Anti-hyperuricemic and anti-inflammatory actions of vaticaffinol isolated from Dipterocarpus alatus in hyperuricemic mice.

The present study was designed to examine the anti-hyperuricemic and anti-inflammatory effects and possible mechanisms of vaticaffinol, a resveratrol tetramer isolated from ethanol extracts of Dipterocarpus alatus, in oxonate-induced hyperuricemic mice. At 1 h after 250 mg·kg-1 potassium oxonate was given, vaticaffinol at 20, 40, and 60 mg·kg-1 was intragastrically administered to hyperuricemic mice once daily for seven consecutive days. Vaticaffinol significantly decreased serum uric acid levels and improved kidney function in hyperuricemic mice. It inhibited hepatic activity of xanthine dehydrogenase (XDH) and xanthine oxidase (XOD), regulated renal mRNA and protein levels of urate transporter 1 (URAT1), glucose transporter 9 (GLUT9), organic anion transporter 1 (OAT1), organic cation transporter 1 (OCT1), OCT2, organic cation/carnitine transporter 1 (OCTN1), and OCTN2 in hyperuricemic mice. Moreover, vaticaffinol markedly down-regulated renal protein levels of NOD-like receptor 3 (NLRP3), apoptosis-associated speck-like (ASC), and Caspase-1, resulting in the reduction of interleukin (IL)-1ß, IL-18, IL-6 and tumor necrosis factor-α (TNF-α) levels in this animal model. Additionally, HPLC and LC-MS analyses clearly testified the presence of vaticaffinol in the crude extract. These results suggest that vaticaffinol may be useful for the prevention and treatment of hyperuricemia with kidney inflammation.

Two new indole alkaloids from Hunteria zeylanica.

Two new indole alkaloids, 14ß-hydroperoxy-eburnamine (1) and 18α-hydroxy-eburnamine (2), together with three known indole alkaloids, (-)-eburnamonine (3), (-)-eburnamenine (4), and eburnamine (5) were isolated from Hunteria zeylanica collected in Hainan Province of China. Their structures were determined by spectroscopic analysis. The relative configuration of 2 was deduced by NOE experiment and evidenced by the calculations for energy minimization with the molecular modeling program Chem3D Ultra 10.0.

Oligostilbenoids with acetylcholinesterase inhibitory activity from Dipterocarpus alatus.

Phytochemical investigation of the stem wood of Dipterocarpus alatus led to the isolation and characterization of four new oligostilbenoids, dipterocarpols A-D (1-4), together with two known resveratrol oligomers, hopeahainol (5) and hopeafuran (6). The structures of the new compounds were determined by comprehensive spectral analysis including 1D and 2D NMR, and high-resolution MS. The absolute configurations were determined by NOESY and CD spectra. Dipterocarpol A (1) and hopeahainol A (5) showed moderate acetylcholinesterase inhibitory activity with IC50 values of 8.28 µM and 11.28 µM, respectively. Furthermore, the discovery of compound 3 gave the first evidence that the biosynthetic origin of resveratrol aneuploids is related to the loss of a half resveratrol unit by oxidative cleavage.

Thiophene acetylenes and furanosesquiterpenes from Xanthopappus subacaulis and their antibacterial activities.

In a search for naturally occurring antibacterial compounds in medicinal plants, six hitherto unknown thiophene acetylenes, named 10,11-threo-xanthopappin D, 10,11-erythro-xanthopappin D, 10,11-cis-xanthopappin B, 5-(but-4-chloro-3-hydroxy-1-ynyl)-2-(Z)-pent-3-ene-1-ynylthiophene, 5-(but-4-chloro-3-hydroxy-1-ynyl)-2-(E)-pent-3-ene-1-ynylthiophene, 5-(but-3,4-dihydroxy-1-ynyl)-2-(Z)-pent-3-ene-1-ynylthiophene and two furanosesquiterpenes, as well as fifteen known compounds, were isolated from Xanthopappus subacaulis, which has been used as a traditional Tibetan medicine in China. A biosynthetic pathway to thiophene acetylenes was proposed and, the isolated compounds were tested for their antibacterial activity against five bacteria. Within the series of thiophene acetylenes tested, 10,11-threo-xanthopappin D with a threo configuration exhibited strong activity against Bacillus subtilis, with a minimum inhibitory concentration (MIC) of 7.25µg/mL, whereas 10,11-erythro-xanthopappin D with erythro configuration possessed broad-spectrum antibacterial activity against Escherichia coli, Bacillus cereus, Staphylococcus aureus and Erwinia carotovora, with MICs of 12.5, 15.5, 7.25 and 7.25µg/mL, respectively. Meanwhile, the compounds 10,11-cis-xanthopappin B, xanthopappin B, 5-(but-4-chloro-3-hydroxy-1-ynyl)-2-(Z)-pent-3-ene-1-ynylthiophene and 5-(but-4-chloro-3-hydroxy-1-ynyl)-2-(E)-pent-3-ene-1-ynylthiophene substituted with a Cl atom at C-14 showed moderate inhibitory activity against E. coli, B. cereus, S. aureus, E. carotovora and B. subtilis, with MICs ranging from 31.25 to 62.5µg/mL. The structures of these compounds were elucidated through the comprehensive analysis of spectroscopic data, including UV, IR, MS and NMR.

Cytotoxic and antimicrobial flavonoids from Cryptocarya concinna.

Five new flavonoids, cryptoconones A-E (1-5), along with six known compounds (6-11), were isolated from the stems of Cryptocarya concinna. The structures of these compounds were elucidated on the basis of spectroscopic data interpretation, and the absolute configurations were determined via circular dichroism spectra and X-ray crystal analysis. The cytotoxic and antimicrobial activities of these compounds were also evaluated. Compounds 9 and 10 exhibited moderate cytotoxic activities against HCT116, HT-29, SW480, and MDA-MB-231 cell lines with IC50 values ranging from 6.25 to 9.35 µM. Compounds 8 and 11 exhibited antimicrobial activity against Fusarium moniliforme and Botrytis cinerea, respectively, with the same minimum inhibitory concentration of 5 µg/mL.

Eremophilane-type sesquiterpenoids with diverse skeletons from Ligularia sagitta.

Five new highly oxygenated eremophilane-type sesquiterpenoids, possessing C19 (1 and 2), C15 (3 and 4), and C14 (8) skeletons, along with eight known eremophilenolides were obtained from the aerial parts of Ligularia sagitta. The absolute configuration of 1 was assigned by X-ray diffraction analysis and that of 3 by ECD spectroscopy. Compounds 1-10 were evaluated for their antibacterial activities against Staphyloccocus aureus, Bacillus subtilis, Escherichia coli, Bacillus cereus, and Erwinia carotovora. Compounds 4 and 5 displayed broad-spectrum inhibitory activity against these bacteria with MIC values of approximately 7.25 µg/mL, followed by 3 and 6 with MIC values in the range of 23.0-125.0 µg/mL. Compounds 3 and 8 showed mild activity against three human tumor cell lines (IC50 ≈ 13 µM). Preliminary structure-activity relationships for these eremophilenolides are reported.

[Effect of early intervention of liver-smoothing and blood-activating decoction combined with acupuncture on patients with post-stroke depression].

To study the effect of early intervention of liver-soothing and Blood-activating decoction combined with acupuncture in improving neurological functions, depressive symptom and life quality of patients with post-stroke depression, and compare with fluoxetine hydrochloride. Specifically, 63 patients with post-stroke depression were randomly divided into the traditional Chinese medicine (TCM) acupuncture group (31 cases) and the western medicine group (32 cases). On the basis of the conventional treatment of the primary disease, the TCM acupuncture group was treated with liver-soothing and blood-activating decoction and acupuncture, while the western medicine group was treated with fluoxetine hydrochloride for four weeks. In the follow-up visit six months later, scores of HAMD, NIHSS and SS-QOL were observed. The scores of HAMD and NIHSS of both groups were significantly decreased (P < 0.01), while the scores of SS-QOL increased significantly, with a notable difference compared with that before the treatment (P < 0.01). Specifically, the TCM acupuncture group's was superior to the western medicine group (P < 0.05). The study suggests that the early intervention of liver-soothing and blood-activating decoction combined with acupuncture on patients with post-stroke depression has the effect in relieving depression symptom and improving neurological functions, thereby improving their quality of life and prognosis.

[Recent researches of synthetic mercury sulfide in traditional medicine system].

OBJECTIVE: Herein, the synthesis, component, microstructure and pharmacological and toxicology researches of the Synthetic Mercury Sulfide (S-HgS) a kind of common drug in Chinese, Mongolia, Tibetan medicine, and Indian medicine system were summarized. The similar cognition about mercury toxicity & pharmacological action from some Asian regions was analyzed, and it can supply some useful direction for the traditional Asian medicine system. METHOD: Recent literatures both domestic and abroad were summarized and analyzed. RESULT: S-HgS is the basis of Vermilion, Mongolia-Vermilion, Zuotai, and Ras-sindoor. Athough the processes of synthesis are very different, but the microstructure and pharmacological & toxicology of S-HgS is similar. CONCLUSION: S-HgS has a far-ranging application,and unique curative effect. New technology such as nanotechnology can be used for improving the advancement of traditional Asian medicine.

Three new steroidal saponins from Fritillaria pallidiflora.

Three new steroidal saponins, pallidiflosides A (1), B (2), and C (3), have been isolated from the dry bulbs of Fritillaria pallidiflora Schrenk. Their structures were elucidated as 26-O-ß-d-glucopyranosyl-(25R)-furost-5,20(22)-dien-3ß,26-diol-3-O-ß-d-xylopyranosyl(1 â†’ 4)-[α-l-rhamnopyranosyl(1 â†’ 2)]-ß-d-glucopyranoside (1); 26-O-ß-d-glucopyranosyl-3ß,26-dihydroxyl-20,22-seco-25(R)-furost-5-en-20,22-dione-3-O-α-l-rhamnopyranosyl(1 â†’ 2)-ß-d-glucopyranoside (2); and (25R)-spirost-5-ene-3ß,17α-diol-3-O-ß-d-glucopyranosyl(1 â†’ 4)-ß-d-galactopyranoside (3) by spectroscopic techniques and chemical means.