Laboratory of Pharmacognosy and Natural Product Derived Medicine, College of Pharmacy, Chung-Ang University, Seoul 06974, Korea.
Molecules. 2021 Jun 23;26(13):3830. doi: 10.3390/molecules26133830.
(AS) is distributed in Korea, Japan, China, and Russia and has reported anti-oxidant, anti-inflammatory, and reducing activities on atopic dermatitis-like skin lesions, along with other beneficial health properties. In the present study, we tried to prove the cancer-preventive activity against prostate cancer. The extracted and isolated compounds, oregonin (), hirsutenone (), and hirsutanonol (), which were isolated from AS, were tested for anti-proliferative activity. To do this, we used the MTT assay; NF-κB inhibitory activity, using Western blotting; apoptosis-inducing activity using flow cytometry; DNA methylation activity, using methylation-specific polymerase chain reaction in androgen-dependent (LNCaP) and androgen-independent (PC-3) prostate cancer cell lines. The compounds (-) showed potent anti-proliferative activity against both prostate cancer cell lines. Hirsutenone () exhibited the strongest NF-κB inhibitory and apoptosis-inducing activities compared with oregonin () and hirsutanonol (). DNA methylation activity, which was assessed for hirsutenone (), revealed a concentration-dependent enhancement of the unmethylated DNA content and a reduction in the methylated DNA content in both PC-3 and LNCaP cells. Overall, these findings suggest that hirsutenone (), when isolated from AS, may be a potential agent for preventing the development or progression of prostate cancer.
（AS）分布于韩国、日本、中国和俄罗斯，具有抗氧化、抗炎和减轻特应性皮炎样皮肤损伤的作用，以及其他有益的健康特性。在本研究中，我们试图证明其对前列腺癌的预防作用。从 AS 中提取和分离的化合物，包括 oregonin()、hirsutenone()和 hirsutanonol()，进行了抗增殖活性测试。为此，我们使用 MTT 法；NF-κB 抑制活性，采用 Western blot 法；采用流式细胞术检测细胞凋亡诱导活性；采用甲基化特异性聚合酶链反应检测雄激素依赖性（LNCaP）和雄激素非依赖性（PC-3）前列腺癌细胞系中的 DNA 甲基化活性。这些化合物（-）对两种前列腺癌细胞系均表现出强烈的抗增殖活性。与 oregonin()和 hirsutanonol()相比，hirsutenone()表现出最强的 NF-κB 抑制和细胞凋亡诱导活性。对 hirsutenone()进行的 DNA 甲基化活性评估显示，在 PC-3 和 LNCaP 细胞中，未甲基化 DNA 含量呈浓度依赖性增加，甲基化 DNA 含量降低。总的来说，这些发现表明，从 AS 中分离出的 hirsutenone()可能是预防前列腺癌发生或进展的潜在药物。
