Wansheng Chen

Timosaponin B-II improves memory and learning dysfunction induced by cerebral ischemia in rats

Sapogenins from Anemarrhenae asphodeloides was reported to improve the learning and memory abilities. In this study, we investigated the effect of Timosaponin B-II(TB-II), a purified extract from A. asphodeloidesb on rat vascular dementia (VD) produced by transient (2h) middle cerebral artery occlusion. The learning and memory abilities of rats were measured by water maze task and passive avoidance task. Daily oral administration of TB-II at two different dose levels of 100 and 200 mg/kg resulted in a significant improvement of the deficit in the learning of the water maze task, beginning 14 days after ischemia. Shortened mean escape latency was detected in TB-II group compared with model group during the same trial days. TB-II treatment also significantly reversed the ischemia-induced retention deficit determined by a one trial step-down type of passive avoidance task. Meanwhile, the expression of interleukin-10, an anti-inflammatory cytokine, and its receptor were significantly increased in TB-II treated VD rats. The results presented the first evidence of a neuroprotective effect of TB-II in the model of vascular dementia. We suggest that the anti-dementia effect by TB-II is derived at least in part from its anti-inflammatory properties.

Hippolachnin A, a New Antifungal Polyketide from the South China Sea Sponge Hippospongia lachne

Hippolachnin A (1), a polyketide possessing an unprecedented carbon skeleton with a four-membered ring, was isolated from the South China Sea sponge Hippospongia lachne. The structure was elucidated using MS and NMR spectroscopic analyses, and the absolute configuration was determined using a calculated ECD method. Hippolachnin A demonstrated potent antifungal activity against three pathogenic fungi, Cryptococcus neoformans, Trichophyton rubrum, and Microsporum gypseum, with a MIC value of 0.41 μM for each fungus.

Anti-inflammatory triterpenes from the leaves of Rosa laevigata.

Bioassay-guided fractionation of an EtOAc extract of the leaves of Rosa laevigata afforded two new 19-oxo-18,19-seco-ursane-type triterpenes (1 and 3), a new ursane-type nortriterpene (2), a new ursane-type triterpene lactone saponin (4), and two new oleanane-type triterpenoids (5 and 6), together with eight known triterpenoids (7-14). Compound 1, a 19-oxo-18,19-seco-28-norursane, possesses a conjugated diene between C-12 and C-17. Several of the isolated compounds (1, 5, 7, 11, and 13) exhibited moderate activities in anti-inflammatory assays in vitro.

Hippolides A-H, acyclic manoalide derivatives from the marine sponge Hippospongia lachne.

Eight new acyclic manoalide-related sesterterpenes, hippolides A-H (1-8), together with two known manoalide derivatives, (6E)-neomanoalide (9) and (6Z)-neomanoalide (10), were isolated from the South China Sea sponge Hippospongia lachne. The absolute configurations of 1-8 were established by the modified Moshers method and CD data. Compound 1 exhibited cytotoxicity against A549, HeLa, and HCT-116 cell lines with IC50 values of 5.22×10(-2), 4.80×10(-2), and 9.78 μM, respectively. Compound 1 also showed moderate PTP1B inhibitory activitiy with an IC50 value of 23.81 μM, and compound 2 showed moderate cytotoxicity against the HCT-116 cell line and PTP1B inhibitory activity with IC50 values of 35.13 and 39.67 μM, respectively. In addition, compounds 1 and 5 showed weak anti-inflammatory activity, with IC50 values of 61.97 and 40.35 μM for PKCγ and PKCα, respectively.

Simplextones A and B, Unusual Polyketides from the Marine Sponge Plakortis simplex

Two novel polyketides, simplextones A (1) and B (2), were isolated from the sponge Plakortis simplex. Their structures were established by spectroscopic methods. The absolute configurations were assigned by modified Moshers method, X-ray crystallographic analysis, and quantum mechanical calculation of the electronic circular dichroism (ECD) spectrum. Compounds 1 and 2 featured an unprecedented polyketide skeleton via the connection of a single carbon-carbon bond to form a cyclopentane. These compounds also exhibited moderate cytotoxicity.

Anti-inflammatory secondary metabolites from the leaves of Rosa laevigata

Bioassay-guided fractionation of a n-BuOH-soluble extract of the leaves of Rosa laevigata led to the isolation of three new 19-oxo-18,19-seco-ur-sane-type triterpenoids, laevigins A-C (1-3), a new oleanane-type triterpenoid saponin, laevigin D (4), a new geranylmethylbenzoate, 5-[(2″E,6″S)-6″,7″-dihydroxy-3″,7″-dimethyl-2″-octen-1″-yl]-2-(β-D-glucopyranosyloxy)-methyl benzoate (5), together with 9 known compounds (6-14). Their structures were elucidated by spectroscopic and chemical methods. Compounds 4, 9, 11, and 12 significantly suppressed the LPS-stimulated NF-κB transcriptional activity and the release of TNFα, IL-1β, IL-6, and IL-10 in mouse RAW 264.7 macrophages. The compound 12 exhibited moderate inhibition on NF-κB transcriptional activity with an IC50 value of 23.21 μM. The IC50 values of compound 12 were measured as 14.32, 8.53, 8.04, and 10.38 μM for the inhibitory activity on TNFα-release, IL-1β-release, IL-6-release, and IL-10-release, respectively.

The medicinal uses of Callicarpa L. in traditional Chinese medicine: an ethnopharmacological, phytochemical and pharmacological review.

ETHNOPHARMACOLOGICAL RELEVANCE Callicarpa L. (Verbenaceae) has been used for centuries in Traditional Chinese Medicine (TCM) for the prevention and treatment of a wide number of health disorders such as inflammation, rheumatism, hematuria, fracture, hematemesis, menoxenia, gastrointestinal bleeding, scrofula, etc. AIMS OF THE REVIEW To assess the scientific evidence for therapeutic Callicarpa in TCM and to identify future research needs. METHODS The available information on the ethnopharmacological uses in Chinese medicine, phytochemistry, pharmacology and clinical practice of Callicarpa species was collected via a library and electronic search (PubMed, ScienceDirect, Google Scholar and CNKI). RESULTS A variety of ethnomedical use of Callicarpa has been recorded in many ancient Chinese books. Phytochemical investigation of this genus has resulted in identification of more than 200 chemical constituents, among which diterpenes, triterpenoids and flavonoids are the predominant groups. The isolates and crude extract have exhibited a wide spectrum of in vitro and in vivo pharmacological effects involving anti-inflammatory, hemostatic, neuroprotective, anti-amnesic, antitubercular, antioxidant, antimicrobial and analgesic activities. Preparations containing Callicarpa species exerted good efficacy on clinical applications of gynecological inflammation, internal and external hemorrhage as well as acne vulgaris and chronic pharyngitis, etc. From the toxicity perspective, only three Callicarpa species have been assessed. CONCLUSIONS Pharmacological results have validated the use of Callicarpa species in the traditional medicine. As literature demonstrated, terpenoids and flavonoids are perhaps responsible for most of the activities shown by the plants of this genus. However, the detailed active compounds and the underlying mechanisms remain a work in progress. In addition, more attention should be paid to C. nudiflora as well as the domain of rheumatism.

A new chromene glycoside from Tithonia diversifolia

A new chromene glycoside, 6-acetyl-2,2-dimethylchromene-8-O-β-D-glucoside, together with four known compounds were isolated from the aerial parts of Tithonia diversifolia. Their structures were established by 1H, 13C NMR, and HMQC together with the other physical and chemical investigations.

New cytotoxic oxygenated sterols from marine bryozoan Bugula neritina

Two new oxygenated sterols, 3β,24(S)-dihydroxycholesta-5,25-dien-7-one (1) and 3β,25-dihydroxycholesta-5,23-dien-7-one (2), were isolated from the marine bryozoan Bugula neritina. Their chemical structures were established on the basis of spectroscopic analysis. Both compounds exhibited cytotoxicity to three human cancer cell lines (HepG2, HT-29 and NCI-H460), with IC50 values between 22.58 and 53.41 µg mL−1.

Steroids from the marine bryozoan Bugula neritina

One new compound, 3β-hydroxy-25-methoxy-(23E)-cholesta-5,23-diene (1), together with five known steroids, cholesteryl myristate (2), cholest-4-en-3-one (3), cholesterol (4), 3β,5α,9α-trihydroxy-(22E,24R)-ergosta7,22-dien-6-one (5), and 3β,5α,6β-trihydroxy-(22E,24R)-ergosta-7,22-diene (6), were isolated and identified from the marine bryozoan Bugula neritina.