Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Assiut, Egypt.
Pharm Biol. 2013 Aug;51(8):1026-34. doi: 10.3109/13880209.2013.775160. Epub 2013 Jun 14.
Polygonum species have been used in the treatment of several types of inflammatory disorders and cancer. Nevertheless, there are no reports related to the anti-inflammatory and anti-proliferative activities of Polygonum bellardii All. (Polygonaceae).
This study investigated the chemical composition of the methanol extract of P. bellardii. The anti-inflammatory and cytotoxic activities of methanol, n-butanol, ethyl acetate extracts and isolated polyphenols were determined.
The chemical structure of the isolated compounds was elucidated using different spectral techniques. MTT assay was used to evaluate the anti-proliferative activity in HeLa, MCF-7 and HepG-2 cells. Inhibition of 5-lipoxygenase (5-LOX) activity and prostaglandin E2 (PGE2) production in stimulated HepG-2 cells were used to assess the anti-inflammatory activity.
The present study resulted in isolation of five compounds (new for the species). They were identified as gallic acid (1), quercetin (2), myricetin (3), quercetin-3-O-β-D-glucopyranoside (5) and myricetin-3-O-α-arabinofuranoside (7). Additionally, a couple of previously isolated compounds such as quercetin-3-O-(5″-acetyl-α-arabinofuranoside) (4) and myricetin-3-O-(5″-acetyl-α-arabinofuranoside) (6) were detected. The n-butanol extract has the highest cytotoxicity in HeLa, MCF-7 and HepG-2 cells, with IC₅₀ values of 15.26, 50.66 and 30.09 µg/ml, respectively. Compound 6 exhibited a marked cytotoxicity in HeLa (IC₅₀ 75.04 µg/ml) and HepG-2 (IC₅₀ 41.03 µg/ml) cells. Crude extracts and pure compounds inhibited the 5-LOX activity and PGE2 production in a dose-dependent manner (0.1-250 µg/ml).
These results explain the traditional uses of P. bellardii and indicate that polyphenols, despite structural similarity, have different cytotoxic and anti-inflammatory effects.
Polygonum 属植物被用于治疗多种炎症性疾病和癌症。然而，目前尚无有关 Bellardia Polygonum All.（Polygonaceae）的抗炎和抗增殖活性的报道。
本研究调查了 Bellardia Polygonum All.甲醇提取物的化学成分。测定了甲醇、正丁醇、乙酸乙酯提取物和分离得到的多酚的抗炎和细胞毒性活性。
采用不同的光谱技术解析分离得到的化合物的化学结构。MTT 法评价化合物在 HeLa、MCF-7 和 HepG-2 细胞中的抗增殖活性。通过抑制 5-脂氧合酶（5-LOX）活性和刺激 HepG-2 细胞中前列腺素 E2（PGE2）的产生来评估抗炎活性。
本研究分离得到了五个化合物（该种新化合物）。它们分别被鉴定为没食子酸（1）、槲皮素（2）、杨梅素（3）、槲皮素-3-O-β-D-吡喃葡萄糖苷（5）和杨梅素-3-O-α-阿拉伯呋喃糖苷（7）。此外，还检测到两种先前分离得到的化合物，即槲皮素-3-O-（5″-乙酰基-α-阿拉伯呋喃糖苷）（4）和杨梅素-3-O-（5″-乙酰基-α-阿拉伯呋喃糖苷）（6）。正丁醇提取物在 HeLa、MCF-7 和 HepG-2 细胞中表现出最高的细胞毒性，IC₅₀值分别为 15.26、50.66 和 30.09 µg/ml。化合物 6 在 HeLa（IC₅₀ 75.04 µg/ml）和 HepG-2（IC₅₀ 41.03 µg/ml）细胞中表现出显著的细胞毒性。粗提取物和纯化合物以剂量依赖的方式抑制 5-LOX 活性和 PGE2 的产生（0.1-250 µg/ml）。
这些结果解释了 Bellardia Polygonum All.的传统用途，并表明尽管结构相似，但多酚类化合物具有不同的细胞毒性和抗炎作用。
