络石藤化学成分及其抗癌活性

简述络石藤中的木脂素、黄酮类化学成分及其抗癌活性的研究近况。     

夏枯草的化学成分和抗癌活性研究

夏枯草为一味软坚散结常用中药,始载于《神农本草经》。夏枯草属植物全球有15种,广泛分布于欧亚的温带地区、非洲西北部及北美洲等地。中国产4种及3变种,即夏枯草及其2个变种:白花夏枯草P.vulgaris L.var.leucantha Schursec.Bailey和狭叶夏枯草P.vulgaris L.var.lanceolata(Barton).Fernald;山菠菜P.asiatica.Nakai及其变种P.asiatica Nakai var.albiflora(koidz.)Nakai;硬毛夏枯草P.hispida.Benth.;大花夏枯草P.grandiflora(linn.)jacq.;白毛夏枯草(Ajuga decumbensThunb.)。夏枯草味苦、辛,性寒,归肝、胆经,具有清火、明目、散结…     

茜草化学成分和抗癌活性研究

目的:研究茜草醋酸乙酯提取物的化学成分和测定其抗癌活性。方法:用硅胶柱色谱分离化学成分,利用各种光谱法确定其化学结构。采用MTT法测定体外抗癌活性,细胞株采用LH1210腹水癌细胞。结果:茜草醋酸乙酯提取物显示体外抗癌活性,从茜草醋酸乙酯提取物低极性部分中分离出6个单体化合物,其结构分别为:β-谷甾醇(Ⅰ)、二氢大叶茜草素(Ⅱ)、大叶茜草素(Ⅲ)、2-甲氧酰基-2,3-环氧基-3-异戊烯基-1,4-萘醌(Ⅳ)、大黄素甲醚(Ⅴ)、齐墩果酸(Ⅵ)。结论:化合物Ⅴ首次从该植物中分离得到,化合物Ⅳ显示了很强的抗癌活性。     

白果槲寄生化学成分及药理活性

综述了白果槲寄生的化学成分及药理活性，揭示了其广阔的临床应用前景。     

抗癌散的抗肿瘤活性成分研究

目的：对抗癌散的抗肿瘤活性成分进行研究。方法：用硅胶、葡聚糖凝胶（Sephadex LH-20）柱色谱等方法进行分离纯化,通过理化性质及光谱数据确定化合物的结构;采用流式细胞术（FCM）对部分单体化合物进行抗肿瘤活性的测定。结果：分离得到β-谷甾醇（Ⅰ）、正丁基-β-D-吡喃果糖苷（Ⅱ）、人参皂苷Rg1（Ⅲ）3个化合物;活性实验结果表明,部分化合物具有一定的抗肿瘤活性。结论：本研究初步阐明了复方抗癌散中的主要化学成分,其中化合物Ⅱ为首次从该植物中分离得到;化合物（Ⅱ）和化合物（Ⅲ）对人肝癌细胞（Bel-7402）有较好的抑制活性。     

蒲葵籽的化学成分及其抗癌活性成分研究

民间,蒲葵籽常与土鸡、猪肉等蒸炖,用于治疗食道癌、白血病、绒毛上皮癌等。目前从蒲葵籽中鉴定的化合物并不多,而从中分离得到的单体化合物就更少了;蒲葵子醇提物的抗癌活性部位筛选还存在很多争议,有待进一步研究;薯蓣皂苷元是中药材蒲葵子中的有效活性成分。     

“太白七药”珠子参化学成分及抗肿瘤活性研究

目的对珠子参中的化学成分进行深入研究,将所得的化合物进行抗肿瘤活性筛选,为揭示其抗肿瘤药理活性及作用机制奠定基础。方法本研究采用D-101大孔树脂、正相硅胶柱层析、反相ODS、Sephadex LH-20、RP-HPLC制备柱色谱法和重结晶等方法,从珠子参的60%乙醇提取物中分离得到7个化合物,通过MS和NMR等方法,鉴定其结构。结果这7个单体的结构分别为三七皂苷R2(notoginsenoside R2)(1)、人参皂苷Rf(ginsenoside Rf)(2)、金盏花苷E(calenduloside E)(3)、太白楤木皂苷Ⅳ(taibaienosideⅣ)(4)、太白楤木皂苷Ⅰ(taibaienosideⅠ)(5)、齐墩果酸(oleanicacid)(6)、人参皂苷Ro(ginsenoside Ro)(7)。除化合物6之外,其余化合物采用MTT法研究其对人源肝癌HepG2细胞株、人源肺癌A549细胞株及人源宫颈癌Hela细胞株的体外抗肿瘤活性。结论化合物3、4和5为首次从该种植物中分离得到。化合物3、4、5对HepG2、Hela及A549细胞的增殖均有显著的抑制作用,而化合物1、2、7均无明显抑制作用。     

独子藤有效成分抗癌活性研究

目的 对独子藤的根和茎的提取物分别作抗癌活性研究.方法 采用MTT法检测两种癌细胞存活率或抑制率.结果 随着提取物浓度的增加,其抗癌效果越显著.结论提取物中有可能含有抗癌活性化合物,我们有必要从中分离出来,为深入认识和合理开发独子藤植物资源提供必要的前提.     

番红花化学成分及生理活性研究概述

文章就番红花的化学成分、生理活性方面的研究进行了综述。     

Bisphosphonate anticancer activity

Bone metastases have a major impact on morbidity and on mortality in cancer patients. Despite its clinical relevance, metastasis remains the most poorly elucidated aspect of carcinogenesis. Different pathways or molecules such as RANK/RANKL/OPG, cathepsin K, endothelin-1, Wnt/DKK1 and Src have recently emerged as potential targets, and preclinical and clinical trials are now underway. The results from clinical trials indicate the importance of treating and preventing bone metastases in many different cancer populations.     

Bisphosphonate anticancer activity

Bone metastases have a major impact on morbidity and on mortality in cancer patients. Despite its clinical relevance, metastasis remains the most poorly elucidated aspect of carcinogenesis. Different pathways or molecules such as RANK/RANKL/OPG, cathepsin K, endothelin-1, Wnt/DKK1 and Src have recently emerged as potential targets, and preclinical and clinical trials are now underway. The results from clinical trials indicate the importance of treating and preventing bone metastases in many different cancer populations.     

葡萄籽提取物化学成分及药理活性的研究进展

目的综述葡萄籽提取物的主要化学成分及药理活性的最新研究进展。方法查阅近年来的国内外相关文献,并进行归纳总结。结果发现葡萄籽提取物包括多酚类、脂质类及其他化学成分,具有抗氧化作用、心血管保护作用、抗肿瘤作用、抗辐射作用及其他药理学活性。结论葡萄籽提取物是一种很有开发价值的天然植物药。     

Chemical compositions and repellent activity of Clerodendrum bungei Steud. essential oil against three stored product insects

BackgroundSeveral species of Verbenaceae have been widely used in medicine, and some species of Verbenaceae have been observed good insecticidal activity, such as Lantana camara and Vitex negundo. There is no report about repellent activity of Clerodendrum bungei Steud. (C. bungei) against stored product insects. The chemical composition of C. bungei essential oil (EO) were identified, repellent activity of methanol extract, EO of C. bungei and two main components of EO against T. castaneum, L. serricorne and L. bostrychophila were evaluated for the first time.ResultsEO of C. bungei was obtained by hydrodistillation and analyzed by gas chromatography-mass spectrometry (GC–MS) and GC. A total of 25 components of the C. bungei EO were identified. The principal compounds in the EO were myristicin (75.0%), 2,2,7,7-Tetramethyltricyclo[6.2.1.0(1,6)]undec-4-en-3-one (4.1%) and linalool (3.4%). Results of bioassays indicated that C. bungei EO exerted strong repellent activity against three target insects. As main constituents, myristicin and linalool also had certain repellency.ConclusionThis work suggests that the EO of C. bungei has promising potential to develop into botanical repellents for the control of pest damage in warehouses and grain stores.Graphical abstract      

Taxol anticancer activity and DNA binding

The interaction of taxol with DNA has major biological importance since it is shown the presence of higher concentration of taxol in the nucleus, than in the human lung tumor cell. Therefore, in this report we examine the interaction of taxol with calf-thymus DNA in aqueous solution at physiological pH, using constant DNA concentration (25 or 1.25 mM phosphate) and various taxol/DNA (phosphate) ratios 1/200 to 1/2. Capillary electrophoresis and Fourier transform infrared (FTIR) difference spectroscopic methods are used to characterize the nature of drug-DNA interaction and to determine the taxol binding site, the binding constant, sequence selectivity, helix stability and biopolymer secondary structure in the taxol-DNA complexes in vitro. Structural analysis showed that taxol is an external DNA binder with no affinity towards DNA intercalation. The major target of taxol is A-T, G-C bases and the backbone PO(2) groups. Two bindings were observed for taxol-DNA complexes with K(1)= 1.4 x 10(4) M(-1) and K(2)=3.5 X 10(3) M(-1). The taxol-DNA interaction is associated with a partial helix stabilization and no major alterations of B-DNA structures.     

Synthesis and anticancer activity of 5'-phthaloylnucleosides

A series of novel 5'-phthaloylnucleosides were synthesized via Mitsunobu reaction starting from AZT or 2'-deoxyadenosine and numerous phthalimides and their sulphur analogues-thioimides. Some of them showed significant anticancer activity.     

去甲斑蝥素-半乳糖衍生物的合成与抗癌活性

设计并合成了肝靶向抗癌前药去甲斑蝥素-半乳糖(NCTD-Gal)偶联物。以去甲斑蝥素为原料，经氨基酸修饰后，再通过酰化、氢解、糖苷化和脱乙酰基反应合成去甲斑蝥素-半乳糖衍生物。合成了7个新β-O-糖苷化合物，结构通过IR、 MS、 ¹H NMR和元素分析确证。对产物4a进行了初步小鼠体内抗肿瘤实验，结果显示，4a中、高剂量组抑瘤率明显高于NCTD组，表明半乳糖苷化对NCTD抗癌作用有一定提高。     

Synthesis and anticancer activity of asparagine analogs

A series of 11 asparagines substituted on N4 was prepared and evaluated for their ability to inhibit the growth of L5178Y leukemia cell cultures. These cells require an exogenous source of L-asparagine and should be sensitive to an asparagine antimetabolite. The compounds were prepared by reaction of phthalylaspartic anhydride with a primary or secondary amine, followed by removal of the phthalyl group with hydrazine. One compound, N,N-dibenzylasparagine, showed significant activity. Additional study of asparagine derivatives bearing large, lipophilic groups at N4 is warranted.