During the past few decades, a large number of animal studies demonstrated that commonly used opioids could provide cardioprotection against ischemia-reperfusion (I/R) injury. Opioid-induced preconditioning or postconditioning mimics ischemic preconditioning (I-Pre) or ischemic postconditioning (I-Post). Both δ- and κ-opioid receptors (OPRs) play a crucial role in opioid-induced cardioprotectio...

Microbial transformation of the antimelanoma agent betulinic acid was studied. The main objective of this study was to utilize microorganisms as in vitro models to predict and prepare potential mammalian metabolites of this compound. Preparative-scale biotransformation with resting-cell suspensions of Bacillus megaterium ATCC 13368 resulted in the production of four metabolites, which were iden...

A series of 3-monohydroxylated bile acids, in unlabeled and radioactive form, of varying side chain length and configuration at C-3 has been synthesized and rigorously characterized. They include: 3 alpha- and 3 beta-hydroxy-5 beta-androstane-17 beta-carboxylic acids (C20); 3 alpha- and 3 beta-hydroxy-5 beta-pregnan-21-oic acids (C21); 3 alpha- and 3 beta-hydroxy-23,24-bisnor-5 beta-cholan-22-o...

Opioid-induced constipation (OIC) imposes a significant burden for patients taking pain medications, often resulting in decreased quality of life. Treatment of OIC with traditional medications for functional constipation can be incompletely effective, leading to nonadherence with opioid treatment and undertreated pain. An emerging class of medications that counteract the adverse effects of opio...

We screened for human renin inhibitory activity in wild vegetables and found the activity in methanol extract of Aralia cordata. Physico-chemical data on the isolated inhibitors were identical to those of (–)-kaur-16-en-19-oic acid (kaurenic acid, KA) and pimaradienoic acids (PDA, 8:2 mixture of pimara-8(14), 15-dien-19-oic acid: pimara-9(11) 15-dien-19-oic acid). KA and PDA also inhibited porc...

The biotransformation of lithocholic acid by Pseudomonas sp. strain NCIB 10590 under anaerobic conditions was studied. The major products were identified as androsta-1,4-diene-3,17-dione and 3-oxochol-4-ene-24-oic acid. The minor products included 17beta-hydroxyandrost-4-ene-3-one, 17beta-hydroxyandrosta-1,4-diene-3-one, 3-oxo-5beta-cholan-24-oic acid, 3-oxochola-1,4-diene-24-oic acid, 3-oxopre...

Opioid-induced constipation (OIC), a prevalent and distressing side effect of opioid therapy, does not reliably respond to treatment with conventional laxatives. OIC can be a treatment-limiting adverse event. Recent advances in medications with peripherally acting μ-opioid receptor antagonists, such as methylnaltrexone, naloxegol, and alvimopan, hold promise for treating OIC and thus extending ...

The biocatalyzed conversion of hyocholic acid (3α,6α,7α-trihydroxy-5β-cholan-24-oic acid) into ω-muricholic (3α,6α,7β-trihydroxy-5β-cholan-24-oic has been obtained exploiting a small library 7α- and 7β-HSDHs (hydroxysteroid dehydrogenases). process optimized performed avoiding the isolation 7-oxo intermediate using appropriate coupled enzymes for in situ cofactor regeneration. Moreover, reducti...

Our ongoing investigations on the stem bark of Uncaria macrophylla afforded a new ursolic triterpene, 3β,6β,19α-trihydroxy-urs-12-en-28-oic acid-24-carboxylic acid methyl ester (1), named uncariursanic acid, and three known ursolic triterpenes including 3β,6β,19α-trihydroxy-23-oxo-urs-12-en-28-oic acid (2), 3β,6β,19α-trihydroxy-urs-12-en-28-oic acid (3) and ursolic acid (4). Their structures we...

Bile salts of the coelacanth, Latimeria chalumnae, Smith, have been analyzed and shown to have three bile alcohols, latimerol, 5 alpha-cyprinol, and 5 alpha-cholestane-3 beta, 7 alpha,-12 alpha,25,26-pentol, two C24 bile acids, chenodeoxycholic acid and cholic acid, one C26 bile acid, probably 3 beta, 7 alpha, 12 alpha-trihydroxy-27-nor-5 alpha-cholestan-26-oic acid, and two C27 bile acids, 3 a...