Anti-cancer, anti-diabetic and other pharmacologic and biological activities of penta-galloyl-glucose.
Anti-cancer, anti-diabetic and other pharmacologic and biological activities of penta-galloyl-glucose.
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DOI：
10.1007/s11095-009-9932-0
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发表时间：
2009-09
影响因子：
3.7
通讯作者：
Lü J
中科院分区：
文献类型：
--
作者：
Zhang J;Li L;Kim SH;Hagerman AE;Lü J
1, 2, 3, 4, 6-五-O-没食子酰-β-D-葡萄糖 (PGG) 是一种多酚化合物，富含多种草药。多项体外和体内研究表明，PGG 具有多种生物活性，这表明 PGG 在治疗和预防包括癌症和糖尿病在内的几种主要疾病方面具有巨大潜力。从化学和功能上来说，PGG 似乎与其成分没食子酸或茶多酚不同。对于抗癌活性，三项已发表的 PGG 体内临床前癌症模型研究支持了选择性抑制恶性肿瘤而不产生宿主毒性的良好功效。潜在机制包括抗血管生成、通过抑制 DNA 复制合成和 S 期阻滞以及 G1 期阻滞来抗增殖作用、诱导细胞凋亡、抗炎和抗氧化。假定的分子靶标包括 p53、Stat3、Cox-2、VEGFR1、AP-1、SP-1、Nrf-2 和 MMP-9。对于抗糖尿病活性，PGG 和类似物似乎可以改善葡萄糖的摄取。然而，人们对 PGG 的吸收、药代动力学和代谢及其毒性特征知之甚少。缺乏大量高纯度PGG一直是限制临床相关模型中癌症预防和治疗功效体内验证的瓶颈。
1, 2, 3, 4, 6-penta-O-galloyl-β-D-glucose (PGG) is a polyphenolic compound highly enriched in a number of medicinal herbals. Several in vitro and a handful of in vivo studies have shown that PGG exhibits multiple biological activities which implicate a great potential for PGG in the therapy and prevention of several major diseases including cancer and diabetes. Chemically and functionally, PGG appears to be distinct from its constituent gallic acid or tea polyphenols. For anti-cancer activity, three published in vivo preclinical cancer model studies with PGG support promising efficacy to selectively inhibit malignancy without host toxicity. Potential mechanisms include anti-angiogenesis, anti-proliferative actions through inhibition of DNA replicative synthesis and S-phase arrest and also G1 arrest, induction of apoptosis, anti-inflammation and anti-oxidation. Putative molecular targets include p53, Stat3, Cox-2, VEGFR1, AP-1, SP-1, Nrf-2 and MMP-9. For anti-diabetic activity, PGG and analogues appear to improve glucose uptake. However, very little is known about the absorption, pharmacokinetics and metabolism of PGG, nor its toxicity profile. The lack of large quantity of highly pure PGG has been a bottleneck limiting in vivo validation of cancer preventive and therapeutic efficacies in clinically relevant models.
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影响因子：
2.5
作者：
Choi, BM;Kim, HJ;Chung, HT
通讯作者：
Chung, HT
影响因子：
5.1
作者：
Dong, H;Chen, SX;Xu, HX
通讯作者：
Xu, HX
影响因子：
2.7
作者：
Feldman, KS;Sahasrabudhe, K;Scheuchenzuber, WJ
通讯作者：
Scheuchenzuber, WJ
影响因子：
5.6
作者：
Cavalher-Machado, Simone Campos;Rosas, Elaine Cruz;Mueller de Oliveira Henriques, Maria das Gracas
通讯作者：
Mueller de Oliveira Henriques, Maria das Gracas
影响因子：
3.1
作者：
Binkley, Robert C.;Ziepfel, Jessica C.;Himmeldirk, Klaus B.
通讯作者：
Himmeldirk, Klaus B.