A new nor-neolignan, named ellisinin A (1), has been isolated from the traditional Tibetan medicinal plants of Cremanthodium ellisii. Its structure has been determined on the basis of spectroscopic evidence, especiall...A new nor-neolignan, named ellisinin A (1), has been isolated from the traditional Tibetan medicinal plants of Cremanthodium ellisii. Its structure has been determined on the basis of spectroscopic evidence, especially by 2DNMR (H-1-(HCOSY)-H-1, HMQC, HMBC).展开更多
A new nor-sesquiterpene lactone ainsliatone A （1） was isolated from the aerial parts of Ainsliaeafulvioides. Its structure was established by the basis of spectroscopic methods and single-crystal X-ray diffraction a...A new nor-sesquiterpene lactone ainsliatone A （1） was isolated from the aerial parts of Ainsliaeafulvioides. Its structure was established by the basis of spectroscopic methods and single-crystal X-ray diffraction analysis.展开更多
Two novel C-nor-B-homo aconane-type diterpenes 4 and 5, featuring a unique eight-membered ring system, were obtained by the treatment of C-nor-C19-diterpenoid alkaloid 3 with HNO2 in 8% and 21% yields, respectively. S...Two novel C-nor-B-homo aconane-type diterpenes 4 and 5, featuring a unique eight-membered ring system, were obtained by the treatment of C-nor-C19-diterpenoid alkaloid 3 with HNO2 in 8% and 21% yields, respectively. Structures of these two compounds were established based on the combination of spectroscopic data, including HRESIMS, 1D and 2D NMR data. A olausible mechanism for the formation of 4 and 5 is also presented.展开更多
Nor-1α, 25-dihydroxy-22-oxo-vitamin D3 4 was synthesized by the coupling of known compound 5 and the A-ring phosphine oxide 6 followed by deprotection of the hydroxy functions.
Erythrinarbine 2, a novel alkaloid was isolated from the stem of Erythrina arborescens Roxb. Its structure and stereochemistry were elucidated on the basis of the spectral analysis (C-13 - H-1 COSY, H-1-H-1 COSY, NOES...Erythrinarbine 2, a novel alkaloid was isolated from the stem of Erythrina arborescens Roxb. Its structure and stereochemistry were elucidated on the basis of the spectral analysis (C-13 - H-1 COSY, H-1-H-1 COSY, NOESY and HMBC).展开更多
Compounds with dual action on cyclic adenosine monophosphate （cAMP） and cyclic guanosine monophosphate （cGMP） may be a treatment option for erectile dysfunction, as they not only promote penile erection but also p...Compounds with dual action on cyclic adenosine monophosphate （cAMP） and cyclic guanosine monophosphate （cGMP） may be a treatment option for erectile dysfunction, as they not only promote penile erection but also prevent the upregulation of phosphodiesterase-5. In this study, we examined the possible relaxant effect and mechanism of 17-nor-subincanadine E （SEC, 0.2-200 pmol I^-1）, a plant-derived alkaloid, in rabbit corpus cavernosum （RbCC） strips that had been precontracted by exposure to phenylephrine （10 pmol I^- 1） or a high concentration of K＋ （60 mmol I^- 1） in vitro. In addition to SEC＇s effect on cAMP and cGMP levels, electrical field stimulation （EFS） in phenylephrine-precontracted RbCC and calcium chloride （1-100 mmol I^-1） evoked responses in depolarized RbCC were analysed. SEC relaxed the phenylephrine-precontracted RbCCs in a concentration-dependent manner. Atropine, guanethidine and N-co-nitro-L-arginine methyl ester （L-NAME） did not have any effect on the relaxation of RBCCs. When 1H-1,2,4oxadiazole[4,3-a] quinoxalin-1-one （ODQ） was added, it effectively blocked the relaxant response of SEC. Although SEC enhanced the maximal relaxation produced by sodium nitroprusside （SNP） and forskolin in phenylephrine-precontracted cavernosal smooth muscle, it caused a decrease in the maximal contractile response induced by calcium chloride in depolarized RbCCs. The relaxant effect of SEC was paralleled by an increase in the tissue levels of the Cyclic nucleotides cAMP and cGMP. We conclude that SEC promotes the relaxation of RbCC, possibly favouring cAMP and cGMP accumulation and calcium blockade. This novel mechanism could be useful for patients who do not benefit from phosphodiesterase inhibitors and for those with endothelial and nitrergic dysfunction, such as patients with diabetes, hypertension and dyslipidaemias.展开更多
The synthesis of 14-epi-19-nor-22-oxa-1α,25（OH）2D3 5 was started from diol 8 via Fall＇s method, oxidation, epimerization, protection, coupling with the 19-nor-A-ring 7, and then deprotection of the hydroxyl functi...The synthesis of 14-epi-19-nor-22-oxa-1α,25（OH）2D3 5 was started from diol 8 via Fall＇s method, oxidation, epimerization, protection, coupling with the 19-nor-A-ring 7, and then deprotection of the hydroxyl functions.展开更多
The novel 19 nor l α ,25 dihydroxy vitamin D 3 analogues possessing an ethyl at the 2 position(4 and 5), were synthesized by coupling 25 hydroxy Windaus Grundmann ketone derivative 20 with A ring syntho...The novel 19 nor l α ,25 dihydroxy vitamin D 3 analogues possessing an ethyl at the 2 position(4 and 5), were synthesized by coupling 25 hydroxy Windaus Grundmann ketone derivative 20 with A ring synthons(15 and 19) respectively. The enantioselective synthesis of substituted bicyclic hexanes structure A ring synthons, started from all cis 3,5 dihydroxy 4 ethyl 1 (methoxycarbonyl)cyclohexane via lipase catalyzd asymmetrization, was demonstrated.展开更多
肝X受体（liver X receptor，LXRs）是核受体超家族成员，能被氧化的胆固醇衍生物结合并激活，在胆固醇逆向转运中起着非常重要的作用。LXRs在人体的代谢和炎症中都有重要作用。现从获得性免疫反应中LXRs通过调控胞膜的重要组成物质-胆...肝X受体（liver X receptor，LXRs）是核受体超家族成员，能被氧化的胆固醇衍生物结合并激活，在胆固醇逆向转运中起着非常重要的作用。LXRs在人体的代谢和炎症中都有重要作用。现从获得性免疫反应中LXRs通过调控胞膜的重要组成物质-胆固醇胞内水平，从而抑制T细胞增殖的方向，在硫转移酶2B-肝X受体-膜转运体G1（SULT281-LXR—ABCG1）轴线上探讨LXRs对获得性免疫的调节作用，以及LXRs对神经元衍生孤核受体（NOR-1）的调控作用，以进一步认识LXRs的调控功能。展开更多
文摘A new nor-neolignan, named ellisinin A (1), has been isolated from the traditional Tibetan medicinal plants of Cremanthodium ellisii. Its structure has been determined on the basis of spectroscopic evidence, especially by 2DNMR (H-1-(HCOSY)-H-1, HMQC, HMBC).
基金supported by program for Changjiang Scholars and Innovative Research Team in University(PCSIRT),NCET Foundation,NSFC(No.30725045)National 863 Program(No.2006AA02Z338)+3 种基金China Postdoctoral Science Foundation(No.20070410711)"973"program of China(No.2007CB507400)Shanghai Leading Academic Discipline Project(No.B906)in part by the Scientific Foundation of Shanghai China(Nos.07DZ19728,06DZ19717,06DZ19005).
文摘A new nor-sesquiterpene lactone ainsliatone A （1） was isolated from the aerial parts of Ainsliaeafulvioides. Its structure was established by the basis of spectroscopic methods and single-crystal X-ray diffraction analysis.
基金support for this research was provided from the National Natural Science Foundation of China(No.30472075)the Excellent Ph.D.Dissertation Foundation of China(No.200367).
文摘Two novel C-nor-B-homo aconane-type diterpenes 4 and 5, featuring a unique eight-membered ring system, were obtained by the treatment of C-nor-C19-diterpenoid alkaloid 3 with HNO2 in 8% and 21% yields, respectively. Structures of these two compounds were established based on the combination of spectroscopic data, including HRESIMS, 1D and 2D NMR data. A olausible mechanism for the formation of 4 and 5 is also presented.
基金Financial support from the National Natural Science foundation of China (No: 29972013) is gratefully acknowledged.
文摘Nor-1α, 25-dihydroxy-22-oxo-vitamin D3 4 was synthesized by the coupling of known compound 5 and the A-ring phosphine oxide 6 followed by deprotection of the hydroxy functions.
文摘Erythrinarbine 2, a novel alkaloid was isolated from the stem of Erythrina arborescens Roxb. Its structure and stereochemistry were elucidated on the basis of the spectral analysis (C-13 - H-1 COSY, H-1-H-1 COSY, NOESY and HMBC).
文摘Compounds with dual action on cyclic adenosine monophosphate （cAMP） and cyclic guanosine monophosphate （cGMP） may be a treatment option for erectile dysfunction, as they not only promote penile erection but also prevent the upregulation of phosphodiesterase-5. In this study, we examined the possible relaxant effect and mechanism of 17-nor-subincanadine E （SEC, 0.2-200 pmol I^-1）, a plant-derived alkaloid, in rabbit corpus cavernosum （RbCC） strips that had been precontracted by exposure to phenylephrine （10 pmol I^- 1） or a high concentration of K＋ （60 mmol I^- 1） in vitro. In addition to SEC＇s effect on cAMP and cGMP levels, electrical field stimulation （EFS） in phenylephrine-precontracted RbCC and calcium chloride （1-100 mmol I^-1） evoked responses in depolarized RbCC were analysed. SEC relaxed the phenylephrine-precontracted RbCCs in a concentration-dependent manner. Atropine, guanethidine and N-co-nitro-L-arginine methyl ester （L-NAME） did not have any effect on the relaxation of RBCCs. When 1H-1,2,4oxadiazole[4,3-a] quinoxalin-1-one （ODQ） was added, it effectively blocked the relaxant response of SEC. Although SEC enhanced the maximal relaxation produced by sodium nitroprusside （SNP） and forskolin in phenylephrine-precontracted cavernosal smooth muscle, it caused a decrease in the maximal contractile response induced by calcium chloride in depolarized RbCCs. The relaxant effect of SEC was paralleled by an increase in the tissue levels of the Cyclic nucleotides cAMP and cGMP. We conclude that SEC promotes the relaxation of RbCC, possibly favouring cAMP and cGMP accumulation and calcium blockade. This novel mechanism could be useful for patients who do not benefit from phosphodiesterase inhibitors and for those with endothelial and nitrergic dysfunction, such as patients with diabetes, hypertension and dyslipidaemias.
文摘The synthesis of 14-epi-19-nor-22-oxa-1α,25（OH）2D3 5 was started from diol 8 via Fall＇s method, oxidation, epimerization, protection, coupling with the 19-nor-A-ring 7, and then deprotection of the hydroxyl functions.
文摘The novel 19 nor l α ,25 dihydroxy vitamin D 3 analogues possessing an ethyl at the 2 position(4 and 5), were synthesized by coupling 25 hydroxy Windaus Grundmann ketone derivative 20 with A ring synthons(15 and 19) respectively. The enantioselective synthesis of substituted bicyclic hexanes structure A ring synthons, started from all cis 3,5 dihydroxy 4 ethyl 1 (methoxycarbonyl)cyclohexane via lipase catalyzd asymmetrization, was demonstrated.
文摘肝X受体（liver X receptor，LXRs）是核受体超家族成员，能被氧化的胆固醇衍生物结合并激活，在胆固醇逆向转运中起着非常重要的作用。LXRs在人体的代谢和炎症中都有重要作用。现从获得性免疫反应中LXRs通过调控胞膜的重要组成物质-胆固醇胞内水平，从而抑制T细胞增殖的方向，在硫转移酶2B-肝X受体-膜转运体G1（SULT281-LXR—ABCG1）轴线上探讨LXRs对获得性免疫的调节作用，以及LXRs对神经元衍生孤核受体（NOR-1）的调控作用，以进一步认识LXRs的调控功能。
