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A review on pharmacological and analytical aspects of diosgenin:a concise report
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Kanika PATEL, Manoj GADEWAR, Vijay TAHILYANI, Dinesh Kumar PATEL
Natural Products and Bioprospecting. 2012, 2 (2): 46-52.
DOI: 10.1007/s13659-012-0014-3
Diosgenin is a steroidal sapogenin found in plants such as Dioscorea nipponoca, Solanum incanum, Solanum xanthocarpum and Trigonella foenum graecum. Diosgenin, biologically active phytochemicals have been used for the treatment of various types of disorder such as leukemia, inflammation, hypercholesterolemia and cancer. It is also able to prevent bone loss to the same extent as that of oestrogen. It is a typical initial intermediate for synthesis of steroidal compounds, oral contraceptives and sex hormones. Dioscorea, Costus and Trigonella are mainly used for the production of diosgenin. On the basis of literature survey it divulges that diosgenin has very impressive pharmacological profile and could be used as a medicine for the treatment of different types of disorders in the future. Thus, the present work aims to provide collective information in concern with its pharmacological activity and phytoanalytical techniques. This review will be beneficial to researches for the development of an alternative method for the treatment of innumerable diseases from diosgenin.
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Inhibition of P-glycoprotein by two artemisinin derivatives
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Babette STEGLICH, Anne MAHRINGER, Ying LI, Gary H. POSNER, Gert FRICKER, Thomas EFFERTH
Natural Products and Bioprospecting. 2012, 2 (2): 59-64.
DOI: 10.1007/s13659-012-0006-3
P-Glycoprotein/MDR1 represents an important component of the blood brain barrier and contributes to multidrug resistance. We investigated two derivatives of the anti-malarial artemisinin, SM616 and GHP-AJM-3/23, concerning their ability to interact with P-glycoprotein. The ability of the two compounds to inhibit P-glycoprotein(P-gp) activity was examined in sensitive CCRF-CEM and P-gp over-expressing and multidrug-resistant CEM/ADR5000 cells as well as in porcine brain capillary endothelial cells(PBCEC) by means of calcein-AM assays. Verapamil as well-known P-gp inhibitor was used as control drug. CEM/ADR5000 cells exhibited cross-resistance to GHP-AJM-3/23, but slight collateral sensitivity to SM616. Furthermore, SM616 inhibited calcein efflux both in CEM/ADR5000 and PBCEC, whereas GHP-AJM-3/23 did only increase calcein fluorescence in PBCEC, but not CEM/ADR5000. This may be explained by the fact that CEM/ADR5000 only express P-gp but not other ATP-binding cassette transporters, whereas PBCEC are known to express several ABC transporters and calcein is transported by more than one ABC transporter. Hence, SM616 may be the more specific P-gp inhibitor. In conclusion, the collateral sensitivity of SM616 as well as the inhibition of calcein efflux in both CEM/ADR5000 cells and PBCEC indicate that this compound may be a promising P-gp inhibitor to treat cancer therapy and to overcome the blood brain barrier.
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Rauvotetraphyllines A–E, new indole alkaloids from Rauvolfia tetraphylla
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Yuan GAO, Dong-Sheng ZHOU, Ling-Mei KONG, Ping HAI, Yan LI, Fei WANG, Ji-Kai LIU
Natural Products and Bioprospecting. 2012, 2 (2): 65-69.
DOI: 10.1007/s13659-012-0012-5
Five new indole alkaloids rauvotetraphyllines A-E(1-5), together with eight known analogues, were isolated from the aerial parts of Rauvolfia tetraphylla. The structures were established by means of spectroscopic methods.
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Cytosporinols A-C, new caryophyllene sesquiterpenoids from Cytospora sp.
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Yan LI, Chang-Wei LI, Cheng-Bin CUI, Xing-Zhong LIU, Yong-Sheng CHE
Natural Products and Bioprospecting. 2012, 2 (2): 70-75.
DOI: 10.1007/s13659-012-0018-z
Three new caryophyllene sesquiterpenoids, cytosporinols A-C(1-3), have been isolated from solid cultures of Cytospora sp. The structures of 1-3 were elucidated primarily by NMR spectroscopy, and 3 was further confirmed by X-ray crystallography. The absolute configurations of the C-11 secondary alcohol in 1 and the 6, 8-diol moiety in 3 were deduced using the modified Mosher and Snatzke's method, respectively. Compounds 2 and 3 showed moderate cytotoxicity against HeLa cells.
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Structure-function relationship of antimicrobial peptide cathelicidin Pc-CATH1
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Li DONG, Juan-Juan YANG, Ying WANG, Huan LIU, Li-Xian MU, Dong-Hai LIN, Ren LAI
Natural Products and Bioprospecting. 2012, 2 (2): 81-86.
DOI: 10.1007/s13659-012-0016-1
Cathelicidin Pc-CATH1 is a cathelicidin-derived myeloid antimicrobial peptide identified from Phasianus colchicus with strong antimicrobial activity against most of bacteria and fungi tested, including the clinically isolated(IS) drug-resistant strains. Considering the uniform distribution of net positive charge in both C-and N-terminus sequence of cathelicidin Pc-CATH1 and most of hydrophobic amino acid(aa) residues positioned in middle of the sequence, the antimicrobial peptide was used to investigate the structure-function relationship by truncating gradually N-or C-terminus amino acid residue. More than 10 modified peptide homologues(20-26 aa length) of cathelicidin Pc-CATH1 were found to keep strong antimicrobial abilities. The possible relationships between bioactivities including antimicrobial and hemolytic abilities, components of secondary structure, hydrophobicity, amphipathicity, net charge, and sequence length were investigated. The current work provided suggestions for structural and functional modification of linear, α-helical antimicrobial peptides containing no disulfided bridges.
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Glucosamine increases the expression of YKL-40 and osteogenic marker genes in hMSC during osteogenic differentiation
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Ramona LIEDER, Sigrídur Thóra REYNISDÓTTIR, Finnbogi THORMÓDSSON, Chuen-How NG, Jon Magnús EINARSSON, Jóhannes GÍSLASON, Jóhannes BJÖRNSSON, Sveinn GUDMUNDSSON, Pétur Henry PETERSEN, Ólafur Eysteinn SIGURJÓNSSON
Natural Products and Bioprospecting. 2012, 2 (2): 87-91.
DOI: 10.1007/s13659-012-0017-0
Human mesenchymal stem cells(hMSC) can be expanded in vitro and differentiated towards osteogenic, chondrogenic or adipogenic lineages, making them an attractive source for tissue engineering and regenerative medicine. Chitinase-like-proteins(CLPs) belong to the family 18 glycosyl hydrolases and are believed to play a role in inflammation and tissue remodelling. The aim of this study was to determine the effect of the aminosugar glucosamine on the expression of the CLP YKL-40 during osteogenic differentiation of hMSC. Glucosamine did not affect multipotency of hMSC nor proliferation rate of undifferentiated hMSC. YKL-40 was expressed during both expansion of undifferentiated hMSC and during osteogenic differentiation. A slight but nonsignificant increase in YKL-40 expression was observed with glucosamine, accompanied by a pH-dependent delay in mineralization. However, glucosamine induced higher expression of osteogenic marker genes.
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