Pharmacology Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
National Centre for Radiation Research and Technology, Atomic Energy Authority, Cairo, Egypt.
Phytomedicine. 2020 Jun;71:153233. doi: 10.1016/j.phymed.2020.153233. Epub 2020 May 16.
Xanthohumol is known to exert anti-inflammatory properties but has poor oral bioavailability. Using advanced micellization technology, it has been possible to markedly enhance its bioavailability.
In the present study, we compared the chronic anti-inflammatory activities of native and micellar xanthohumol in the rat adjuvant arthritis model, using diclofenac as a reference drug.
Adjuvant arthritis was induced by injecting Freund's complete adjuvant into the right hind paw of rats and monitoring paw volume over 3 weeks. The drugs were given daily for 3 weeks, starting from the day of adjuvant inoculation. Serum was collected at the end of the experiment to measure inflammatory and oxidative stress parameters. Statistical comparisons between different groups were carried out by one-way analysis of variance followed by Tukey-Kramer multiple comparison test.
Micellar solubilized xanthohumol showed a better anti-inflammatory activity than its native form. The reduction in paw volume was reflected in corresponding changes in relevant mediators of inflammation like tumor necrosis factor-α, interleukin-6 and C-reactive protein, myloperoxidase and lipid peroxidation markers.
The findings confirm that micellar solubilization of xanthohumol enhances its anti-inflammatory activity, probably as a result of improving its bioavailabilty. The solubilized xanthohumol may prove to be a promising adjuvant tool for anti-inflammatory treatment and a potential anti-inflammatory alternative to synthetic drugs.
已知黄腐酚具有抗炎特性，但口服生物利用度较差。通过先进的胶束化技术，可以显著提高其生物利用度。
本研究比较了天然黄腐酚和胶束化黄腐酚在大鼠佐剂性关节炎模型中的慢性抗炎活性，并以双氯芬酸作为参考药物。
通过向大鼠右后爪注射完全弗氏佐剂诱导佐剂性关节炎，并在 3 周内监测爪体积。从佐剂接种之日起，每日给予药物 3 周。实验结束时收集血清，测量炎症和氧化应激参数。通过单因素方差分析，然后进行 Tukey-Kramer 多重比较检验，对不同组之间的统计比较。
胶束增溶的黄腐酚比其天然形式具有更好的抗炎活性。爪体积的减少反映了炎症相关介质如肿瘤坏死因子-α、白细胞介素-6 和 C 反应蛋白、髓过氧化物酶和脂质过氧化标志物的相应变化。
这些发现证实了胶束增溶黄腐酚增强了其抗炎活性，可能是由于提高了其生物利用度。增溶的黄腐酚可能成为抗炎治疗的有前途的辅助工具，并且可能成为合成药物的潜在抗炎替代品。
