Ryan M E, Ramamurthy S, Golub L M
State University of New York at Stony Brook, New York, USA.
Curr Opin Periodontol. 1996;3:85-96.
Matrix metalloproteinases (MMPs), produced by both infiltrating and resident cells of the periodontium, play a role in physiologic (e.g., tooth eruption) and pathologic (e.g., periodontitis) events. The evidence for the role of MMPs in periodontal destruction has accumulated over three and a half decades, and it is now recognized that an imbalance between activated MMPs and their endogenous inhibitors leads to pathologic breakdown of the extracellular matrix during periodontitis. This understanding has stimulated the search for a number of synthetic inhibitors that could be used as potential therapeutic agents. Tetracycline analogues, as proteinase inhibitors, are currently closer to being used clinically than any other agents in periodontal therapy. Other MMP inhibitors, such as Batimastat (British Bio-technology, Oxford, UK), are currently being tested clinically for inhibition of cancer metastasis and other diseases. Multiple mechanisms of MMP inhibition by tetracycline analogues have been proposed. The nonantimicrobial chemically modified tetracyclines are potent inhibitors of MMPs, preventing collagen breakdown and alveolar bone loss in animal models of periodontitis. In addition, nonantimicrobial low doses of the commercially available semisynthetic tetracycline doxycycline, have been used in human clinical trails to reduce MMP activity in the gingival crevicular fluid and gingival tissues, with a resultant reduction in pocket depth and attachment loss. Of particular interest, periodontal research on the nonantimicrobial properties of tetracycline has generated new therapeutic approaches to a variety of medical disorders characterized by excess MMP activity.
基质金属蛋白酶(MMPs)由牙周组织中的浸润细胞和驻留细胞产生,在生理过程(如牙齿萌出)和病理过程(如牙周炎)中发挥作用。关于MMPs在牙周组织破坏中作用的证据在三十五年多的时间里不断积累,现在人们认识到,在牙周炎期间,活化的MMPs与其内源性抑制剂之间的失衡会导致细胞外基质的病理性降解。这种认识激发了人们寻找多种可作为潜在治疗药物的合成抑制剂。四环素类似物作为蛋白酶抑制剂,目前在牙周治疗中比其他任何药物更接近临床应用。其他MMP抑制剂,如batimastat(英国牛津的British Bio-technology公司生产),目前正在进行临床试验,用于抑制癌症转移和其他疾病。人们提出了四环素类似物抑制MMPs的多种机制。非抗菌化学修饰四环素是MMPs的有效抑制剂,可防止牙周炎动物模型中的胶原降解和牙槽骨丧失。此外,市售的半合成四环素强力霉素的非抗菌低剂量已用于人体临床试验,以降低龈沟液和牙龈组织中的MMP活性,从而使牙周袋深度和附着丧失减少。特别值得关注的是,关于四环素非抗菌特性的牙周研究为多种以MMP活性过高为特征的医学疾病带来了新的治疗方法。