Pyrans

Publication Title: 
Current Pharmaceutical Design

Melatonin and the following approved or investigational synthetic melatoninergic agonists are compared with regard to half-life, receptor affinity, metabolism and additional properties: TIK-301, piromelatine, GG-012, AH-001, AH-017, agomelatine, ramelteon, GR 196429, MA-2, tasimelteon, UCM765, and UCM924. Apart from restrictions from the respective approvals, theoretical limits of treatment are outlined as they result from chronobiological, genetic, epigenetic, degenerative or toxicological considerations.

Author(s): 
Hardeland, R¸diger
Publication Title: 
Bulletin of the World Health Organization

Eleven Thai isolates and one West African isolate of Plasmodium falciparum were tested for their susceptibility to the Chinese antimalarial drugs artemisinine (qinghaosu) and artemether. The isolates were cultivated by the Trager-Jensen candle-jar technique and exposed to the action of the drugs for 36-48 hours. Artemisinine inhibited growth of most isolates at 10(-7)-10(-8) mol/litre and artemether at 10(-8) mol/litre (with an initial parasitaemia of 0.5-1.0%).

Author(s): 
Thaithong, S.
Beale, G. H.
Publication Title: 
Cancer Letters

The in vitro anti-tumor promoting effect of the methanolic extracts of iridoids containing three plants and several pure iridoids isolated from other plants, has been evaluated. The alcoholic extracts of Paederia scandens, P. scandens var. mairei and the Ayurvedic herbal remedy Picrorhiza kurrooa were tested against the Epstein-Barr virus. Among the 15 iridoids evaluated, the glycoside, paederoside, displayed the highest order of anti-tumor promoting activity.

Author(s): 
Kapadia, G. J.
Sharma, S. C.
Tokuda, H.
Nishino, H.
Ueda, S.
Publication Title: 
Journal of Ethnopharmacology

ETHNOPHARMACOLOGICAL RELEVANCE: Ajuga bracteosa Wall Ex Benth. (Labiateae) is described in Ayurveda for the treatment of rheumatism, gout, palsy and amenorrhea. AIM OF THE STUDY: The aim of present investigation is to study anti-inflammatory activity of Ajuga bracteosa, to understand possible mechanism of action and to identify the constituents responsible for its activity.

Author(s): 
Gautam, Raju
Jachak, Sanjay M.
Saklani, Arvind
Publication Title: 
BMC complementary and alternative medicine

BACKGROUND: The objective of this review is to determine the effectiveness of Harpagophytum procumbens preparations in the treatment of various forms of musculoskeletal pain. METHODS: Several databases and other sources were searched to identify randomized controlled trials, quasi-randomized controlled trials, and controlled clinical trials testing Harpagophytum preparations in adults suffering from pain due to osteoarthritis or low back pain.

Author(s): 
Gagnier, Joel J.
Chrubasik, Sigrun
Manheimer, Eric
Publication Title: 
Analytical Chemistry

Alzheimer's disease is the most common cause of the loss of cognitive function among the elderly, and the aggregation and deposition of misfolded beta-amyloid protein (Abeta) contribute to this progressive central nervous system decline. Therefore, compounds that inhibit or even reverse Abeta aggregation might be useful for the treatment or prevention of Alzheimer's disease.

Author(s): 
Cheng, Xun
van Breemen, Richard B.
Publication Title: 
Biochemical and Biophysical Research Communications

We report molecular modeling and functional confirmation of Ole and HT binding to HIV-1 integrase. Docking simulations identified two binding regions for Ole within the integrase active site. Region I encompasses the conserved D64-D116-E152 motif, while region II involves the flexible loop region formed by amino acid residues 140-149. HT, on the other hand, binds to region II. Both Ole and HT exhibit favorable interactions with important amino acid residues through strong H-bonding and van der Waals contacts, predicting integrase inhibition.

Author(s): 
Lee-Huang, Sylvia
Huang, Philip Lin
Zhang, Dawei
Lee, Jae Wook
Bao, Ju
Sun, Yongtao
Chang, Young-Tae
Zhang, John
Huang, Paul Lee
Publication Title: 
Biochemical and Biophysical Research Communications

We have identified oleuropein (Ole) and hydroxytyrosol (HT) as a unique class of HIV-1 inhibitors from olive leaf extracts effective against viral fusion and integration. We used molecular docking simulation to study the interactions of Ole and HT with viral targets. We find that Ole and HT bind to the conserved hydrophobic pocket on the surface of the HIV-gp41 fusion domain by hydrogen bonds with Q577 and hydrophobic interactions with I573, G572, and L568 on the gp41 N-terminal heptad repeat peptide N36, interfering with formation of the gp41 fusion-active core.

Author(s): 
Lee-Huang, Sylvia
Huang, Philip Lin
Zhang, Dawei
Lee, Jae Wook
Bao, Ju
Sun, Yongtao
Chang, Young-Tae
Zhang, John
Huang, Paul Lee
Publication Title: 
FEBS letters

Recent experimental study found that OLE (olive leaf extract) has anti-HIV activity by blocking the HIV virus entry to host cells [Lee-Huang, S., Zhang, L., Huang, P.L., Chang, Y. and Huang, P.L. (2003) Anti-HIV activity of olive leaf extract (OLE) and modulation of host cell gene expression by HIV-1 infection and OLE treatment. Biochem. Biophys. Res. Commun. 307, 1029; Lee-Huang, S., Huang, P.L., Zhang, D., Lee, J.W., Bao, J., Sun, Y., Chang, Y.-Tae, Zhang, J.Z.H. and Huang, P.L. (2007) Discovery of small-molecule HIV-1 fusion and integrase inhibitors oleuropein and hydroxytyrosol.

Author(s): 
Bao, J.
Zhang, D. W.
Zhang, J. Z. H.
Huang, P. Lee
Huang, P. Lin
Lee-Huang, S.
Publication Title: 
Chemical & Pharmaceutical Bulletin

A new secoiridoid glucoside designated amaronitidin (1) was isolated from the Peruvian folk medicine "Hercampuri" (Gentianella nitida) along with three known secoiridoid glucosides. Their structures were determined by extensive spectroscopic investigation.

Author(s): 
Kawahara, N.
Masuda, K.
Sekita, S.
Satake, M.
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