Azide Method Applied in the Synthesis of Antineoplastic Active Meterials-N''-Phenyacetyl-N-Substituted Glutamine

The results of studies of Antineopalston A10 show it's degradation products, such as glutamines and isoglutamines, having antitumor activity. According to these, some N'-phenylacetyl-N-substituted glutamines are designed and synthesized for researching their antitumor activity. In the syntheses of these compounds, the acid azides are prepared first, which then react with amines at low temperature to transform to the target molecules. The mild reaction conditions and good yields and the optical activity maintaining are the merits of this method. Evaluation of antitumor activity of the target molecules is carried out by MTT method to L1210 cell strain. The result showes some compounds can inhibit growth of the cancer cells.     

喹噁啉类药物抗肿瘤与抗菌活性的研究进展

喹噁啉类药物是畜牧生产中大量使用的抗菌促生长添加剂,同时在医药领域也进行着大量的研究,在国际上得到广泛的重视。主要介绍了目前国内外在喹噁啉类药物在抗肿瘤和抗菌生物活性方面作用的研究进展,并且探讨了其作用的机理。     

银杏外种皮中银杏酚酸抗肿瘤活性的研究

从银杏外种皮中提取银杏酚酸,对银杏酚酸的抗肿瘤活性进行了研究。结果表明:银杏酚酸浓度为10,20,40 mg/kg.d时,对小鼠S180肉瘤的抑制率分别为38.93%,42.90%和62.94%,40 mg/kg.d的抑瘤率超过了阳性对照药物Cy;银杏酚酸使荷瘤小鼠的胸腺重量减轻,但无明显差异,中低剂量组能显著提高荷瘤小鼠脾脏的重量,但高剂量组却减轻脾脏重量;银杏酚酸能抑制人宫颈癌Hela细胞增殖,并呈时间和药物浓度的依赖性,当银杏酚酸浓度为24 mg/L时,对Hela细胞的增殖抑制率超过70%。     

食用菌多糖的结构修饰及其修饰后的抗肿瘤活性研究进展

食用菌多糖是一种重要的生物大分子物质,具有多种生物活性。多糖的生物活性与本身的结构有着直接联系,因此,对多糖结构进行修饰,选择一个合适的修饰方法成为研究多糖的一个重要方向。大量的实验研究表明,选择合适的方法对食用菌多糖进行结构修饰,能够提高多糖的抗肿瘤活性,并降低多糖的毒副作用。本文主要简单地介绍了食用菌多糖结构修饰的方法包括硫酸化、羧甲基化、磷酸化、乙酰化等,以及食用菌多糖进行结构修饰后对肿瘤细胞的作用机制 在食用菌多糖结构修饰中,抗氧化、抗病毒、抗凝血、免疫调节等生物活性以及羧甲基化、磷酸化、乙酰化、烷基化等修饰方法还需要进一步研究。     

Marine-Derived Penicillium purpurogenum Reduces Tumor Size and Ameliorates Inflammation in an Erlich Mice Model

Background: This study addresses the antitumoral properties of Penicillium purpurogenum isolated from a polluted lagoon in Northeastern Brazil. Methods: Ethyl Acetate Extracellular Extract (EAE) was used. The metabolites were studied using direct infusion mass spectrometry. The solid Ehrlich tumor model was used for antitumor activity. Female Swiss mice were divided into groups (n = 10/group) as follows: The negative control (CTL−), treated with a phosphate buffered solution; the positive control (CTL+), treated with cyclophosphamide (25 mg/kg); extract treatments at doses of 4, 20, and 100 mg/kg; animals without tumors or treatments (Sham); and animals without tumors treated with an intermediate dose (EAE20). All treatments were performed intraperitoneally, daily, for 15 days. Subsequently, the animals were euthanized, and the tumor, lymphoid organs, and serum were used for immunological, histological, and biochemical parameter evaluations. Results: The extract was rich in meroterpenoids. All doses significantly reduced tumor size, and the 20 and 100 mg/kg doses reduced tumor-associated inflammation and tumor necrosis. The extract also reduced the cellular infiltration of lymphoid organs and circulating TNF-α levels. The extract did not induce weight loss or renal and hepatic toxic changes. Conclusions: These results indicate that P. purpurogenum exhibits immunomodulatory and antitumor properties in vivo. Thus, fungal fermentation is a valid biotechnological approach to the production of antitumor agents.     

窿缘桉内生真菌Chaetomium sp.Eef-10的鉴定及活性成分分析

【目的】确定内生真菌Eef-10的分类地位,分离和鉴定该真菌中的次生代谢产物并评价其抗细菌和抗肿瘤细胞活性,以期得到具有抗细菌和抗肿瘤活性的天然活性化合物。【方法】内生真菌的鉴定采用形态学和分子生物学相结合的方法;次生代谢产物的分离和纯化主要采用减压硅胶柱层析、葡聚糖凝胶LH-20和半制备高效液相色谱等方法;化合物的鉴定主要依据~1H NMR和~(13)C NMR等波谱学数据以及相关的参考文献;采用MTT显色法测定了次生代谢产物对5种不同供试细菌的抑制活性;采用CCK8法测定了次生代谢产物对2种不同癌细胞的抑制活性。【结果】从内生真菌Eef-10中分离到的3个化合物,分别鉴定为Atraric acid(化合物Ⅰ)、2, 4-二羟基-3, 6-二甲基苯甲酸乙酯(Ethyl 2, 4-dihydroxy-3, 6-dimethylbenzoate)(化合物Ⅱ)和4-甲基-5, 6-二氢-2H-吡喃-2-酮(4-methyl-5, 6-dihydro-2 H-pyran-2-one)(化合物Ⅲ)。化合物Ⅱ对5种革兰阴性细菌表现出强抑制活性,最大半数抑制质量浓度(IC_(50))为35.87～55.50μg/mL,化合物Ⅰ的IC_(50)为67.25～130.55μg/mL,化合物Ⅲ的IC_(50)均大于200μg/mL。抗肿瘤细胞活性的测定结果表明,化合物Ⅱ对人肝癌细胞株Hep-G2的IC_(50)为1.50μg/mL,活性强于阳性对照喜树碱(IC_(50)为3.6μg/mL)。【结论】从内生真菌Chaetomium sp. Eef-10中分离得到化合物Ⅰ～Ⅲ,化合物Ⅱ对桉树青枯病菌和Hep-G2细胞具有较好的抑制作用。     

翡翠贻贝糖胺聚糖的制备及其生理活性初探

探讨了翡翠贻贝中提取糖胺聚糖的蛋白酶水解及乙醇沉淀等条件，所制备的翡翠贻贝糖胺聚糖含GAG72.1%，经动物实验，当剂量为80mg/kg体重时，对昆明小鼠移植性肿瘤S-180的抑瘤率可达52.4%，且有增强免疫力的活性。     

翡翠贻贝糖胺聚糖的制备及其生理活性初探

探讨了翡翠贻贝中提取糖胺聚糖的蛋白酶水解及乙醇沉淀等条件，所制备的翡翠贻贝糖胺聚糖含GAG72.1%，经动物实验，当剂量为80mg/kg体重时，对昆明小鼠移植性肿瘤S-180的抑瘤率可达52.4%，且有增强免疫力的活性。     

药物共晶(HTHB)_4·(SiW_(12)O_(40))合成、表征及抗肿瘤活性研究

利用溶剂热法探索合成一种未见报道的四氢小檗碱与硅钨酸药物共晶(HTHB)_4·(Si W_(12)O_(40)),通过X-射线单晶衍射、IR、XRPD和TGA等方法确定结构。X-射线单晶衍射数据分析结果表明,该化合物属四方晶系,P4/n空间群,晶胞参数:a=23.7874(15)?,b=17.2595(16)?,c=23.7874(15)?,V=9 766.1(13)?3,F(000)=7 496,Z=4。体外抗肿瘤活性试验结果表明,相同药物浓度下药物共晶(HTHB)_4·(Si W_(12)O_(40))抗肿瘤活性优于四氢小檗碱和硅钨酸抗肿瘤活性。