金顶侧耳多糖PC—4的结构确定与抗肿瘤活性的研究

３％氯乙酸浸提过的金顶侧耳子实体中分离纯化另一水溶性多糖ＰＣ－４。该多糖分子量经为１８９ｋＤ。纸层析与气相层析分析表明其为单一聚糖。经高磺酸氧化,Ｓｍｉｔｈ降解,甲基化,层析,气质联机分析,核磁其振（Ｈ－ＮＭＲ,１３Ｃ－ＮＭＲ）谱及红外光谱测定等,可确定Ｃ－４的主链结构由β－（１→３）糖苷键相连的葡萄糖构成,部份残基Ｃ６,上带有分支。约每５个糖残基有两个侧链,侧链仅为１个葡萄糖残基。     

金顶侧耳酸提水溶性多糖的研究——PC-3的分离、纯化与结构确定

金顶侧耳(Pleurotus citrinopileatus)子实体的3%三氯乙酸提取液经甲醇分级,十六烷基三甲基溴化铵等进一步提纯得到水溶性多糖PC-3。经Sepharose CL-4B柱层析,醋酸纤维素薄膜电泳、聚丙烯酰胺凝胶电泳鉴定,PC-3为均一级份。G.C.与P.C.分析表明,Gal、Man为该多糖的组份,其单糖摩尔比为2.5∶1.0。PC-3的分子量约为67000,比旋光度[α]_D~(18°)=+28°。经核磁共振谱等分析,PC-3不含β型糖苷键。部份酸水解、高碘酸氧化、Smith降解、完全甲基化、G.C.及G.C.-M.S.的分析表明,PC-3是由α(1→6)糖苷键相连的半乳糖构成分子的主链,部分残基C_2上带有分支,每5个Gal残基带有1个侧链,侧链为α(1-2)Man-α(1-2)Man。     

猴头菌水溶性多糖的分离纯化与结构表征

从猴头菌子实体中分离得到一种新型的水溶性杂多糖HEPF2,分子量大小为1.66′104Da,该多糖由岩藻糖、半乳糖和葡萄糖以1.00:3.69:5.42比例构成,同时也含有微量的3-O-甲基鼠李糖。进一步利用傅立叶变换红外光谱法、糖组成分析、甲基化分析、部分酸水解法和核磁共振法等方法进行结构鉴定,检测结果表明,该杂多糖中包含1→4、1→6结合的葡萄糖和1→6结合的半乳糖残基,连接于主链的侧链残基,包括岩藻糖残基、少数的端基葡萄糖和半乳糖残基。核磁共振法检测结果还表明,1→4结合葡萄糖为β构型,(1→6)结合半乳糖、(1→2,6)结合半乳糖和端基葡萄糖均为α构型。     

短裙竹荪多糖Dd-S3P的分离纯化及其性质研究

短裙竹荪子实体经2％Na2CO3溶液提取,用蛋白酶法和Sevag法相结合除去蛋白,乙醇分级沉淀,级分3经DEAE－SephadexA－25柱层析纯化得到短裙竹蒸蒸荪多糖DdS3P．经测定该多糖为均一组分,分子量约为3．8×105,红外光谱呈现出典型的多糖吸收峰,含有α-型糖苷连接键,紫外扫描无核酸和蛋白质的特征吸收峰．纸层析和气相层析分析得知Dd－S3P含有D-葡萄糖（D－Glc）、D-甘露糖（D－Man）和D-木糖（D－Xyl）,其摩尔比为1．83：1．00：1．21．经动物试验表明此多糖对小鼠S-180有一定的抑制作用,抑瘤率约31．3％．     

金针菇(Flammulina Velutipes(Curt.ex Fr.)Sing.)子实体多糖PA_(5)DE的提取及性质研究

 从金针菇Flammulina velutipes(Curt.ex Fr.)Sing.子实体中提取水溶性多糖,经乙醇分级,DEAE-Sephadex A-25纯化,得PA_5DE。以聚丙烯酰胺凝胶电泳和凝胶柱Sepharose 4B层析证明是化学均一性多糖,分子量是47.1万。用GLC、I.R、~13C-N.M.R.分析表明含有D-葡萄糖、D-甘露糖、D-岩藻糖。PA_5DE分子可能具有分支结构,含β-型糖苷键,存在β(1→3)和β(1→6)型糖苷键连接,并有抑制肿瘤S-180的活性。     

引种西洋参叶水溶性多糖的研究——中性多糖PN的分离、纯化与结构分析

从引种西洋参中提取的水溶性多糖,经分离纯化得一分子量较小的中性多糖——PN。PN的分子量为7.4kD,主要成份为葡萄糖。经Sepbadex G-50凝胶柱层析和电泳方法分析为均一级份。经纤维素酶解,部分酸水解,高碘酸盐氧化和smith降解,红外光谱,甲基化,~(13)C-NMR分析表明,其具多分枝结构,分子主链由β-(1-4)连接的葡萄糖构成。分枝点率为25％,分枝点为0—6,其它残基在侧链上,分枝率为47.8％。     

梭柄松苞菇多糖组分的部分理化性质及对S-180瘤抑制活性研究

【目的】分离和纯化梭柄松苞菇子实体多糖, 并对其结构和抗肿瘤活性进行研究。【方法】采用热水浸提法提取梭柄松苞菇子实体多糖, 采用DE-52纤维素柱和Sephadex G-100进行多糖的分离纯化, HPGPC测定多糖分子量, HPLC测定单糖组成, 红外光谱进行结构分析, 甲基化实验测定连接方式, 核磁共振测定异头碳构型, 采用S-180荷瘤小鼠模型对梭柄松苞菇子实体多糖抗肿瘤活性进行研究, 并测定了荷瘤小鼠血清细胞因子TNF-α、IL-2和IL-6的含量。【结果】从梭柄松苞菇子实体中分离纯化得到多糖命名为CVP-A, 结果表明, CVP-A平均分子量为10 289, 单糖组成主要为葡萄糖, 还含有少量木糖, 含量比约为15:2, 甲基化实验, 核磁共振以及红外光谱分析结果表明CVP-A主链为(1→4)-α-D-葡聚糖, 侧链连接在主链葡萄糖残基2号碳位置, S-180荷瘤小鼠模型实验表明, CVP-A对实验性S-180实体瘤具有较好的抑制作用, 连续10 d腹腔注射25、50和75 mg/(kg·d) CVP-A的昆明小鼠的肿瘤抑制率分别为31.99%、42.68%和60.18%, 小鼠血清细胞因子测定表明, CVP-A能提高荷瘤小鼠血清TNF-α、IL-2和IL-6的含量。【结论】梭柄松苞菇多糖可能作为一个潜在的抗癌药物而开发利用。     

徐长卿中一种新葡聚糖化学结构的研究

从常用中药徐长卿中获得一分子量为 1.5× 10 4 的多糖CPB 1。比旋光度 [α]D= 15 1.4°(0 .96 ,H2 O)。单糖组成分析表明仅含葡萄糖。甲基化分析、部分酸水解、乙酰解、IR及NMR数据表明CPB 1的主链由α D 1,4连接的葡萄糖残基组成 ,其侧链由 1,4和 1,6连接的葡萄糖残基构成。每五个葡萄糖残基组成的重复单元中含有一个分枝 ,位于主链葡萄糖残基的O 6位上     

轻度降解核磁共振法研究多糖链结构

 建立了轻度降解~(13)C核磁共振法研究多糖结构的方法。美国瓜胶和国产胶1在70℃下用90％甲酸降解3小时。用Bio-Gel p-4的凝胶色谱分离。含20个以上糖残基的片断为主要降解成份。用~(13)C核磁共振法研究,确定它们都是具有以β1-4甘露糖为骨架,其中某些甘露糖的6位碳有α-半乳糖侧链的结构。这些结果与组成分析和甲基化分析结果一致。     

根瘤菌TISTR 386胞外酸性多糖的结构研究

根瘤菌TISTR 386胞外酸性多糖有二种九糖的重复单位构成。重复单位主要成份是D一葡萄糖,D一半乳糖和D一葡萄糖醛酸,它们的克分子比例分别是6：l：2和5：2：2。另外还含有一些丙酮酸和醋酸。甲基化分析表明,这个多糖由一个(1→3)键,一个(1→6)键,三个(1→4)键,一个(1→4,1→6)键连结的葡萄糖残基,一个(1→3)键连结的D-半乳糖残基,以及一个(1→3)键,一个(1→4)键连结的D-葡萄糖醛酸残基所组成。非还原末端糖残基是D葡萄糖或是带有丙酮酸的D一半乳糖,这也是二种九糖重复单位区别所在。     

Growth-inhibitory activity of the d-mannan of saccharomyces cerevisiae X2180-1A-5 mutant strain against mouse-implanted sarcoma 180 and ehrlich-carcinoma solid tumor

The d-mannan of Saccharomyces cerevisiae X2180-1A-5 mutant strain, which possesses a main chain composed of α-(1→6) linked d-mannopyranosyl residues and a small proportion of branches composed of α-(1→2)- and α-(1→3)-linked d-mannopyranosyl residues, showed strong growth-inhibitory activity against mouse-implanted Sarcoma 180 and Ehrlich-carcinoma solid tumor. The observation that the level of this activity was nearly identical with that of the d-mannan of a wild-type strain of bakers' yeast, which possesses a high proportion of branches composed of α-(1→2)- and α-(1→3)-linked d-mannopyranosyl residues, suggests that the branches are not essential for antitumor activity. The partial acid-degradation products of both d-mannans, the molecular weight of which was one-third of that of each parent d-mannan, had only one half of the antitumor activity of the parent d-mannans. This suggests that molecular size is the most important factor for the differences in activity of the polysaccharides of wild and mutant strains.     

Structural Characterization of an Alkali-Soluble Polysaccharide from Angelica sinensis and Its Antitumor Activity in Vivo

A novel alkali-soluble polysaccharide (AASP) was isolated from Angelica sinensis (Oliv.) Diels under aqueous alkali treatment, and its structural characterization and antitumor activity in Vivo were evaluated in present study. Results of HPGPC and IC revealed that AASP was a neutral polysaccharide containing Ara, Gal and Glc in the mole ratio of 1.00 : 2.26 : 24.43, with the average molecular weight of 4.7 kDa. Periodate oxidation, Smith degradation, methylation, FT-IR, and NMR analyses further demonstrated that a preliminary structure of AASP was proposed as follows: (1→3)-linked arabinose, (1→6)-linked galactose, and (1→), (1→4), (1→6), (1→3,6)-linked glucose with α- and β-configuration. In Vivo antitumor assays, AASP exhibited prominent antitumor effects on H22 hepatoma cells with an inhibitory ratio of 48.57 % and effectively protected thymuses and spleens of tumor-bearing mice. Besides, AASP displayed a proliferation stimulating activity of immunocytes (splenocytes, peritoneal macrophages and natural killer cells), and an auxo-action for cytokines release (TNF-α, IL-2 and IFN-γ), leading to the apoptosis of H22 solid tumors cells via G0/G1 phase arrested. The above data demonstrated that AASP holds great application potential to be a safe and effective antitumor supplement in the future.     

Correlation of structure to antitumor activities of five derivatives of a beta-glucan from Poria cocos sclerotium

A water-insoluble (1-->3)-beta-D-glucan isolated from fresh sclerotium of Poria cocos was, respectively, sulfated, carboxymethylated, methylated, hydroxyethylated, and hydroxypropylated, to afford five water-soluble derivatives. Their weight-average molecular masses (Mw) and intrinsic viscosities ([eta]) were determined by size-exclusion chromatography combined with laser light scattering (SEC-LLS), LLS, and viscometry in phosphate buffer solution (PBS) at 37 degrees C. The antitumor activities, against Sarcoma 180 tumor cell (S-180) and gastric carcinoma cell strain (MKN-45 and SGC-7901) of the native beta-glucan and the five derivatives, were tested in vitro and in vivo. The Mw values of the five derivatives in PBS were determined to be 3.8 x 10(4), 18.9 x 10(4), 16.0 x 10(4), 76.8 x 10(4), and 224.3 x 10(4), respectively. The high Mw values of the hydroxyethylated and hydroxypropylated derivatives in aqueous solution resulted from aggregation, and their true Mw values obtained in dimethyl sulfoxide were 20.1 x 10(4) and 19.1 x 10(4). The sulfated and carboxymethylated derivatives having DS of 1.0-1.3 show good water solubility, and exist as relatively expanded chains in aqueous solution. Interestingly, the native beta-glucan did not show antitumor activity, whereas the sulfated and carboxymethylated derivatives exhibit significant antitumor activities against S-180 and gastric carcinoma tumor cells. This work showed that good water solubility, relatively high chain stiffness, and moderate molecular mass of the derivatives in aqueous solution contribute beneficial to enhancement of antitumor activity.     

化学修饰对金顶侧耳多糖抗病毒（CB_5）活性的影响

从金顶侧耳子实体中分离纯化一半乳甘露聚糖ＰＣ－３,其分子量约为６７ｋＤ,一级结构为α（１→６）糖苷键相连的Ｇａｌ构成分子的主链,部份残基Ｃ_２上带有分支,分支结构为α（１－２）Ｍａｎ－α（１－２）Ｍａｎ。按高碘酸氧化、部份酸水解,甲基化、硫酸化程序对ＰＣ－３的结构进行化学修饰;并分别将ＰＣ－３及其衍生物与柯萨奇病毒Ｂ_５进行体外实验,结果表明,ＰＣ－３经硫酸化后,显著地提高了抗病毒活性;而高碘酸氧化,甲基化,部份酸水解产物则降低了抗ＣＢ_５的活性。     

Synthesis and anticancer evaluation of thiazolyl-chalcones

Thirty-seven (E)-1-(4-methyl-2-arylaminothiazol-5-yl)-3-arylprop-2-en-1-ones were synthesized via Claisen-Schmidt condensation of 1-(4-methyl-2-(arylamino)thiazol-5-yl)ethanone with the corresponding arylaldehydes. All these thiazolyl-chalcones were characterized and evaluated by MTT assay on human cancer cell lines BGC-823, PC-3, NCI-H460, BEL-7402 in vitro. Compounds 5, 8, 26, 37 and 41 are effective against cancer cell lines with IC(50)s below 10 μM. The antitumor activity in ICR mice bearing sarcoma 180 tumors indicates compounds 10 and 41 have moderate in vivo activity with 22-25% tumor-weight inhibition.     

Purification and properties of the endo-1,4-β-glucanase III from Ruminococcus albus

Endoglucanase III (EGIII) was purified from Ruminococcus albus culture supernatant. An enzyme having a molecular weight of 53,000 was stabilized by mercaptoethanol and inhibited by sulfhydryl group-blocking reagents, and exhibited its highest CMC-degrading activity of pH 5.7 and 55°C. The enzyme hydrolyzed cellobiose (G2) and cellotriose (G3) only negligibly, but significantly hydrolyzed cellotetraose (G4), cellopentaose (G5) and cellohexaose (G6). The major hydrolysis reactions conducted by the enzyme were G4→2G2, G5→G2+G3, G6→G2+G4 and G6→2G3. The V_max values of these reactions increased remarkably while the K_m values decreased significantly with an increase in degree of polymerization of the substrate.     

Antitumor activity of recombinant human tumor necrosis factor in combination with hyperthermia against heterotransplanted human prostatic carcinoma and its lymph node metastasis in nude mice.

The antitumor activity of recombinant human tumor necrosis factor (rhTNF) against heterotransplanted human prostatic carcinoma (PC-3) and spontaneous lymphatic tumor metastasis was studied in vivo. The spontaneous lymphatic metastasis of PC-3 tumor was found in approximately 50% of cases. Significant antitumor activity was observed with repeated intratumoral administration of a large dose of rhTNF, not only on the subcutaneous tumor xenografts but also on the lymph node metastases. Strong antitumor activity could be achieved even with the intratumoral administration of a small dose of rhTNF in combination with mild hyperthermia on either the transplanted tumors or on the metastatic tumors.     

Sulfation of (1→3)-β-d-glucan from the fruiting bodies of Russula virescens and antitumor activities of the modifiers

A water-insoluble (1→3)-β-d-glucan isolated from the fresh fruiting bodies of Russula virescens was sulfated using sulfur trioxide-pyridine complex as reagent in dimethyl sulfoxide. Depending on the reaction conditions, the products showed different degrees of sulfation (DS) ranging from 0.17 to 1.17 and different weight average molecular weights (M_ws) ranging from 2.5 × 10⁴ to 1.2 × 10⁵ Da. Moreover, the antitumor activities of the five sulfated derivatives against Sarcoma 180 tumor cell were tested both in vitro and in vivo. The results indicated that the native (1→3)-β-d-glucan did not show antitumor activity, while the sulfated derivatives exhibited enhanced antitumor activities. This study demonstrated that DS and M_w could influence the antitumor activities of the sulfated derivatives.