Division of Cardiology, Department of Internal Medicine, Shuang Ho Hospital, Ministry of Health and Welfare, Taipei Medical University, New Taipei City 23561, Taiwan.
Department of Medical Education, Linkou Chang Gung Memorial Hospital, Taoyuan City 33305, Taiwan.
Int J Mol Sci. 2024 Sep 29;25(19):10518. doi: 10.3390/ijms251910518.
(bitter melon), a traditional medicinal plant, has been demonstrated to have potential in managing diabetes, gastrointestinal problems, and infections. Among its bioactive compounds, momordicine I, a cucurbitane-type triterpenoid, has attracted attention due to its substantial biological activities. Preclinical studies have indicated that momordicine I possesses antihypertensive, anti-inflammatory, antihypertrophic, antifibrotic, and antioxidative properties, indicating its potential as a therapeutic agent for cardiovascular diseases. Its mechanisms of action include modulating insulin signaling, inhibiting inflammatory pathways, and inducing apoptosis in cancer cells. The proposed mechanistic pathways through which momordicine I exerts its cardiovascular benefits are via the modulation of nitric oxide, angiotensin-converting enzymes, phosphoinositide 3-kinase (PI3K)/ protein kinase B (Akt), oxidative stress, apoptosis and inflammatory pathways. Furthermore, the anti-inflammatory effects of momordicine I are pivotal. Momordicine I might reduce inflammation through the following mechanisms: inhibiting pro-inflammatory cytokines, reducing adhesion molecules expression, suppressing NF-κB activation, modulating the Nrf2 pathway and suppressing c-Met/STAT3 pathway. However, its therapeutic use requires the careful consideration of potential side effects, contraindications, and drug interactions. Future research should focus on elucidating the precise mechanisms of momordicine I, validating its efficacy and safety through clinical trials, and exploring its pharmacokinetics. If proven effective, momordicine I could considerably affect clinical cardiology by acting as a novel adjunct or alternative therapy for cardiovascular diseases. To date, no review article has been published on the role of bitter-melon bioactive metabolites in cardiovascular prevention and therapy. The present work constitutes a comprehensive, up-to-date review of the literature, which highlights the promising therapeutic potential of momordicine I on the cardiovascular system and discusses future research recommendations.
苦瓜，一种传统的药用植物，已被证明在治疗糖尿病、胃肠道问题和感染方面具有潜力。在其生物活性化合物中，苦瓜素 I，一种葫芦烷型三萜，由于其显著的生物活性而引起了关注。临床前研究表明，苦瓜素 I 具有降压、抗炎、抗肥厚、抗纤维化和抗氧化作用，表明其作为心血管疾病治疗剂的潜力。其作用机制包括调节胰岛素信号、抑制炎症途径和诱导癌细胞凋亡。苦瓜素 I 发挥心血管益处的拟议机制途径是通过调节一氧化氮、血管紧张素转换酶、磷酸肌醇 3-激酶（PI3K）/蛋白激酶 B（Akt）、氧化应激、细胞凋亡和炎症途径。此外，苦瓜素 I 的抗炎作用至关重要。苦瓜素 I 可能通过以下机制减轻炎症：抑制促炎细胞因子、降低粘附分子表达、抑制 NF-κB 激活、调节 Nrf2 途径和抑制 c-Met/STAT3 途径。然而，其治疗用途需要仔细考虑潜在的副作用、禁忌症和药物相互作用。未来的研究应侧重于阐明苦瓜素 I 的精确机制，通过临床试验验证其疗效和安全性，并探索其药代动力学。如果被证明有效，苦瓜素 I 可能会通过作为心血管疾病的新型辅助或替代治疗方法，对临床心脏病学产生重大影响。迄今为止，尚无关于苦瓜生物活性代谢物在心血管预防和治疗中的作用的综述文章发表。本工作是对文献的全面、最新综述，强调了苦瓜素 I 对心血管系统的有前途的治疗潜力，并讨论了未来的研究建议。
