Pathogens that express resistance to multiple drugs are becoming the norm, complicating treatment and increasing human morbidity. Acylsugars or resin glycosides from the morning glory family (Convolvulaceae) are amphipathic modulators of the efflux pumps responsible for the drug-resistant phenotype in prokaryotic and eukaryotic cells. These inhibitory effects could be used to overcome the acquired resistance to common anticancer or antimicrobial drugs by lowering the current effective therapeutic doses, thus decreasing toxic side-effects in refractory malignancies. Active chemosensitizers identified by in vitro screening methods have demonstrated the therapeutic potential of resin glycosides for further exploration as coadjuvants to avoid drug resistance and restore the clinical utility of chemotherapy in treating infections and cancer. To date, more than 20 resin glycosides have been documented as inhibitors or modulators of efflux pumps, mainly isolated from species of the genus Ipomoea. Resin glycosides have shown the ideal structural features associated with multidrug-resistant efflux pump substrates. An overview is given to the acylsugar diversity and their amphiphilicity properties for bioactivity as leads of efflux pump inhibitors for drug development.

对多种药物产生抗药性的病原体正在成为常态，使治疗复杂化并增加了人类发病率。牵牛花科（旋花科）的酰基糖或树脂糖苷是外排泵的两亲性调节剂，负责原核和真核细胞中的耐药表型。通过降低当前有效的治疗剂量，这些抑制作用可用于克服获得的对常见抗癌药或抗微生物药物的耐药性，从而减少难治性恶性肿瘤的毒性副作用。通过体外筛选方法鉴定出的活性化学增敏剂已显示出树脂糖苷作为共佐剂的潜在开发潜力，可以进一步避免药物耐药性并恢复化学疗法在治疗感染和癌症中的临床效用。迄今为止，番薯。树脂苷已显示出与耐多药外排泵基质相关的理想结构特征。概述了酰基糖的多样性及其两亲性特性（作为药物开发的外排泵抑制剂的先导）具有生物活性。