The structure-activity relationship review of the main bioactive constituents of Morus genus plants

Abstract

Morus genus plants are mainly distributed in the temperate to tropical areas over the world and include 17 species and two subspecies. Due to their excellent pharmacological activity, security in food additives and high value in the national economy, Morus genus plants have drawn more and more attention in recent years. In the light of the references published over the last few decades, flavonoids, benzofurans, stilbenes, and Diels-Alder adducts have been reported to be the main bioactive constituents of Morus genus plants. This review summarizes the compounds with excellent bioactivities isolated from Morus genus plants as well as their structure-activity relationships (SARs), which might be useful for the further research and development of Morus genus plants. The aromatic heterocycles with excellent bioactivities isolated from Morus genus plants as well as their structure-activity relationships (SARs) were summarized.

Keywords: Bioactive constituents; Morus genus plants; Structure–activity relationships.

Fig. 1

Characteristic structure of compounds from Morus genus plants and structural moieties

Fig. 2

Structures of compounds 1–31 (the structure of A₁–A₁₀ see Fig. 1) for SARs study of α-glucosidase inhibitory activity (the unit of IC₅₀: μM)

Fig. 3

Structures of compounds 19, 20, and 32–44 (the structure of A₁–A₃ see Fig. 1) for SARs study of lipase inhibitory activity. Relative PL inhibition (%) was calculated as 100—(activity of sample with substrate—negative control of sample without substrate)/(activity of without sample and with substrate—negative control of without sample and substrate) × 100%

Fig. 4

Structures of compounds 8, 15, 18, and 45–49 (for the structure of A₁, A₁₁, and A₁₂ see Fig. 1) for SARs study of tyrosinase inhibitory activity (the unit of IC₅₀: μM)

Fig. 5

Structures of compounds 8, 15, 20, 34, 46, and 50–55 (for the structure of A₁, A₂, and A₁₂ see Fig. 1) for SARs study of β-secretase and acetylcholinesterase inhibitory activity (the unit of EC₅₀ and IC₅₀: μM)

Fig. 6

Structures of compounds 8, 15, 37, 39, 56–62 (for the structure of A₁ and A₂ see Fig. 1) for SARs study of cytotoxicity