Sulfated and Sulfur-Containing Steroids and Their Pharmacological Profile

The review focuses on sulfated steroids that have been isolated from seaweeds, marine sponges, soft corals, ascidians, starfish, and other marine invertebrates. Sulfur-containing steroids and triterpenoids are sourced from sedentary marine coelenterates, plants, marine sediments, crude oil, and other geological deposits. The review presents the pharmacological profile of sulfated steroids, sulfur-containing steroids, and triterpenoids, which is based on data obtained using the PASS program. In addition, several semi-synthetic and synthetic epithio steroids, which represent a rare group of bioactive lipids that have not yet been found in nature, but possess a high level of antitumor activity, were included in this review for the comparative pharmacological characterization of this class of compounds. About 140 steroids and triterpenoids are presented in this review, which demonstrate a wide range of biological activities. Therefore, out of 71 sulfated steroids, thirteen show strong antitumor activity with a confidence level of more than 90%, out of 50 sulfur-containing steroids, only four show strong antitumor activity with a confidence level of more than 93%, and out of eighteen epithio steroids, thirteen steroids show strong antitumor activity with a confidence level of 91% to 97.4%.     

来源于一种蛹拟青霉的抗肿瘤活性组分的分离纯化

在实验室大规模主要虫生真菌药物模型筛选的基础上,对安徽农业大学虫生真菌实验室保存的菌株蛹拟青霉[Paecilomyces militaris（Kob．）Brown ＆ Smith ex Liang]RCEF0718的抗肿瘤活性进行了进一步的研究。通过硅胶柱及凝胶柱的多步分离纯化,得到的化合物对多种肿瘤细胞具备良好的抑制活性。     

黑木耳多糖抗肿瘤作用的实验研究

用１８～２０ｇ的昆明系小白鼠研究水溶性、碱溶性及碱不溶性三种黑木耳多糖对移植性肉瘤－１８０的抗肿瘤活性。水溶性和碱溶性黑木耳多糖按５０ｍｇ／ｋｇ和２００ｍｇ／ｋｇ分别分为两个剂量组及一个对照组，每组实验动物数为１０只；碱不溶性黑木耳多糖按１０ｍ／ｋｇ和３０ｍｇ／ｋｇ分为两个剂量组及一个对照组，每组实验动物６只。每天经腹腔注射一次，连续天，停药一周后检查肿瘤抑制率。结果表明：水溶性黑木耳多糖注射剂量     

40株虫生真菌菌丝体提取物抗肿瘤活性的初步研究

以中国仓鼠卵巢(CHO)细胞株为模型,用Resazurin法检测生长抑制率,对40株虫生真菌菌丝体的提取物进行体外抗肿瘤活性试验.结果表明,黄山被毛孢Hirsutella huangshanensis菌株RCEF0851和RCEF0868菌丝体提取物对CHO细胞株的抑制活性最强,其乙酸乙酯和二氯甲烷混合溶剂提取物在100 μg·mL-1时对CHO细胞的抑制率分别为(98.58±1.12)%、(98.47±2.11)%;其甲醇提取物在100 μg·mL-1浓度时对CHO细胞的抑制率也分别达到(97.30±1.83)%和(96.28±1.96)%.复筛的结果表明,RCEF0851和RCEF0868菌丝体提取物对CHO细胞的半数抑制浓度IC50分别为29.24 μg·mL-1和28.87 μg·mL-1.另外,环链拟青霉Paecilomyces cateniannulatus菌株RCEF0508菌丝的乙酸乙酯和二氯甲烷混合溶剂提取物在100 μg·mL-1时对CHO细胞的抑制率也达(95.96±2.01)%,这些菌株值得进一步深入研究.     

丹贝异黄酮对肿瘤的抑制效应

用丹贝异黄酮提取物对携S－180肿瘤的BALB／C小鼠作用，结果丹贝异黄酮提取物高剂量时有30．9％的抑瘤率，并能显著提高荷瘤小鼠的胞腺指数，脾指数和巨噬细胞的吞噬作用。以分离纯的大豆和丹贝黄酮的5个单体染料木素糖苷、大豆苷元糖苷、黄豆黄素苷元、染料木素苷元，大豆苷元（gensitin,daidzin,glycitein,genistein,daidzein)分别作用于乳腺癌MCF－7细胞株，子宫癌HeLa细胞株和卵巢癌HO－8910细胞株，研究各单体对各种癌细胞株的抑制剂和IC50值。结果显示，染料木素在10^-4mol.L^-1时对3株癌细胞均有较高的抑制剂，大豆苷元在10^-4mol.L^-1时对卵巢癌HO－8910细胞株有较强的抑制效果，丹贝异黄酮比大豆异黄酮有更的抑制肿瘤的作用，其中染料木素有更广泛，更强的活性，而糖苷几乎有抑制肿瘤的作用。     

海洋细菌Bacillus pumilus PLM4产抗肿瘤多糖的发酵条件优化研究

从广西北部湾红树林海洋淤泥中筛选到的海洋细菌B acillus pum ilus PLM 4具有产生抗肿瘤多糖的能力。通过单因素试验找到了该海洋细菌产生抗肿瘤多糖的最佳发酵碳源、氮源,分别为可溶性淀粉和牛肉膏,最佳发酵pH和海盐用量分别为pH 7.0和6%~10%。通过正交试验对B.pum ilus PLM 4产生抗肿瘤多糖的发酵条件进行了优化,其最佳发酵条件为:可溶性淀粉3.0%,牛肉膏1.5%,海盐6.0%,pH 7.0,30°C下发酵5 d。     

密花核果木抗肿瘤有效部位的筛选研究

采用3-(4,5-二甲基噻唑-2)-2,5-二苯基四氮唑溴盐(MTT)法,以2种人肿瘤细胞株(SGC-7901、SPCA-1)为研究对象,对海南地区核果木属植物密花核果木的抗肿瘤有效部位进行筛选研究。采用硅胶柱色谱分离技术对石油醚、氯仿萃取部位进行进一步的分离,获得不同极性组分。抗肿瘤活性试验结果表明,石油醚、氯仿萃取部位及其不同极性组分显示不同程度的肿瘤细胞增殖抑制活性,是其抗肿瘤有效部位。     

Three New Resveratrol Derivatives from the Mangrove Endophytic Fungus Alternaria sp.

Three new resveratrol derivatives, namely, resveratrodehydes A–C (1–3), were isolated from the mangrove endophytic fungus Alternaria sp. R6. The structures of these compounds were elucidated by analysis of their MS, 1D and 2D NMR spectroscopic data. All compounds showed broad-spectrum inhibitory activities against three human cancer cell lines including human breast MDA-MB-435, human liver HepG2, and human colon HCT-116 by MTT assay (IC₅₀ < 50 μM). Among them, compounds 1 and 2 both exhibited marked cytotoxic activities against MDA-MB-435 and HCT-116 cell lines (IC₅₀ < 10 μM). Additionally, compounds 1 and 3 showed moderate antioxidant activity by DPPH radical scavenging assay.     

人参皂苷M1硬脂酸酯抗肿瘤活性的研究

研究人参皂苷M1硬脂酸酯(SM1)对小鼠肝癌腹水型(HepA)细胞和小鼠胃癌(MFC)细胞的生长抑制作用。采用动物移植瘤模型,以生理盐水组、阳性药环磷酰胺组作对照,对SM1抗癌活性进行筛选评价。对于小鼠肝癌(HepA)细胞,SM1给药组瘤重为1.44±0.57克,其肿瘤抑制率为51.66%,与生理盐水处理的对照组瘤重(2.97±0.54克)比较差异具有极显著统计学意义(P0.001);对于小鼠胃癌(MFC)细胞,SM1给药组瘤重为1.60±0.68克,其肿瘤抑制率为52%,与生理盐水处理的对照组瘤重(3.32±1.39克)比较差异具有显著统计学意义(P0.05)。SM1能显著抑制小鼠体内肝癌细胞和胃癌细胞的生长,具有显著的抗肿瘤作用。     

硫磺菌菌丝体粗多糖对小鼠Lewis肺癌的体内抑制

对硫磺菌(Laetiporus sulphureus)液体发酵菌丝粗多糖进行体内抗肿瘤研究,结果表明:硫磺菌粗多糖对Lewis肺癌的体内最大抑制作用为35.7%,粗多糖组对胸腺和脾脏的影响显著小于环磷酰胺.