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基于微乳液的药物递送系统识别了胡的类化合物作为抗肥胖化合物

Tian-Kai Meng¹, Ruo-Lei Han¹, Peng Ma¹

¹Yangzhi Rehabilitation Hospital, Sunshine Rehabilitation Center, School of Life Sciences and Technology, Tongji University, Shanghai, 200092, China.

Acta pharmacologica Sinica

|March 21, 2025

概括

一种新的微乳液输送系统增强了疏水化合物的溶性,有助于治疗肥胖症. 来自黑胡的皮佩林通过增加细胞中的信号来降低小鼠的脂肪水平和体重.

科学领域:

药理学和药物输送药理学和药物输送
代谢疾病和肥胖症研究研究
自然产品化学化学

背景情况:

肥胖是导致心脏病和糖尿病等代谢疾病的主要危险因素.
合成抗肥胖药物有不良影响,引发了对天然产品替代品的兴趣.
低水溶性和低生物可用性限制了许多疏水性天然化合物的有效性.

研究的目的:

开发一种基于微乳液的药物输送系统,以提高疏水性抗肥胖化合物的可溶性和生物可用性.
用Drosophila的高脂肪饮食模型识别具有抗肥胖作用的天然化合物.
阐明已识别的化合物的作用机制,并评估它们的 in vivo 疗效.

主要方法:

开发一个微乳液系统 (克雷莫福EL,乙醇,乙烯酸盐) 用于液体高脂肪饮食 (LHFD) 在Drosophila.
在LHFD模型中对161种传统中医药化合物的抗肥胖作用进行查.
研究了皮佩林对三糖醇水平,肠细胞中的细胞质Ca2+,TRP通道激活和Magro表达的影响.
评估了微乳液封装化合物的输送到小鼠的远端组织,并评估了体重减轻.

主要成果:

微乳液系统有效地提高了Drosophila的疏水化合物溶解度,而不会影响食物摄入或生存.
黑胡中的类化合物皮佩林 (PIP) 显著降低了中的三糖醇水平.
皮佩林通过激活TRP通道在肠细胞中增加了细胞溶液Ca2+ ,通过CREB激活抑制了Magro表达.
微乳液的输送成功地将疏水化合物运送到小鼠肝脏和大脑血管系统,而皮佩林减少了体重.

结论:

一个基于微乳液的U-GLAD平台促进了用于治疗肥胖症的疏水化合物的输送.
皮佩林通过调节细胞内信号传递和脂酶表达,显示出显著的抗肥胖作用.
这项研究为开发基于天然产品的治疗方法提供了一个有希望的策略,用于治疗肥胖和相关代谢障碍.

关键词:

这种植物是Drosophila.饮食引起的肥胖症饮食引起的肥胖症药物输送是药物输送的过程.乳液乳液是一种乳液.胡的类化合物胡的类化合物

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