1.肉苁蓉化学成分及其生物活性研究 2.椭圆叶花锚化学成分的研究
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摘要
衰老是所有人类和多细胞生物一个正常的生理过程,延缓衰老在理论和实践上都有重要意义。运用现代生物医学技术从传统中草药中寻找和发现抗衰老的药物将会带来许多新的发现和突破。
肉苁蓉(Cistanche deserticola Y C.Ma),为列当科(Orobanchaceac)肉从蓉属多年生寄生草本植物,广泛分布于西北各省,是传统的补益类中药。现代临床和药理研究已证明肉苁蓉具有延缓衰老的作用。我们从肉苁蓉70%的乙醇提取部位共分离到15个化合物,其中12个化合物经光谱分析鉴定为:2'-乙酰基类叶升麻苷(Cd-1)、类叶升麻苷(Cd-2)、肉苁蓉苷C(Cd-3)、kankanoside G(Cd-4)、松果菊苷(Cd-5)、异类叶升麻苷(Cd-6)、肉苁蓉苷A(Cd-7)、红景天苷(Cd-8)、半乳糖醇(Cd-9)、薯蓣皂苷元(Cd-10)、β-胡萝卜苷(Cd-11)、β-谷甾醇(Cd-12)和硬脂酸(Cd-13)。其中7个化合物进行了对线粒体肿胀程度的影响
首次得到了第一个苯乙醇苷的单晶——红景天苷的单晶,,并通过X-射线衍射确定了它的绝对结构。通过化学发光法比较了红景天苷及其苷元捕获超氧阴离子的活性,发现它们的活性没有显著差异,说明它们的抗氧化活性主要与苷元结构有关。
椭圆叶花锚(Halenia elliptica D.Don)为龙胆科(Gentianaceae)花锚属一年生草本植物,主要分布于我国西部,在藏药中是一味治疗肝炎的药物。其乙醇提取物具有抑制乙肝表面抗原的活性。椭圆叶花锚富含口山酮和口山酮苷,在我们前期的研究中,已从石油醚和乙酸乙酯部位分离到了十个口山酮苷元。在此我们作了进一步的研究,从乙酸乙酯部位分离到一个口山酮苷和香豆素,从水部位分离到五个水溶性成分,经光谱分析鉴定分别为:1-O-β-D-葡萄吡喃糖]-3-羟基-4,5-二甲氧基口山酮(HE-1)、4-甲基-8-羟基香豆素(HE-2)、4-羧基-8-甲氧基香豆素(HE-3)和4-羧基-8-羟基香豆素(HE-4),其中HE-3为首次发现的新化合物,HE-2和HE-4为首次从自然界中分离得到,HE-1为首次从该植物中分离得到,其余各化合物HE-5～HE-7的结构正在鉴定中。
首次得到了1,7-二羟基-2,3,4-三甲氧基口山酮的单晶,并通过X-射线衍射确定了其晶体结构。
首次对椭圆叶花锚中九种口山酮的APCI和ESI的质谱行为进行了对照研究,九种口山酮的(+)APCI-MS都给出了明显的[M+H]~+离子,(-)APCI-Ms则给出了更多的碎片离子。结果表明APCI更适合口山酮类化合物的质谱测定。
1-羟基-2,3,5-三甲氧基口山酮(xan-1)、1-羟基-2,3,4,5-四甲氧基口山酮(xan-2)、1-羟基-2,3,7-三甲氧基口山酮(xan-3)以及1-羟基-2,3,4,7-四甲氧基口山酮(xan-4)是椭圆叶花锚中的四个主要化学成分,我们建立了等度HPLC法测定这四种口山酮的方法,研究了不同pH的缓冲液对这四种口山酮保留行为的影响,发现pH不仅显著地改变它们的保留时间,还对它们之间的分离度有很大的影响,在缓冲液的pH=8.0的条件下,这四种化合物能达到很好的分离,本方法快速、灵敏、重现性好,适合作为含量测定的方法。
The aging is one normal physiological process of the human body and the common characteristic of all poly-cellular organisms.To delay the aging process has the theoretical and practical importance to every person.Looking for the anti-aging drugs from the Traditional Chinese Medicine combined with modern biomedicine techniques will bring many new outbreaks and discoveries to us.
Cistanche deserticola Y.C.Ma,one of the plants of Orobanchaccae family,is a perennial and parastic herb growing in the northwest of China and widely known as a stminal tonic.It has been proven to have antisenile activity by modern clinical and pharmacological studies.Fifteen compounds were isolated from 70%ethanol extract of the sterm of Cistanche deserticola and twelvw of them were identified as 2'-acetylacteoside(Cd-1),acteoside(Cd-2),cistanosideC(Cd-3),kankanoside G(Cd-4), echinacoside(Cd-5),isoacteoside(Cd-6),cistanoside A(Cd-7),salidroside(Cd-8), galactitol(Cd-9),diosgenin(Cd-10),β-daucosterol(Cd-11),β-sitosterol(Cd-12)and octadecanoic acid(Cd-13) on the basis of spectra data.Seven of them was tested for the effect of anti-swelling of rat liver mitochondria.
The first single crystal of phenylethanoid glycosides,crystal of salidroside,was prepared and the crystal structure was determined by X-ray first time.The antioxidant activity of salidroside,evaluated as superoxide anion scavengers by chemiluminescence,studied by compared with it's aglycon,tyrosol.There was no significant difference in antioxidant activities between salidroside and tyrosol.It is obvious that the aromatic hydroxyl group is closely related to the superoxide anion scavenging action rather than the glucosyl moiety.
Halenia elliptica D.Don(Gentianaceae),as an annual plant,is widely distributed in west of China.The aerial part or full part of this plant has been used as a Tibetan medicinal herb to cure hepatic diseases for long time.It is found that the EtOH extract of H.elliptica has an inhibiting effect on the HBsAg.This plant in rich in xanthone aglycones and glycosides.In previous research,ten xanthone aglycones had been isolated from petroleum ether and ethyl acetate portion respectively.Further separation was taken,and a new xanthone glycoside and a coumarin were isolated from ethyl acetate portion and three water soluble coumarin were isolated from water portion.Them were identified as 1-O-β-D-glucopyranosyloxy-3-hydroxy-4,5-dimethoxyxanthone(HE-1), 4-methyl-8-hydroxycoumarin(HE-2),8-methoxy-4- carboxylcoumarin(HE-3),and 8-hydroxy-4-carboxylcoumarin(HE-4) on the basis of spectral data.HE-3 is a new compound and never found before.HE-2 and HE-4 is a new natural compound and never isolated from nature before.HE-1 was first isolated from genus Halenia.
A single crystal of dihydroxy xanthone,1,7-dihydroxy-2,3,4-trimethoxyxanthone monohydrate,was prepared and the crystal structure was determined by X-ray diffraction.It was first elucidated the structures by X-ray single-crystal analysis.
The APCI and ESI mass spectrometric behavior of nine xanthones isolated from Halenia elliptica was studied.These compounds gave dominant[M+H]~+ ion in positive mode of APCI and more fragment ion in negative mode of APCI.APCI is the best choice for the structural identification and determination of xanthones.
1-hydroxy-2,3,5-trimethoxyxanthone(xan-1),1-hydroxy-2,3,4,5-tetramethoxyxanthone(xan-2), 1-hydroxy-2,3,7-trimethoxyxanthone(xan-3),and 1-hydroxy-2,3,4,7-tetramethoxyxanthone(xan-4) are four major constituents in Halenia ellipitica.An isocratic RP-HPLC method for simultaneous determination of these xanthones was developed.Effect of change in buffer pH was studied.The pH change was not only significant in the retention but also in the resolution of four xanthone.A good separation between these four was performed in the buffer of pH=8.0.This method is simple,quick,sensitive,reliable and reproducible.It is the best choice for the determination of major xanthones in Halenia ellipitica.
肉苁蓉(Cistanche deserticola Y C.Ma),为列当科(Orobanchaceac)肉从蓉属多年生寄生草本植物,广泛分布于西北各省,是传统的补益类中药。现代临床和药理研究已证明肉苁蓉具有延缓衰老的作用。我们从肉苁蓉70%的乙醇提取部位共分离到15个化合物,其中12个化合物经光谱分析鉴定为:2'-乙酰基类叶升麻苷(Cd-1)、类叶升麻苷(Cd-2)、肉苁蓉苷C(Cd-3)、kankanoside G(Cd-4)、松果菊苷(Cd-5)、异类叶升麻苷(Cd-6)、肉苁蓉苷A(Cd-7)、红景天苷(Cd-8)、半乳糖醇(Cd-9)、薯蓣皂苷元(Cd-10)、β-胡萝卜苷(Cd-11)、β-谷甾醇(Cd-12)和硬脂酸(Cd-13)。其中7个化合物进行了对线粒体肿胀程度的影响
首次得到了第一个苯乙醇苷的单晶——红景天苷的单晶,,并通过X-射线衍射确定了它的绝对结构。通过化学发光法比较了红景天苷及其苷元捕获超氧阴离子的活性,发现它们的活性没有显著差异,说明它们的抗氧化活性主要与苷元结构有关。
椭圆叶花锚(Halenia elliptica D.Don)为龙胆科(Gentianaceae)花锚属一年生草本植物,主要分布于我国西部,在藏药中是一味治疗肝炎的药物。其乙醇提取物具有抑制乙肝表面抗原的活性。椭圆叶花锚富含口山酮和口山酮苷,在我们前期的研究中,已从石油醚和乙酸乙酯部位分离到了十个口山酮苷元。在此我们作了进一步的研究,从乙酸乙酯部位分离到一个口山酮苷和香豆素,从水部位分离到五个水溶性成分,经光谱分析鉴定分别为:1-O-β-D-葡萄吡喃糖]-3-羟基-4,5-二甲氧基口山酮(HE-1)、4-甲基-8-羟基香豆素(HE-2)、4-羧基-8-甲氧基香豆素(HE-3)和4-羧基-8-羟基香豆素(HE-4),其中HE-3为首次发现的新化合物,HE-2和HE-4为首次从自然界中分离得到,HE-1为首次从该植物中分离得到,其余各化合物HE-5～HE-7的结构正在鉴定中。
首次得到了1,7-二羟基-2,3,4-三甲氧基口山酮的单晶,并通过X-射线衍射确定了其晶体结构。
首次对椭圆叶花锚中九种口山酮的APCI和ESI的质谱行为进行了对照研究,九种口山酮的(+)APCI-MS都给出了明显的[M+H]~+离子,(-)APCI-Ms则给出了更多的碎片离子。结果表明APCI更适合口山酮类化合物的质谱测定。
1-羟基-2,3,5-三甲氧基口山酮(xan-1)、1-羟基-2,3,4,5-四甲氧基口山酮(xan-2)、1-羟基-2,3,7-三甲氧基口山酮(xan-3)以及1-羟基-2,3,4,7-四甲氧基口山酮(xan-4)是椭圆叶花锚中的四个主要化学成分,我们建立了等度HPLC法测定这四种口山酮的方法,研究了不同pH的缓冲液对这四种口山酮保留行为的影响,发现pH不仅显著地改变它们的保留时间,还对它们之间的分离度有很大的影响,在缓冲液的pH=8.0的条件下,这四种化合物能达到很好的分离,本方法快速、灵敏、重现性好,适合作为含量测定的方法。
The aging is one normal physiological process of the human body and the common characteristic of all poly-cellular organisms.To delay the aging process has the theoretical and practical importance to every person.Looking for the anti-aging drugs from the Traditional Chinese Medicine combined with modern biomedicine techniques will bring many new outbreaks and discoveries to us.
Cistanche deserticola Y.C.Ma,one of the plants of Orobanchaccae family,is a perennial and parastic herb growing in the northwest of China and widely known as a stminal tonic.It has been proven to have antisenile activity by modern clinical and pharmacological studies.Fifteen compounds were isolated from 70%ethanol extract of the sterm of Cistanche deserticola and twelvw of them were identified as 2'-acetylacteoside(Cd-1),acteoside(Cd-2),cistanosideC(Cd-3),kankanoside G(Cd-4), echinacoside(Cd-5),isoacteoside(Cd-6),cistanoside A(Cd-7),salidroside(Cd-8), galactitol(Cd-9),diosgenin(Cd-10),β-daucosterol(Cd-11),β-sitosterol(Cd-12)and octadecanoic acid(Cd-13) on the basis of spectra data.Seven of them was tested for the effect of anti-swelling of rat liver mitochondria.
The first single crystal of phenylethanoid glycosides,crystal of salidroside,was prepared and the crystal structure was determined by X-ray first time.The antioxidant activity of salidroside,evaluated as superoxide anion scavengers by chemiluminescence,studied by compared with it's aglycon,tyrosol.There was no significant difference in antioxidant activities between salidroside and tyrosol.It is obvious that the aromatic hydroxyl group is closely related to the superoxide anion scavenging action rather than the glucosyl moiety.
Halenia elliptica D.Don(Gentianaceae),as an annual plant,is widely distributed in west of China.The aerial part or full part of this plant has been used as a Tibetan medicinal herb to cure hepatic diseases for long time.It is found that the EtOH extract of H.elliptica has an inhibiting effect on the HBsAg.This plant in rich in xanthone aglycones and glycosides.In previous research,ten xanthone aglycones had been isolated from petroleum ether and ethyl acetate portion respectively.Further separation was taken,and a new xanthone glycoside and a coumarin were isolated from ethyl acetate portion and three water soluble coumarin were isolated from water portion.Them were identified as 1-O-β-D-glucopyranosyloxy-3-hydroxy-4,5-dimethoxyxanthone(HE-1), 4-methyl-8-hydroxycoumarin(HE-2),8-methoxy-4- carboxylcoumarin(HE-3),and 8-hydroxy-4-carboxylcoumarin(HE-4) on the basis of spectral data.HE-3 is a new compound and never found before.HE-2 and HE-4 is a new natural compound and never isolated from nature before.HE-1 was first isolated from genus Halenia.
A single crystal of dihydroxy xanthone,1,7-dihydroxy-2,3,4-trimethoxyxanthone monohydrate,was prepared and the crystal structure was determined by X-ray diffraction.It was first elucidated the structures by X-ray single-crystal analysis.
The APCI and ESI mass spectrometric behavior of nine xanthones isolated from Halenia elliptica was studied.These compounds gave dominant[M+H]~+ ion in positive mode of APCI and more fragment ion in negative mode of APCI.APCI is the best choice for the structural identification and determination of xanthones.
1-hydroxy-2,3,5-trimethoxyxanthone(xan-1),1-hydroxy-2,3,4,5-tetramethoxyxanthone(xan-2), 1-hydroxy-2,3,7-trimethoxyxanthone(xan-3),and 1-hydroxy-2,3,4,7-tetramethoxyxanthone(xan-4) are four major constituents in Halenia ellipitica.An isocratic RP-HPLC method for simultaneous determination of these xanthones was developed.Effect of change in buffer pH was studied.The pH change was not only significant in the retention but also in the resolution of four xanthone.A good separation between these four was performed in the buffer of pH=8.0.This method is simple,quick,sensitive,reliable and reproducible.It is the best choice for the determination of major xanthones in Halenia ellipitica.
引文
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