托瑞米芬的研究进展

托瑞米芬（toremifene）是新一代抗雌激素、抗肿瘤药物,其化学成分是三苯乙烯的衍生物,分子式为C26H28NOCl·C6H8O7,相对分子质量为598,将从托瑞米芬的化学合成、托瑞米芬的抗肿瘤作用机制、托瑞米芬的实验研究、托端米芬的药物动力学、临床研究及不良反应等方面进行阐述。     

A lactose-binding lectin from the marine sponge Cinachyrella apion (Cal) induces cell death in human cervical adenocarcinoma cells

Cancer represents a set of more than 100 diseases, including malignant tumors from different locations. Strategies inducing differentiation have had limited success in the treatment of established cancers. Marine sponges are a biological reservoir of bioactive molecules, especially lectins. Several animal and plant lectins were purified with antitumor activity, mitogenic, anti-inflammatory and antiviral, but there are few reports in the literature describing the mechanism of action of lectins purified from marine sponges to induce apoptosis in human tumor cells. In this work, a lectin purified from the marine sponge Cinachyrella apion (CaL) was evaluated with respect to its hemolytic, cytotoxic and antiproliferative properties, besides the ability to induce cell death in tumor cells. The antiproliferative activity of CaL was tested against HeLa, PC3 and 3T3 cell lines, with highest growth inhibition for HeLa, reducing cell growth at a dose dependent manner (0.5-10 μg/mL). Hemolytic activity and toxicity against peripheral blood cells were tested using the concentration of IC(50) (10 μg/mL) for both trials and twice the IC(50) for analysis in flow cytometry, indicating that CaL is not toxic to these cells. To assess the mechanism of cell death caused by CaL in HeLa cells, we performed flow cytometry and western blotting. Results showed that lectin probably induces cell death by apoptosis activation by pro-apoptotic protein Bax, promoting mitochondrial membrane permeabilization, cell cycle arrest in S phase and acting as both dependent and/or independent of caspases pathway. These results indicate the potential of CaL in studies of medicine for treating cancer.     

Synthesis of 1-substituted carbazolyl-1,2,3,4-tetrahydro- and carbazolyl-3,4-dihydro-β-carboline analogs as potential antitumor agents

A series of 1-substituted carbazolyl-1,2,3,4-tetrahydro- and carbazolyl-3,4-dihydro-β-carboline analogs have been synthesized and evaluated for antitumor activity against human tumor cells including KB, DLD, NCI-H661, Hepa, and HepG2/A2 cell lines. Among these, compounds 2, 6, 7, and 9 exhibited the most potent and selective activity against the tested tumor cells. As for inhibition of topoisomerase II, compounds 1-14 and 18 showed better activity than etoposide. Among them, compounds 3, 4, 7, 9, and 10 exhibited potent activity. The structure and activity relationship (SAR) study revealed correlation between carbon numbers of the side chain and biological activities. The molecular complex with DNA for compound 2 was proposed.     

Studies on the synthesis of derivatives of marine-derived bostrycin and their structure-activity relationship against tumor cells

A series of new derivatives (5-29) of marine-derived bostrycin (1) were synthesized. The in vitro cytotoxic activities of all compounds were evaluated against MCF-7, MDA-MB-435, A549, HepG2, HCT-116 and MCF-10A cells using the MTT method. The compounds 7, 8, 22, 23, 25, 28 and 29 of the total showed comparable activity to epirubicin, the positive control, against the tested cancer cell lines. However, these compounds also exhibited cytotoxicity towards MCF-10A cells. The structure-activity relationship (SAR) of bostrycin derivatives was also discussed based on the obtained experimental data.     

人参皂苷代谢产物M1及其脂肪酸酯EMl抗肿瘤活性研究进展

目的:介绍人参皂苷代谢产物20—O—β—D—吡喃葡萄糖—20(S)—原人参二醇皂苷(M1)及其脂肪酸酯(EM1)抗肿瘤活性和EMl合成的研究进展,为其深入研究提供参考。方法:对近年来有代表性的文献进行分析、归纳。结果:人参皂苷代谢产物及其脂肪酸酯有抗肿瘤活性。结论:EM1抑制肿瘤作用比M1强,EM1可能是人参皂苷在体内的真正的活性形式。EM1的药代动力学和生理学需进一步深入研究。     

马粪海胆壳棘多糖的分离、纯化和抗肿瘤活性的研究

马粪海胆Hemicentrotus pulcherrimus壳棘经脱脂、热水煮沸、浓缩、去蛋白、去核酸、脱色和分级等一系列步骤,得到硫酸多糖XB-1;利用高效液相色谱仪等检测该多糖的相对分子质量为190万,并证明其组分具有均一性;XB-1经水解、衍生化和气相色谱分析,确定其单糖组分为岩藻糖和硫酸基;采用正交试验确定了XB-1的最佳提取条件;体外抗肿瘤试验结果显示,XB-1对肺腺癌细胞、乳腺癌细胞和宫颈癌细胞均有不同程度的抑制作用。     

类柠檬苦素的生物活性研究进展

类柠檬苦素是一类三萜类植物次生代谢产物,主要存在于芸香科或楝科植物中。人们探求柑橘类果汁苦味的原因时发现了该类物质,并对其进行了研究。其表现出来的多种生物活性,如抗肿瘤、抗疟疾、抗氧化等,对人类健康具有重要意义。就目前已发现的类柠檬苦素的各种生物活性进行综述,并讨论其开发利用前景。     

Recent Development of Scientific Researches on Arsenics

In recent yuars,environmental arsenic contamination is a major problem in many parts of the world. There are many reports from many nations on human exposure to arsenic in drinking water has been linkedto various diseases and chronic arsenic poisoning symptoms . Though arsenic has been known as a poison for thousands of years, there have long been reports of benfical effects.Chinese medicine has used arsenic as a medicinal for thousands of years,especially studies have identified arsenic trioxide as a powerful and dramatic therapy for acute promyelocytic leukaemia(APL),which suggested many scholor use this drug to cure various tumors.     

银杏叶聚戊烯基磷酸酯体内外抗肿瘤的生物活性研究

研究了聚戊烯基磷酸酯(PPH)体外对肿瘤细胞和体内抗移植性肿瘤的抑制作用。从银杏叶中分离制备聚戊烯醇混合物(C75~C110),选择POC l3为磷酰化剂和三乙胺为碱性水解剂,经过磷酰化和水解二步反应,合成聚戊烯基磷酸单酯。以氟脲嘧啶(5-Fu)为对照,体外肿瘤细胞株选择SGC-7901人胃癌、LoVo人结肠腺癌和Hela人宫颈癌;体内移植性肿瘤细胞株选择肝癌实体型(Heps)、肉瘤(S180)、艾氏癌实体(EC),用不同剂量的PPH进行抗肿瘤药效实验。结果表明,银杏叶PPH在高浓度下(0.4 g/L)作用72 h,对3种体外细胞株抑瘤率达到60%~80%;对Heps、S180和EC等移植性瘤株抑瘤率达到50%~65%。这说明银杏叶PPH具有明显的抑制肿瘤的生物活性。     

不同品种茶叶的抗癌活性研究

本研究应用分光光度法和高效液相色谱法测定了4种不同茶叶的化学成分和儿茶素的含量,结果表明,茶叶品种不同,其化学成分、儿茶素的组成与配比差异较大,这是决定其抗癌作用的物质基础。