Taira Nozomi, Nguyen Binh Cao Quan, Be Tu Pham Thi, Tawata Shinkichi
Department of Bioscience and Biotechnology, The United Graduate School of Agricultural Sciences, Kagoshima University , Kagoshima 890-0065, Japan.
Department of Bioscience and Biotechnology, Faculty of Agriculture, University of the Ryukyus , Senbaru 1, Nishihara-cho, Okinawa 903-0213, Japan.
J Agric Food Chem. 2016 Jul 13;64(27):5484-9. doi: 10.1021/acs.jafc.6b01785. Epub 2016 Jul 1.
Propolis from different areas has been reported to inhibit oncogenic/aging kinase PAK1, which is responsible for a variety of conditions, including cancer, longevity, and melanogenesis. Here, a crude extract of Okinawa propolis (OP) was tested against PAK1 activity, Caenorhabditis elegans (C. elegans) longevity, melanogenesis, and growth of cancer cells. We found that OP blocks PAK1 and exhibits anticancer activity in the A549 cell (human lung cancer cell) line with IC50 values of 6 μg/mL and 12 μg/mL, respectively. Most interestingly, OP (1 μg/mL) significantly reduces reproduction and prolongs the lifespan of C. elegans by activating the HSP-16.2 gene, as shown in the PAK1-deficient strain. Furthermore, OP inhibits melanogenesis in a melanoma cell line (B16F10) by downregulating intracellular tyrosinase activity with an IC50 of 30 μg/mL. Our results suggest that OP demonstrated a life span extending effect, C. elegans, anticancer, and antimelanogenic effects via PAK1 inactivation; therefore, this can be a potent natural medicinal supplement against PAK1-dependent diseases.
据报道，来自不同地区的蜂胶可抑制致癌/衰老激酶PAK1，PAK1与多种病症有关，包括癌症、寿命和黑色素生成。在此，对冲绳蜂胶（OP）的粗提物进行了PAK1活性、秀丽隐杆线虫（线虫）寿命、黑色素生成及癌细胞生长方面的测试。我们发现，OP可阻断PAK1，并在A549细胞（人肺癌细胞）系中表现出抗癌活性，其IC50值分别为6μg/mL和12μg/mL。最有趣的是，如在PAK1缺陷菌株中所示，OP（1μg/mL）通过激活HSP-16.2基因显著降低线虫的繁殖率并延长其寿命。此外，OP通过下调细胞内酪氨酸酶活性，在黑色素瘤细胞系（B16F10）中抑制黑色素生成，IC50为30μg/mL。我们的结果表明，OP通过PAK1失活表现出延长寿命、对线虫、抗癌及抗黑色素生成的作用；因此，它可能是一种针对PAK1依赖性疾病的有效天然药物补充剂。
