Rilpivirine, a recently developed drug of choice for initial treatment of HIV-1 infection, can greatly reduce HIV-related inflammation, but in turn, may be associated with adverse secondary effects, including disturbances in lipid metabolism and ultimately in adipose tissue distribution and function. In recent years, research findings on the benefits of anti-oxidant foods and supplements have been employed in counter-acting both oxidative stress as well as inflammation in order to reduce the adverse side effects of anti-retroviral therapy. One such natural flavonoid which possesses anti-inflammatory and anti-oxidative properties is quercetin. This study investigated the effect of quercetin in overcoming the side effects incurred due to rilpivirine administration. The results show substantial reduction in the accumulation of triglyceride levels in a dose- and time-dependent manner for adipose cells treated with either rilpivirine or quercetin alone and in combination, as evidenced by morphological pictures and quantitative measurement of triglycerides throughout the differentiation process. Levels of inflammatory markers such as resistin and IL-8 were increased as compared to the untreated cells. No significant changes in leptin were observed on treatment of adipose cells with rilpivirine alone and its levels were almost comparable to control. Levels of oxidative markers like superoxide dismutase, catalase, and glutathione were also decreased. Treatment with quercetin showed a decrease in the inflammatory status and an increase in the oxidative status of adipose cells, thereby exhibiting its anti-inflammatory and anti-oxidative properties. However, further assessment of lipid metabolism and adipose tissue function in patients administered with rilpivirine-based regimes is advisable considering that totally neutral effects of rilpivirine on lipid homeostasis cannot be anticipated from the current study in vitro. It is concluded that rilpivirine causes an anti-adipogenic and pro-inflammatory response pattern but only at high concentrations, whereas quercetin has been observed to decrease inflammation and restore the levels of anti-oxidant enzymes.

Rilpivirine是最近开发的用于HIV-1感染初始治疗的首选药物，可以大大减轻与HIV相关的炎症，但反过来可能与不良的次级作用相关，包括脂质代谢紊乱，最终影响脂肪组织分布和功能。近年来，关于抗氧化食品和补品的益处的研究成果已被用于抵消氧化应激和炎症，以减少抗逆转录病毒疗法的不良副作用。槲皮素是一种具有抗炎和抗氧化特性的天然黄酮。这项研究调查了槲皮素在克服因使用rilpivirine引起的副作用中的作用。结果表明，单独用利比韦林或槲皮素联合处理的脂肪细胞，甘油三酸酯水平的累积显着降低，呈剂量和时间依赖性，这在整个分化过程中得到了形态学图片和甘油三酸酯的定量测量结果。与未处理的细胞相比，炎症标记物（例如抵抗素和IL-8）的水平升高。单独使用利匹韦林治疗脂肪细胞时，瘦素未见明显变化，其水平几乎与对照相当。诸如超氧化物歧化酶，过氧化氢酶和谷胱甘肽的氧化标记物的水平也降低了。槲皮素治疗后，脂肪细胞的炎症状态降低，氧化状态增加，从而显示出其抗炎和抗氧化的特性。然而，考虑到无法从当前的体外研究中预测到rilpivirine对脂质稳态的完全中性作用，建议对接受rilpivirine方案的患者进一步评估脂质代谢和脂肪组织功能。结论是，利匹韦林引起抗脂肪形成和促炎反应，但仅在高浓度时才发生，而槲皮素可减少炎症并恢复抗氧化酶的水平。