Obesity contributes to the genesis of many metabolic disorders including dyslipidemia, coronary heart disease (CHD), nonalcoholic fatty liver, type 2 diabetes, etc. Pancreatic lipase plays a vital role in food fat digestion and absorption. Therefore, to control obesity, inhibition of pancreatic lipase is the active therapy. Thus, novel natural product derived labdane appended triazoles with pancreatic lipase inhibition potential were designed and synthesized. Among these hybrids, 6b and 6f exhibited excellent inhibitory activity (IC₅₀ 0.75 ± 0.02 μM and 0.77 ± 0.01 μM), slightly better than that of the positive control Orlistat (IC₅₀ 0.8 ± 0.03 μM). Compounds 6c, 6e, and 6g–j inhibited the PL comparable to that of positive control. Interestingly none of the compounds showed cytotoxicity (Hep G2) in the concentration range from 0.5 to 100 μM. Overall results reveal the potential of labdane appended triazoles as antiobesity agents.

中文翻译：

---

天然产物衍生的Labdane附加三唑类作为有效的胰腺脂肪酶抑制剂的发现

肥胖是导致许多代谢异常的原因，包括血脂异常，冠心病（CHD），非酒精性脂肪肝，2型糖尿病等。胰腺脂肪酶在食物脂肪的消化吸收中起着至关重要的作用。因此，控制肥胖是抑制胰腺脂肪酶的有效疗法。因此，设计并合成了具有胰脂肪酶抑制潜能的新的天然产物衍生的附有拉丹烷的三唑。在这些杂种中，6b和6f表现出优异的抑制活性（IC ₅₀ 0.75±0.02μM和0.77±0.01μM），略好于阳性对照Orlistat（IC ₅₀ 0.8±0.03μM）。化合物6c，6e和6g – j对PL的抑制作用与阳性对照相当。有趣的是，在0.5至100μM的浓度范围内，没有一种化合物显示出细胞毒性（Hep G2）。总体结果显示，附有拉丹的三唑类药物可作为减肥药。