Current pharmaceutical research is energetically excavating the pharmacotherapeutic role of herb-derived ingredients in multiple malignancies’ targeting. Luteolin is one of the major phytochemical components that exist in various traditional Chinese medicine or medical herbs. Mounting evidence reveals that this phytoconstituent endows prominent therapeutic actions on diverse malignancies, with the underlying mechanisms, combined medication strategy, and pharmacokinetics elusive. Additionally, the clinical trial and pharmaceutical investigation of luteolin remain to be systematically delineated. The present review aimed to comprehensively summarize the updated information with regard to the anticancer mechanism, combined medication strategies, pharmacokinetics, clinical trials, and pharmaceutical researches of luteolin. The survey corroborates that luteolin executes multiple anticancer effects mainly by dampening proliferation and invasion, spurring apoptosis, intercepting cell cycle, regulating autophagy and immune, inhibiting inflammatory response, inducing ferroptosis, and pyroptosis, as well as epigenetic modification, and so on. Luteolin can be applied in combination with numerous clinical anticarcinogens and natural ingredients to synergistically enhance the therapeutic efficacy of malignancies while reducing adverse reactions. For pharmacokinetics, luteolin has an unfavorable oral bioavailability, it mainly persists in plasma as glucuronides and sulfate-conjugates after being metabolized, and is regarded as potent inhibitors of OATP1B1 and OATP2B1, which may be messed with the pharmacokinetic interactions of miscellaneous bioactive substances in vivo. Besides, pharmaceutical innovation of luteolin with leading-edge drug delivery systems such as host–guest complexes, nanoparticles, liposomes, nanoemulsion, microspheres, and hydrogels are beneficial to the exploitation of luteolin-based products. Moreover, some registered clinical trials on luteolin are being carried out, yet clinical research on anticancer effects should be continuously promoted.

中文翻译：

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黄酮成分木犀草素：抗癌机制、联合用药策略、药代动力学、临床试验和药物研究


当前的药物研究正在积极挖掘草药成分在多种恶性肿瘤靶向中的药物治疗作用。木犀草素是存在于各种中药或草药中的主要植物化学成分之一。越来越多的证据表明，这种植物成分对多种恶性肿瘤具有显着的治疗作用，但其潜在机制、联合用药策略和药代动力学尚不清楚。此外，木犀草素的临床试验和药物研究仍有待系统地描述。本综述旨在全面总结木犀草素的抗癌机制、联合用药策略、药代动力学、临床试验和药学研究等方面的最新信息。研究证实，木犀草素主要通过抑制增殖和侵袭、促进细胞凋亡、拦截细胞周期、调节自噬和免疫、抑制炎症反应、诱导铁死亡和焦亡以及表观遗传修饰等多种抗癌作用。木犀草素可与临床上多种抗癌药及天然成分联合应用，协同增强恶性肿瘤的治疗效果，同时减少不良反应。就药代动力学而言，木犀草素具有不利的口服生物利用度，代谢后主要以葡萄糖苷酸和硫酸盐结合物的形式存留在血浆中，被认为是OATP1B1和OATP2B1的有效抑制剂，可能会干扰体内多种生物活性物质的药代动力学相互作用。 。 此外，木犀草素的药物创新以及主客体复合物、纳米颗粒、脂质体、纳米乳、微球和水凝胶等领先的药物递送系统也有利于木犀草素产品的开发。此外，一些木犀草素的注册临床试验正在进行中，但抗癌作用的临床研究仍需继续推进。