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化学修饰增强灰树花多糖肽的体外和体内抗癌活性。

Enhancement of in vitro and in vivo anticancer activities of polysaccharide peptide from Grifola frondosa by chemical modifications.

机构信息

Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Hong Kong SAR, China.

出版信息

Pharm Biol. 2011 Nov;49(11):1114-20. doi: 10.3109/13880209.2011.569557. Epub 2011 May 20.

Abstract

CONTEXT

Grifola frondosa (Polyporaceae), maitake, is a widely consumed edible mushroom in some Asian countries. The fruit bodies and mycelia of maitake have shown different bioactive compounds with anticancer and other therapeutic properties.

OBJECTIVE

This study evaluated three chemically modified maitake polysaccharide-peptides' (MPSP) adjuvant effect (in vivo) and anticancer activity (in vitro growth inhibitory effect) compared with crude MPSP from G. frondosa.

MATERIALS AND METHODS

We investigated the possibility of enhancing the adjuvant effect and anticancer effect of crude MPSP by using simple chemical modification methods to convert crude MPSP to phosphorylated, acetylated or esterified MPSPs. The adjuvant effect and growth inhibitory effect were evaluated by C6 cell inoculated rat model with cyclophosphamide (CPA) treatment and in vitro cell viability assay, respectively.

RESULTS

All four tested MPSPs showed significant adjuvant effect to CPA treatment on rats inoculated with C6 cancer cells. In addition, an obvious growth inhibitory effect was observed in C6 cancer cells but not in normal brain cells treated with various forms of MPSPs. Only phosphorylation could significantly (p < 0.05) improve the adjuvant effect (in vivo) and growth inhibitory effect. A same rank order (phosphorylated MPSP > esterified MPSP ≥ acetylated MPSP ≥ crude MPSP) of efficacy was observed in both the in vivo and in vitro assays.

DISCUSSION AND CONCLUSION

This study showed chemical phosphorylation could markedly enhance both adjuvant effects and growth inhibitory effects. This study demonstrated the feasibility of enhancing the efficacy of MPSP by using a simple chemical modification method, and this provides a foundation for future study in this area.

摘要

背景

灰树花(多孔菌科),舞茸,是亚洲一些国家广泛食用的一种食用菌。舞茸的子实体和菌丝体表现出不同的具有抗癌和其他治疗特性的生物活性化合物。

目的

本研究评估了三种化学修饰的舞茸多糖肽(MPSP)的佐剂效应(体内)和抗癌活性(体外生长抑制作用),并与灰树花子实体中的粗 MPSP 进行了比较。

材料和方法

我们研究了通过使用简单的化学修饰方法将粗 MPSP 转化为磷酸化、乙酰化或酯化 MPSP,来增强粗 MPSP 的佐剂效应和抗癌作用的可能性。通过用环磷酰胺(CPA)处理接种 C6 癌细胞的大鼠模型评估佐剂效应,通过体外细胞活力测定评估生长抑制效应。

结果

四种测试的 MPSP 均表现出对 C6 癌细胞接种大鼠的 CPA 治疗有显著的佐剂作用。此外,在 C6 癌细胞中观察到明显的生长抑制作用,但在未用各种形式的 MPSP 处理的正常脑细胞中未观察到。只有磷酸化能显著(p<0.05)提高佐剂效果(体内)和生长抑制效果。在体内和体外试验中均观察到相同的效力等级(磷酸化 MPSP>酯化 MPSP≥乙酰化 MPSP>粗 MPSP)。

讨论与结论

本研究表明,化学磷酸化可以显著增强佐剂作用和生长抑制作用。本研究表明,通过使用简单的化学修饰方法增强 MPSP 的疗效是可行的,为该领域的进一步研究提供了基础。

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