Protein tyrosine phosphatase 1B inhibitors from natural sources

Abstract

Since PTP1B enzyme was discovered in 1988, it has captured the research community's attention. This landmark discovery has stimulated numerous research studies on a variety of human diseases, including cancer, inflammation, and diabetes. Tremendous progress has been made in finding PTP1B inhibitors and exploring PTP1B regulatory mechanisms. This review investigates for the natural PTP1B inhibitors, and focuses on the common characteristics of the discovered structures and structure-activity relationships. To facilitate understanding, all the natural compounds are here divided into five different classes (fatty acids, phenolics, terpenoids, steroids, and alkaloids), according to their skeletons. These PTP1B inhibitors of scaffold structures could serve as a theoretical basis for new concept drug discovery and design.

Progress of Bromophenols in Marine Algae from 2011 to 2020: Structure, Bioactivities, and Applications

“…PTP1B is a negative regulator of insulin signaling via dephosphorylation of the insulin receptor tyrosine residues and downstream substrates to reduce the role of insulin [ 62 ]. It is well accepted that this enzyme is a promising target for hypoglycemic agent discovery, and a recent review deals with PTP1B inhibitors from natural sources [ 63 ]. In the past decade, several BPs with hypoglycemic activity targeting PTB1B have been discovered.…”

Glucose Uptake Stimulatory and PTP1B Inhibitory Activities of Pimarane Diterpenes from Orthosiphon stamineus Benth

“…In addition, a methine proton at δ H 5.88 (1H, m, H-11) exhibited long-range correlations with carbon signals at δ C 77.6 (C-8), 49.8 (C-10), 48.4 (C-13), and 166.3 (C-7 ), indicating the second benzoyl group located at C-11. All the above data revealed that compound 1 was a pimarane-type diterpene [9,[29][30][31] and was identical with siphonol A, except only for a lack of an acetyl moiety at C-7. The downfield chemical shift of methine proton H-7 (δ H 5.51 ppm) in siphonol A [13] is quite different from the upfield chemical shift of methine proton H-7 (δ H 4.32 ppm) in 1.…”

“…There are many PTP1B inhibitors from medicinal plants. Up to now, around 56 families of genera from the natural source were found to inhibit PTP1B activity [9]. Among them, some plants and their secondary metabolites are derived from desert and steppe in the Middle East, such as Artemisia judaica, Centaurium erythraea, Achillea santolina, Capparis spinosa, Moringa peregrina, Retama raetam, Terminalia chebula, and Ziziphus spina-christi [10].…”

Pimarane Diterpenoids from the Seeds of Caesalpinia minax as PTP1B Inhibitors and Insulin Sensitizers

“…Hence, it is urgent to identify potent and selective small-molecular PTP1B inhibitors. Natural products, including fatty acids, phenolics, terpenoids, steroids and alkaloids, provide a great amount of PTP1B inhibitors with structural diversity [ 5 , 6 ].…”