Two filamentous fungi, Cunninghamella bainieri ATCC 9244 and Aspergillus niger BCRC 32720, were used to investigate the biotransformation of isosteviol lactone (4alpha-carboxy-13alpha-hydroxy-13,16- seco-ent-19-norbeyeran-16-oic acid 13,16-lactone) ( 2), which was derived by reacting isosteviol ( ent-16-oxobeyeran-19-oic acid) ( 1) with m-chloroperbenzoic acid. Incubation of 2 with C. bainieri ...

Context The therapeutic action of opioid analgesics is compromised by peripheral adverse effects, among which constipation is the most disabling, as laxatives often fail to provide satisfactory relief. To address this problem, opioid receptor antagonists with limited systemic bioavailability (retarded naloxone) or a peripherally restricted site of action (alvimopan, methylnaltrexone) have been ...

Naloxegol is approved for the treatment of opioid-induced constipation (OIC) in adults with chronic noncancer pain. Population exposure-response models were developed using data from a phase II study comprising 185 adults with OIC. The weekly probability of response defined as having ≥3/week spontaneous bowel movements (SBMs) and ≥1 SBM/week increase over baseline was characterized by a longitu...

Two additional novel minor diterpene glycosides were isolated from the commercial extract of the leaves of Stevia rebaudiana Bertoni. The structures of the new compounds were identified as 13-{β-D-glucopyranosyl-(1 → 2)-O-[β-D-glucopyranosyl-(1 → 3)-β-D-glucopyranosyl-oxy} ent-kaur-16-en-19-oic acid {β-D-xylopyranosyl-(1 → 2)-O-[β-D-glucopyranosyl-(1 → 3)]-O-β-D-glucupyranosyl-ester} (1), and 1...

Three new compounds, cadalen-15-oic acid (1), 3,7-dihydroxy-3(4H)-isocadalen-4-one (2), and dicadalenol (3), were isolated from the aerial parts of Heterotheca inuloides (Mexican arnica), together with the known compounds 7-hydroxycadalene (4), 7-hydroxy-4alphaH-3,4-dihydrocadalene (5), 1alpha-hydroxy-1(4H)-isocadalen-4-one (6), 1alpha-hydroxy-4alphaH-1,2,3,4-tetrahydrocadalen-15-oic acid (7), ...

A bioassay-guided fractionation and chemical investigation of the trunk of Berberis koreana resulted in the isolation and characterization of two new triterpenoids, 23-trans-p-coumaroyloxy-2alpha,3alpha-dihydroxyolean-12-en-28-oic acid (1), and 23-cis-p-coumaroyloxy-2alpha,3alpha-dihydroxyolean-12-en-28-oic acid (2), along with seven known triterpenoids (3-9). The structures of the new compound...

Oleanolic acid (OA, 3β-hydroxyolean-12-en-28-oic acid) is a ubiquitous pentacyclic multifunctional triterpenoid, widely found in several dietary and medicinal plants. Natural and synthetic OA derivatives can modulate multiple signaling pathways including nuclear factor-κB, AKT, signal transducer and activator of transcription 3, mammalian target of rapamycin, caspases, intercellular adhesion mo...

To study the possible role of bile acids in carcinogenesis of the large bowel faecal bile acid profiles were analysed in detail in 14 patients with large bowel cancer and compared with 14 matched healthy subjects. The total faecal bile acid excretion was lower in the patients (297.3 +/- 402.8 mumol/day) than in the healthy subjects (470.6 +/- 231.1 mumol/day) (p less than 0.01), although the di...

Four new mulinane-type diterpenoids besides the known compounds mulin-11,13-dien-20-oic acid, 13α-hydroxyazorellane, 13β-hydroxyazorellane, mulinolic acid, azorellanol, and mulin-11,13-dien-18-acetoxy-16,20-dioic acid were isolated from the Chilean plant Azorella trifurcata. One of the new metabolites isolated, 7α-acetoxy-9-epi-13β-hydroxymulinane, possesses a new trans-syn-trans arrangement in...