Dali University, Dali, China.
Integr Cancer Ther. 2011 Sep;10(3):NP12-23. doi: 10.1177/1534735411413467. Epub 2011 Jul 6.
The organic extract of Periplaneta americana L. (Dictyoptera; Blattidae) has been traditionally used in southwestern China as an alternative medicine against disorders such as hepatitis, trauma, gastric ulcers, burns, and heart disease. The present study describes bioassay-guided purification and chemotherapeutic evaluation of the 60% ethanolic fraction of P americana organic extracts (PAE60). The most effective cytotoxic fraction was determined by way of repeated in vitro screenings against 12 distinct cultured human carcinoma cell lines: Eca 109, BGC823, HO8910, LS174T, CNE, HeLa, K562, PC-3, A549, BEL 7404, HL-60, and KB, followed by in vivo antitumor assays of the lead fraction (PAE60). The complexity of enriched active fraction was qualitatively evaluated using thin layer chromatography. Reconstituted PAE60 was effective at inhibiting HL-60, KB, CNE, and BGC823 cell growth with IC(50) values <20 µg mL-(1). PAE60 reduced tumor growth in S180-bearing immunocompetent mice by 72.62% after 10 days following oral doses of 500 mg kg d-(1) compared with 78.75% inhibition following 40 mg kg d-(1) of cyclophosphamide (CTX). Thymus and spleen indices of S180-bearing mice treated with PAE60 were significantly greater (P < .05) than CTX treatment groups, suggesting potential immunomodulation of antitumor host defenses by PAE60. Antiviral activity was also investigated and PAE60 inhibited herpes simplex type-2 replication (IC(50) = 4.11 ± 0.64 µg mL-(1)) with a selectivity index (CC(50) to IC(50) ratio) of 64.84 in Vero cells but was less effective on type-1 virus (IC(50) of 25.6 ± 3.16 µg mL-(1)). These results support future clinical trials on P. americana as an alternative or complementary medicinal agent.
美洲大蠊（蜚蠊目；蜚蠊科）的有机提取物在我国西南地区一直被用作治疗肝炎、创伤、胃溃疡、烧伤和心脏病等疾病的替代药物。本研究描述了对美洲大蠊 60%乙醇提取物（PAE60）的生物活性指导的分离和化学治疗评估。通过对 12 种不同培养的人癌细胞系（Eca 109、BGC823、HO8910、LS174T、CNE、HeLa、K562、PC-3、A549、BEL 7404、HL-60 和 KB）进行反复的体外筛选，确定了最有效的细胞毒性级分，然后对该先导级分（PAE60）进行体内抗肿瘤试验。采用薄层层析法对富含活性级分的复杂性进行定性评价。再构成的 PAE60 对 HL-60、KB、CNE 和 BGC823 细胞生长的抑制作用具有 IC50 值<20μg mL-1（1）。PAE60 经口给予 500mg kg d-1（1）后，在第 10 天可使 S180 荷瘤免疫功能正常的小鼠肿瘤生长减少 72.62%，而 40mg kg d-1（1）环磷酰胺（CTX）的抑制率为 78.75%。用 PAE60 治疗的 S180 荷瘤小鼠的胸腺和脾脏指数明显大于 CTX 治疗组（P<.05），表明 PAE60 对抗肿瘤宿主防御具有潜在的免疫调节作用。还研究了抗病毒活性，PAE60 抑制单纯疱疹 2 型复制（IC50=4.11±0.64μg mL-1），在 Vero 细胞中的选择性指数（CC50/IC50 比值）为 64.84，但对 1 型病毒的作用较弱（IC50 为 25.6±3.16μg mL-1）。这些结果支持对美洲大蠊进行临床试验，作为替代或补充药物。
