Li Ji, Larregieu Caroline A, Benet Leslie Z
Department of Clinical Pharmacy, School of Basic Medicine and Clinical Pharmacy, China Pharmaceutical University, Nanjing 211198, China.
Department of Bioengineering & Therapeutic Science, University of California, San Francisco, CA 94143-0912, USA.
Chin J Nat Med. 2016 Dec;14(12):888-897. doi: 10.1016/S1875-5364(17)30013-4.
Natural products (NPs) are compounds that are derived from natural sources such as plants, animals, and micro-organisms. Therapeutics has benefited from numerous drug classes derived from natural product sources. The Biopharmaceutics Drug Disposition Classification System (BDDCS) was proposed to serve as a basis for predicting the importance of transporters and enzymes in determining drug bioavailability and disposition. It categorizes drugs into one of four biopharmaceutical classes according to their water solubility and extent of metabolism. The present paper reviews 109 drugs from natural product sources: 29% belong to class 1 (high solubility, extensive metabolism), 22% to class 2 (low solubility, extensive metabolism), 40% to class 3 (high solubility, poor metabolism), and 9% to class 4 (low solubility, poor metabolism). Herein we evaluated the characteristics of NPs in terms of BDDCS class for all 109 drugs as wells as for subsets of NPs drugs derived from plant sources as antibiotics. In the 109 NPs drugs, we compiled 32 drugs from plants, 50% (16) of total in class 1, 22% (7) in class 2 and 28% (9) in class 3, none found in class 4; Meantime, the antibiotics were found 5 (16%) in class 2, 22 (71%) in class 3, and 4 (13%) in class 4; no drug was found in class 1. Based on this classification, we anticipate BDDCS to serve as a useful adjunct in evaluating the potential characteristics of new natural products.
天然产物（NPs）是源自植物、动物和微生物等天然来源的化合物。治疗学已从众多源自天然产物的药物类别中受益。生物药剂学药物处置分类系统（BDDCS）被提出作为预测转运体和酶在决定药物生物利用度和处置方面重要性的基础。它根据药物的水溶性和代谢程度将药物分为四个生物药剂学类别之一。本文综述了109种源自天然产物的药物：29%属于1类（高溶解性，广泛代谢），22%属于2类（低溶解性，广泛代谢），40%属于3类（高溶解性，低代谢），9%属于4类（低溶解性，低代谢）。在此，我们根据BDDCS类别评估了所有109种药物以及源自植物来源作为抗生素的天然产物药物子集的特性。在这109种天然产物药物中，我们整理了32种植物来源的药物，1类占总数的50%（16种），2类占22%（7种），3类占28%（9种），4类未发现；同时，抗生素在2类中发现5种（16%），3类中发现22种（71%），4类中发现4种（13%）；1类未发现药物。基于这种分类，我们预计BDDCS将作为评估新天然产物潜在特性的有用辅助工具。
