Pharmacologic Activities¬ of 3’-Hydroxypterostilbene: Cytotoxic, Anti-Oxidant, Anti-Adipogenic, Anti-Inflammatory, Histone Deacetylase and Sirtuin 1 Inhibitory Activity

Abstract

-Purpose: Delineate the selected pharmacodynamics of a naturally occurring stilbene 3'-Hydroxypterostilbene. Objective: Characterize for the first time the pharmacodynamics bioactivity in several in-vitro assays with relevant roles in heart disease, inflammation, cancer, and diabetes etiology and pathophysiology. Methods: 3'-Hydroxypterostilbene was studied in in-vitro assays to identify possible bioactivity. Results: 3'-Hydroxypterostilbene demonstrated anti-oxidant, anti-inflammatory, cytotoxic, antiadipogenic, histone deacetylase, and sirtuin-1 inhibitory activity. Conclusions: The importance of understanding individual stilbene pharmacologic activities were delineated. Small changes in chemical structure of stilbene compounds result in significant pharmacodynamic differences.

Evaluation of 90 day repeated dose oral toxicity and reproductive/developmental toxicity of 3'-hydroxypterostilbene in experimental animals

“…Collectively, the increased anti-oxidant, anti-adipogenic activity, cell selectivity and COX-2 specificity of 3'-HPT was found in support of its activity in preventing cardiovascular and pulmonary diseases. Coupled with HDAC and SIRT1 inhibitory activity, 3'-HPT has been found to demonstrate protective effects from neurodegenerative diseases and select cancers [14]. …”

Biological actions and molecular effects of resveratrol, pterostilbene, and 3′-hydroxypterostilbene

“…3′-Hydroxypterostilbene ( trans -3,5-dimethoxy-3′,4′-dihydroxystilbene), one of metabolites of pterostilbene [ 30 ], can also be isolated from whole plant of the herb Sphaerophysa salsula , a shrub widely distributed in central Asia and northwest China [ 31 ]. A recent study indicated that 3′-hydroxypterostilbene possesses anti-adipogenic, -inflammatory, -oxidant, and Sirt-1 inhibitory activities [ 79 ]. However, there is a paucity of published studies involving biological activities of 3′-hydroxypterostilbene ( Table 3 ).…”

“…It was suggested that methoxylation on hydroxyl groups of pterostilbene or TMS could hinder their metabolism and appeared to have better pharmacokinetic characteristics than their natural occurring analog, resveratrol [ 83 ]. Moreover, Chiou et al [ 79 ] demonstrated that pterostilbene was more potent than resveratrol in preventing colon tumorigenesis via activation of the Nrf2-mediated antioxidant signaling pathway. Likewise, other research group indicated that pterostilbene was more effective than resveratrol as an anti-inflammatory agent for inhibition of colon carcinogenesis in HT-29 human adenocarcinoma cell line [ 19 ].…”

3′-Hydroxypterostilbene Suppresses Colitis-Associated Tumorigenesis by Inhibition of IL-6/STAT3 Signaling in Mice

“…Resveratrol (3,4′,5- trans -trihydroxylstilbene) and pterostilbene (3,5- trans -dimethoxy-4-hydroxystilbene) are two well-known stilbenes which are extensively studied because of their biological properties and potential in therapeutic and preventive application. , Pterostilbene is the dimethyl ether analogue of resveratrol and appears to have greater bioavailability than resveratrol because of its lipophilic nature with two methoxy groups. − A novel natural pterostilbene analogue, 3′-hydroxypterostilbene ( trans -3,5-dimethoxy-3′,4′-hydroxystilbene), has been isolated from Chinese folk medicine in Sphaerophysa salsula, Pterocarpus marsupium, and honey bee propolis (Figure ). An in vitro study has documented the pharmacologic activities of 3′-hydroxypterostilbene as having antioxidant, anti-inflammatory, cytotoxic, and antiadipogenic effects . 3′-Hydroxypterostilbene is also reported to be more active than pterostilbene in inducing apoptosis in sensitive and resistant leukemia cells .…”