海绵的化学成分及其生物活性进行综述。方法通过综述国内外相关文献,归纳总结了该属海绵的研究概况。结果从该属海绵中已分离鉴定110个化合物,主要为含有异腈基、异硫氰酸酯和甲酰胺等含氮基团的倍半萜、二萜类化合物。这类化合物具有抗疟、抗虫、抗污损、抗肿瘤、抗菌等多样的生物活性。结论为Acanthella属海绵的化学成分及生物活性的进一步研究提供依据。     

枫蓼肠胃康的研究进展

枫蓼肠胃康由牛耳枫、辣蓼组成。研究表明,该复方中含有补身烷倍半萜类、黄酮类、生物碱类、有机酸类等化学成分,具有保护胃黏膜、抗溃疡性结肠炎、抗炎镇痛、抗菌等多方面的药理作用。在临床上常用的有枫蓼肠胃康颗粒剂、片剂、冲剂等,多用于急性肠胃炎、肠易激综合征、溃疡性结肠炎等。综述枫蓼肠胃康化学成分、药理作用、临床应用的研究进展,为其进一步研究和开发提供科学依据。     

The pharmacodynamics of 4-(p-chlorophenylthio)butanol (W-2719) in humans.

4-(p-Chlorophenylthio)butanol (W-2719) is absorbed, metabolized and excreted when administered orally to human volunteers. The butyrate (W-2718) and the acetate (W-2683) metabolites were found in plasma with W-2683 being the major biotransformation product and detectable seven days after administration with an apparent half-life of 33.2 h. p-Chlorothiophenol appeared to be the major biotransformation product in urine and was detectable through day 6. As in plasma, the other major biotransformation product was W-2683, which was again detectable through day 7 and had a t 1/2 in urine of 40.8 h. The minor metabolite found in urine was W-2718. No W-2719 was found in either plasma or urine after oral administration.