Equisetin is an anti-obesity candidate through targeting 11β-HSD1

Obesity is increasingly prevalent globally, searching for therapeutic agents acting on adipose tissue is of great importance. Equisetin (EQST), a meroterpenoid isolated from a marine sponge-derived fungus, has been reported to display antibacterial and antiviral activities. Here, we revealed that EQST displayed anti-obesity effects acting on adipose tissue through inhibiting adipogenesis in vitro and attenuating HFD-induced obesity in mice, doing so without affecting food intake, blood pressure or heart rate. We demonstrated that EQST inhibited the enzyme activity of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), a therapeutic target of obesity in adipose tissue. Anti-obesity properties of EQST were all offset by applying excessive 11β-HSD1's substrates and 11β-HSD1 inhibition through knockdown in vitro or 11β-HSD1 knockout in vivo. In the 11β-HSD1 bypass model constructed by adding excess 11β-HSD1 products, EQST's anti-obesity effects disappeared. Furthermore, EQST directly bond to 11β-HSD1 protein and presented remarkable better intensity on 11β-HSD1 inhibition and better efficacy on anti-obesity than known 11β-HSD1 inhibitor. Therefore, EQST can be developed into anti-obesity candidate compound, and this study may provide more clues for developing higher effective 11β-HSD1 inhibitors.

Effects of cembrane-type diterpenes on proliferation of PC12 cells and their antagonistic effects on neurotoxicity induced by glutamate / 中西医结合学报

To investigate the effects of cembrane-type diterpenes extracted from Sinularia flexibilis on the proliferation of PC12 cells and their protective effects on PC12 cells exposed to glutamate.

Isolation and identification of compounds from marine mangrove plant Avicennia marina / 北京大学学报(医学版)

Objective:To investigate the chemical constituents from Avicennia marina.Methods:The isolation and purification of the CH2Cl2 and n-BuOH fractions of this plant were performed,and the chemical structures were elucidated by spectral analysis as well as comparison of their spectral data with literature values.Results:Three novel compounds were obtained and identified as erythro-guaiacylglycerol-?-ferulic acid ether(1),marinnone A(16) and marinnone B(17),along with eighteen known compounds as threo-guaiacylglycerol-?-ferulic acid ether(2),eleutheroside E2(3),(+)-lirioresinol A(4),dihydroxymethyl-bis(3,5-dimethoxy-4-hydroxyphenyl) tetrahydrofuran-9-O-?-glucopyranoside(5),(+)-lyoniresinol 3a-O-?-D-glucopyranoside(6),(-)-lyoniresinol 3a-O-?-D-glucopyranoside(7),epi-pinoresinol(8),leucoseceptoside A(9),jionoside C(10),salsaside A(11),ilicifolioside A(12),acteoside(13),isoacteoside(14),ethyl ferulate(15),avicennone D(18),avicenone E(19),avicennol C(20),and stenocarpoquinone B(21).Conclusion:Three new compounds(1,16 and 17) were obtained and thirteen known compounds,2-12,14 and 15 were isolated from Avicennia genus for the first time.

Chemical constituents from chinese marine sponge Cinachyrella australiensis / 北京大学学报(医学版)

Objective: To investigate the secondary metabolites from Chinese marine Sponge Cinachyrella australiensis. Methods: Column chromatography techniques including HPLC were used for the separation and purification of the compounds, and extensive spectral analyses including various 2D NMR spectra were employed for structure elucidation. Results: Nineteen compounds were obtained ,including 2 methyoxy 6,12,15 trien 8 yne octadecanoic acid(1), 2 benzenedicarboxylic acid dibutyl ester(2), 1,2 benzenedicarboxylic acid bis(2 ethylhexyl)ester(3), ( ) (3S) 1,2,3,4 tetrahydro ? carboline 3 carboxylic acid(4), L Tryptophan (5), p hydroxylbenzaldehyde (6), p hydroxyl benzylethanol(7), p hydroxyl benzyl propanol(8), cholesta 4 en 3 ol(9), 2 methyl 6 amino 9 (2 deoxy ? D ribofuranosyl purine(10), 2' Deoxyadenosine (11), 6 amino 9 ? D ribofuranosyl 9H purine (12),uracil(13), thymine(14), thymidine(15), 1 (2 deoxy ? D Ribofuranosyl)uracil(16), 1 ethyl ? (2 deoxy) ? D ribofuranos(17),isolumichrome(18),and zarzissine(19).Conclusion:Compounds 1 and 18 are new natural products,and compounds 2 to 17 as well as 19 are isolated from this species for the first time.

Nucleosides from Anthopleura stell / 中草药

To study the chemical constituents of sea anemone, Anthopleura stell Verrill.Methods　The chemical constituents were isolated and purified by chromatographic methods and their structures elucidated by chemical evidences and spectra data.Results　5 nucleosides were obtained and identified from the ethanolic extract as 2-hydroxy purine (Ⅰ); deoxyinosine (Ⅱ); 1-methylxanthosine (Ⅲ); deoxyguanosine (Ⅳ), and deoxyribo-thymidine (Ⅴ).Conclusion　Compound Ⅲ was a new natural product， while the others were found from sea anemone for the first time.

Study on nucleotidoids from n-butyl alcohol part of sponge Cinachyrella australiensis / 中草药

Object To search for bioactive secondary metabolites from marine organisms, the marine sponge Cinachyrella australiensis was collected from Hainan Island, Southern China Sea to develop the efficient drug for human beings. Methods Silic gel flash chromatography in association with reverse phase semipreparative HPLC was performed for the isolation and purification of the ethanol extracts, and extensive spectroscopy including 2D NMR spectra as well as the comparison of the spectral data with those reported in literatures was applied for the structure elucidation. Results Seven nucleotidoids were isolated and identified. They are named as 2-methyl-6-amino-9-(2-deoxy-?-D-ribofuranosyl)-purine (Ⅰ), 2′-deoxyadenosne (Ⅱ), 6-amino-9-?-D-ribofuranosyl-9H-punne (Ⅲ), uracill (Ⅳ), thymine (Ⅴ), thymidine (Ⅵ), 1-(2-deoxy-?-D-ribofuranosyl) uracil (Ⅶ). Conclusion The sponge C. australiensis is systemically separated, and then two kinds of nucleotidoids compound are extracted.

Chemical constituents of mangrove plant Excoecaria agallocha in Hainan Province / 中草药

Objective To study the chemical constituents from mangrove Excoecaria agallocha.Methods The chemical constituents were separated and purified by chromatographic methods after solventextraction and were identified by spectroscopic analyses(EI-MS,1D NMR).Results Twelve compoundswere isolated from this plant and identified as:14-taraxeren-3-one(Ⅰ),dibutyl phthalate(Ⅱ),?-amyrin(Ⅲ),18-oleanen-3-ol(Ⅳ),18-oleanen-3-one(Ⅴ),phaeophytin A(Ⅵ),betulin(Ⅶ),?-rosasterol(Ⅷ),?-sitosterol(Ⅸ),betulinic aicd(Ⅹ),oleanolic acid(Ⅺ),ursolic acid(Ⅻ).Conclusion CompoundsⅦ,Ⅷ,Ⅹ,andⅫare isolated from this plant for the first time.

CHEMICAL CONSTITUENTS FROM CHINESE ANTHO-PLEURA XANTHOGRAMMICA BERKLY(II) / 中国海洋药物

From ethyl acetate fraction of Chinese Anthopleura xanthogrammica B, collected from Qingdao beach, three new glycerolipids named 1-O-hexadecanoyl-2-O (9-oc-tadecenoyl )-3-O-( 9, 12-octadecadienoyl ) glycerol (3)'1-O-hexadecahoyl-3-O-(14-eiosyle-cenoyl)glycerol (4)and l-O-(9,12-octadecadienoyl)-2-O-(9,12-octadecadienoyl)glycerol (5) as well as two lipidic acids named 9,12-octadecadienoic acidd) and 9,14-docosandienoic acid (2) were isolated. Their structures were identified by various spectrial(IR,PNMR ,CNMR, MS,et al)analysis and chemical conversion.

Study of synergistic effects of Spirulina platensis on inducing IL-2 / 中国海洋药物

It has been shown that Spirulina platensis can regulate imminological functions.We report here that crude extract and purified components (phycocyanin and polysaccharide) from Spirulina platensis can induce secretion of IL 2 in splenocyte of BALB/C mice by means of MTT method.In the present study,we showed that all experimental components can't enhance proliferation of CTLL which was used in MTT method,but induce IL 2 secretion in splenocyte of BALB/C mice in three different concentration (0.01,0.1,1 g?L -1 ).Indeed the purified components especially phycocyanin part showed stronger IL 2 inducing activity than the crude one.IL 2 level was grow up when the incubation time of splenocyte and Spirulina platensis increased.In the concentration of 1 g?L -1 ,detected Spirulina platensis in our study assist IL 2 inducing of ConA (2mg?L -1 ) in splenocyte of BALB/C mice.

Xanthone derivatives from medicinal plant Swertia mileensis / 中草药

Object Isolation and structural identification of xanthone derivative from medicinal plant Swertia mileensis T N Ho et W L Shih were carried out Methods The chemical constituents were isolated and purified by extensive silica gel column chromatography and their structures were elucidated by chemical evidences and spectral analysis Results There were 12 xanthone analogues named 1 hydroxy 2, 3, 4, 5 tetramethoxyxanthone, (Ⅰ); 1 hydroxy 2, 3, 7 trimethoxyxanthone, (Ⅱ); 1 hydroxy 2, 3, 5, 7 tetramethoxyxanthone, (Ⅲ); 1, 5 dihydroxy 2, 3 dimethoxyxanthone, (Ⅳ); 1, 5 dihydroxy 2, 3, 7 trimethoxyxanthone, (Ⅴ); 1 hydroxy 2, 3, 5 trimethoxyxanthone, (Ⅵ); 1, 5 dihydroxy 2, 3, 4, 7 tetramethoxyxanthone, (Ⅶ); 1, 8 dihydroxy 2, 3, 6 trimethoxyxanthone, (Ⅷ); 1 hydroxy 2, 3, 4, 7 tetramethoxyxanthone, (Ⅸ); 1, 2, 3, 5 tetromethoxyxanthone, (Ⅹ); 1 hydroxyl 2, 3, 4, 6 tetramethoxyxanthone, (Ⅺ); 1 hydroxyl 2, 3, 6, 8 tetramethoxyxanthone, ( ⅩⅡ ) Conclusion Compounds Ⅰ, Ⅲ, Ⅳ, Ⅴ, Ⅶ ⅩⅡ were first isolated from S. mileensis