College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, China.
College of Pharmacy, School of Medicine, Hangzhou Normal University, Hangzhou 311121, China.
Molecules. 2021 Mar 10;26(6):1499. doi: 10.3390/molecules26061499.
Natural products are important sources for drug discovery, especially anti-tumor drugs. β-Elemene, the prominent active ingredient extract from the rhizome of , is a representative natural product with broad anti-tumor activities. The main molecular mechanism of β-elemene is to inhibit tumor growth and proliferation, induce apoptosis, inhibit tumor cell invasion and metastasis, enhance the sensitivity of chemoradiotherapy, regulate the immune system, and reverse multidrug resistance (MDR). Elemene oral emulsion and elemene injection were approved by the China Food and Drug Administration (CFDA) for the treatment of various cancers and bone metastasis in 1994. However, the lipophilicity and low bioavailability limit its application. To discover better β-elemene-derived anti-tumor drugs with satisfying drug-like properties, researchers have modified its structure under the premise of not damaging the basic scaffold structure. In this review, we comprehensively discuss and summarize the potential anti-tumor mechanisms and the progress of structural modifications of β-elemene.
天然产物是药物发现的重要来源，特别是抗肿瘤药物。β-榄香烯是从莪术根茎中提取的主要活性成分，是一种具有广泛抗肿瘤活性的代表性天然产物。β-榄香烯的主要分子机制是抑制肿瘤生长和增殖、诱导细胞凋亡、抑制肿瘤细胞侵袭和转移、增强放化疗敏感性、调节免疫系统、逆转多药耐药（MDR）。榄香烯口服乳和榄香烯注射液于 1994 年获得中国食品药品监督管理局（CFDA）批准，用于治疗各种癌症和骨转移。然而，其亲脂性和低生物利用度限制了其应用。为了发现具有更好的药物样特性的更好的源于β-榄香烯的抗肿瘤药物，研究人员在不破坏基本骨架结构的前提下对其结构进行了修饰。在这篇综述中，我们全面讨论和总结了β-榄香烯的潜在抗肿瘤机制和结构修饰的进展。
