Llavaneras A, Ramamurthy N S, Heikkilä P, Teronen O, Salo T, Rifkin B R, Ryan M E, Golub L M, Sorsa T
Central University of Venezuela School of Dentistry and School of Pharmacy, Caracas.
J Periodontol. 2001 Aug;72(8):1069-77. doi: 10.1902/jop.2001.72.8.1069.
Chemically modified non-antimicrobial tetracyclines (CMTs) have been shown to inhibit pathologically elevated collagenase (and other matrix metalloproteinase, MMP) activity and bone resorption in vivo and in vitro.
In the current study, suboptimal doses of CMT-8 (a non-antimicrobial chemically modified doxycycline) and a bisphosphonate (clodronate, an anti-bone resorption compound) were administered daily, either as a single agent or as a combination therapy, to rats with experimental periodontitis induced by repeated injection of bacterial endotoxin (LPS) into the gingiva. At the end of the 1-week protocol, the gingival tissues were dissected, extracted, and the extracts analyzed for MMPs (collagenases and gelatinases) and for elastase, and the defleshed jaws were morphometrically analyzed for alveolar bone loss.
LPS injection significantly (P<0.001) increased alveolar bone loss and increased collagenase (MMP-8), gelatinase (MMP-9), and elastase activities. Treatment of the LPS-injected rats with suboptimal CMT-8 alone or suboptimal clodronate alone produced slight reductions in the tissue-destructive proteinases and no significant reductions in alveolar bone loss. However, a combination of suboptimal CMT-8 and clodronate "normalized" the pathologically elevated levels of MMPs, elastase, and alveolar bone loss, indicating synergistic inhibition of tissue breakdown in this animal model of periodontitis.
Combination of a CMT and a bisphosphonate may be a useful treatment to optimally suppress periodontal destruction and tooth loss and in other tissue-destructive inflammatory diseases such as arthritis.
化学修饰的非抗菌四环素(CMTs)已被证明在体内和体外均可抑制病理性升高的胶原酶(以及其他基质金属蛋白酶,MMP)活性和骨吸收。
在本研究中,将次优剂量的CMT-8(一种化学修饰的非抗菌强力霉素)和一种双膦酸盐(氯膦酸盐,一种抗骨吸收化合物)每日单独或联合给药,用于通过向牙龈反复注射细菌内毒素(LPS)诱导实验性牙周炎的大鼠。在1周方案结束时,解剖、提取牙龈组织,并对提取物进行MMPs(胶原酶和明胶酶)和弹性蛋白酶分析,对去除软组织的颌骨进行形态计量分析以评估牙槽骨丧失情况。
注射LPS显著(P<0.001)增加了牙槽骨丧失,并增加了胶原酶(MMP-8)、明胶酶(MMP-9)和弹性蛋白酶的活性。用次优剂量的CMT-8单独或次优剂量的氯膦酸盐单独治疗注射LPS的大鼠,可使组织破坏性蛋白酶略有降低,但牙槽骨丧失无显著减少。然而,次优剂量的CMT-8和氯膦酸盐联合使用可使MMPs、弹性蛋白酶和牙槽骨丧失的病理性升高水平“正常化”,表明在该牙周炎动物模型中对组织破坏具有协同抑制作用。
CMT与双膦酸盐联合使用可能是一种有效的治疗方法,可最佳地抑制牙周破坏和牙齿丧失,以及用于治疗其他组织破坏性炎症性疾病,如关节炎。