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巴瓦基宁可以选择性调节PPAR γ,并维持2型糖尿病患者的骨质平衡
Jingwen Liu1, Xiaoye Li2, Hong Wang2
1Experiment Center for Science and Technology, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China.
Phytotherapy research : PTR
|June 12, 2023
概括
选择性PPAR γ调节剂巴瓦基宁 (BVC) 促进骨健康和胰岛素敏感性,没有传统TZD药物的副作用. 这种化合物为代谢障碍和骨维护提供了有前途的治疗方法.
科学领域:
- 药理学 药理学是指药理学的学科.
- 内分泌学 在内分泌学.
- 骨生物学 骨生物学 骨生物学
背景情况:
- thiazolidinediones (TZDs) 是一种用于2型糖尿病 (T2DM) 的全氧酶增殖器激活受体 (PPAR) γ激动剂.
- TZDs会导致体重增加和骨质损失等不良影响,限制了它们的临床使用.
- 需要选择性PPAR γ调节器来保持治疗效益,同时避免副作用.
研究的目的:
- 调查选择性PPAR γ调节器巴瓦基宁 (BVC) 对其对骨质稳定和代谢调节的影响.
- 评估BVC前药物 (BN) 在治疗T2DM相关并发症方面的治疗潜力.
主要方法:
- 用BVC治疗的MC3T3-E1和C3H10T1/2细胞的评估骨质分化.
- 在RANKL刺激的RAW 264.7细胞中评估骨质细胞的形成.
- 将合成的BVC前药物 (BN) 给瘦素受体缺乏和饮食诱导的肥胖小鼠.
- 在体内对体重,脂质代谢,胰岛素敏感性,骨质量和生物机械性质的评估.
主要成果:
- 在正常和高葡萄糖条件下,BVC显著增强了前骨质细胞和介质细胞干细胞的骨质分化.
- BVC抑制了骨质细胞分化.
- 在体内,BVC前药物 (BN) 阻止了体重增加,改善了脂质代谢和胰岛素敏感性.
- 在小鼠模型中,BN治疗维持了骨质和生物力学特性.
结论:
- 巴瓦基宁 (BVC) 是一种选择性的PPAR γ调节剂,可维持骨质平衡,并表现出胰岛素敏感性.
- BVC前药物 (BN) 有效地规避了与TZD相关的副作用,如骨损失和体重增加.
- BVC及其前药物代表了T2DM的潜在治疗策略,具有更好的安全性.
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