College of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou, Fujian, China.
Department of Chinese Medicine, M Kandiah Faculty of Medicine & Health Sciences, Universiti Tunku Abdul Rahman, Kajang, Selangor, Malaysia.
Hypertens Res. 2024 Nov;47(11):3193-3199. doi: 10.1038/s41440-024-01907-0. Epub 2024 Sep 19.
Modern medicines often follow a "single-compound, single-target" paradigm, which may not be effective against complex diseases with multifactorial causes. Medicinal plants, such as Orthosiphon stamineus-widely used in Southeast Asia for its significant vasodilatory and antihypertensive properties-offer an alternative. These effects are largely attributed to the synergistic actions of sinensetin, eupatorin, and 3'-hydroxy-5,6,7,4'- tetramethoxyflavone (TMF). The present study was designed to explore the interactions among these compounds and their collective impact on vasodilation. The current investigation utilized in vitro aortic ring assays and an orthogonal stimulus-response compatibility approach to unveil the synergistic interactions of sinensetin, eupatorin, and TMF in specific combination ratios within compatibility groups. The current results showed that G2, G7, G27, and G28 achieved vasodilatory efficacies exceeding 100%, with recorded efficacies of 190%, 148%, 117.6%, and 116.25%, respectively. Conversely, formulation F1 exhibited only additive effects with an efficacy of 88.02%. The dose-response study revealed G28 exhibited the strongest concentration-dependent vasodilatory responses, with a maximum response (R) of 119.05 ± 3.29% and an EC of 6.78 ± 0.70 µg/mL. Conversely, G2, despite showing the highest efficacy in the orthogonal stimulus-response compatibility study, demonstrated a lower vasodilatory effect, with R R and EC recorded at 85.78 ± 12.67% and 15.32 ± 3.07 µg/mL, respectively. These findings highlight the complexities of compound interactions in plants and underscore the potential of botanical medicines as comprehensive healthcare solutions for multifactorial diseases.
现代药物通常遵循“单一化合物，单一靶点”的范式，对于多因素病因导致的复杂疾病可能效果不佳。药用植物，如在东南亚广泛用于其显著的血管扩张和降压特性的越南参，提供了一种替代方法。这些作用主要归因于橙皮素、泽兰黄素和 3'-羟基-5,6,7,4'-四甲氧基黄酮（TMF）的协同作用。本研究旨在探索这些化合物之间的相互作用及其对血管舒张的综合影响。本研究采用体外主动脉环测定和正交刺激-反应相容性方法，揭示了橙皮素、泽兰黄素和 TMF 在特定组合比例下在相容性组内的协同相互作用。目前的结果表明，G2、G7、G27 和 G28 的血管舒张效力超过 100%，记录的效力分别为 190%、148%、117.6%和 116.25%。相反，配方 F1 仅表现出相加作用，效力为 88.02%。剂量反应研究表明，G28 表现出最强的浓度依赖性血管舒张反应，最大反应（R）为 119.05 ± 3.29%，EC 为 6.78 ± 0.70 µg/mL。相反，尽管 G2 在正交刺激-反应相容性研究中表现出最高的效力，但血管舒张作用较低，记录的 R 和 EC 分别为 85.78 ± 12.67%和 15.32 ± 3.07 µg/mL。这些发现强调了植物中化合物相互作用的复杂性，并突出了植物药作为多因素疾病综合医疗解决方案的潜力。
