Ptp1b Inhibitors From Isodon Ternifolius Collected in Vietnam

Abstract

From the whole plant of Isodon ternifolius collected in Vietnam, four triterpens including ursaldehyde (1), ursolic acid (2), b-sitosterol (3) and b-sitosteryl ferulate (4) were purified. Their chemical structures were determined by interpretation of NMR and MS data and comparison with the literatures. Compounds 1-4 were evaluated for their inhibitory activity against PTP1B enzyme activity using in vitro assay. Compounds 1 and 2 displayed potential activities with IC50 values of 16.92 ± 0.12 and 3.42 ± 0.45 μM, respectively. This is the first time that compounds 1 and 4 have been isolated from the Isodon genus and I. ternifolius has been evaluated for the PTP1B inhibitory activity.

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“…The plant, shown in Fig. 1 along with its systematic position, is a shrub mainly found in tropical and subtropical countries 9 . Preparation of the Leaf Extract: 24 Kg of the leaves of the plant Isodon ternifolius (D.Don) Kudo at the flowering stage was collected and thoroughly washed with tap water and then shade dried at room temperature for two weeks with intermittent shuffling 10 .…”

“…Eleven compounds (6,7,17,23,30,33,35,53,73,75, and 81) were highly distributed with log Vd ss values ranging between 0.462 and 0.845. And the other seventeen phytocompounds (3,8,9,16,18,21, 39, 44, 52, 56, 60, 61, 63, 64, 66, 69, and 71) were predicted to be poorly distributed with log VD ss values ranging from-0.21 to-1.775. On the other hand, the remaining phytocompounds were found to be moderately distributed.…”

Methanol extract of Isodon ternifolius (D. Don) KUDO leaves has antimicrobial and antioxidant activities but no neuroprotective activity.

“…A large number of terpenoids have been isolated and identified from I. ternifolius. Some of the diterpenoids have been found to have anti-tumour (Zou et al, 2012;Zou et al, 2013;Liao et al, 2014;Zhang et al, 2020;Elshamy et al, 2023), anti-stemness (Yuan et al, 2017), protein tyrosine phosphatase 1B (PTP1B) inhibitory (Pham et al, 2020) and anti-fibrotic (Deng et al, 2023) activities. The scientific statements about the activities of this plant against microbial infections and free radical-induced oxidative damages still need to be made.…”