UPM-MAKNA Laboratory of Cancer Research, Institute of Bioscience, Universiti Putra Malaysia, UPM Serdang, 43400, Serdang, Selangor, Malaysia.
Faculty of Veterinary Medicine, Universiti Putra Malaysia, UPM Serdang, Serdang, Malaysia.
Inflammopharmacology. 2018 Aug;26(4):939-949. doi: 10.1007/s10787-017-0432-2. Epub 2018 Jan 29.
The effect of Orthosiphon stamineus aqueous (OSA) extract against osteoarthritis (OA) was investigated in explant cartilage culture and in postmenopausal OA rat model. Female rats were bilaterally ovariectomized (OVX). Osteoarthritis was induced after surgical recovery, by intra-articular injection of monosodium iodoacetate (MIA) into the right knee. Rats were grouped (n = 8) into: healthy sham control; non-treated OA; OA + diclofenac (positive control 5 mg/kg); and two doses OSA (150-300 mg/kg). After 4 weeks' treatment, rats were evaluated for OA-related parameters and biomarkers. The OSA reduced proteoglycan and ROS release from the cartilage explants under inflammatory (IL-1b) conditions. In the OA-induced rats' cartilages, the OSA downregulated the mRNA expressions for IL-1β, IL-6, IL-10, TNF-α, NF-κβ, NOS2, PTGS2, PTGER2, ACAN, COL2A1, MMP1, MMP13, ADAMTS4, ADAMTS5 and TIMP1, mostly dose-dependently. The OSA reduced the OA rats' serum levels for PGE, CTX-II, TNF-α, MMP1, MMP13, PIINP, OPG, RANKL, OC and BALP, but not dose-dependently. The OSA contained polyphenols and flavonoids (tetramethoxyflavone). The OSA alleviated articular cartilage degradation, inflammation, collagenase/aggrecanase activities, to improve joint and subchondral bone structure. O. stamineus mitigated osteoarthritis by downregulating inflammation, peptidases and aggrecanases, at a dose equivalent to about 30 mg/kg for humans.
金钱草水提物（OSA）对骨关节炎（OA）的作用在离体软骨培养和绝经后 OA 大鼠模型中进行了研究。雌性大鼠双侧卵巢切除术（OVX）。手术后恢复后，通过向右膝关节内注射单碘乙酸钠（MIA）诱导骨关节炎。将大鼠分为（n=8）：健康假手术对照；未治疗的 OA；OA+双氯芬酸（阳性对照 5mg/kg）；和两个剂量的 OSA（150-300mg/kg）。治疗 4 周后，评估大鼠与 OA 相关的参数和生物标志物。OSA 减少了软骨外植体在炎症（IL-1b）条件下释放的蛋白聚糖和 ROS。在诱导 OA 的大鼠软骨中，OSA 下调了 IL-1β、IL-6、IL-10、TNF-α、NF-κβ、NOS2、PTGS2、PTGER2、ACAN、COL2A1、MMP1、MMP13、ADAMTS4、ADAMTS5 和 TIMP1 的 mRNA 表达，大多数呈剂量依赖性。OSA 降低了 OA 大鼠血清中 PGE、CTX-II、TNF-α、MMP1、MMP13、PIINP、OPG、RANKL、OC 和 BALP 的水平，但不是剂量依赖性的。OSA 含有多酚和类黄酮（四甲氧基黄酮）。OSA 通过下调炎症、胶原酶/聚集酶活性，缓解关节软骨降解，改善关节和软骨下骨结构，从而减轻骨关节炎。金钱草以相当于人类约 30mg/kg 的剂量减轻骨关节炎，通过下调炎症、肽酶和聚集酶。
