To study the biopharmaceutics characteristics of paris saponin Ⅶ(PSⅦ). The solubility of PSⅦ was evaluated by measurement of the equilibrium solubility in different solvents and media. The permeability of PSⅦ was ...To study the biopharmaceutics characteristics of paris saponin Ⅶ(PSⅦ). The solubility of PSⅦ was evaluated by measurement of the equilibrium solubility in different solvents and media. The permeability of PSⅦ was evaluated by measuring the oil/water partition coefficient(lgP_(app)) and determining the apparent permeability coefficient(PC_(app)) on a mono-layer Caco-2 cell model. The effects of p-glycoprotein and multidrug resistance related protein 2 on PSⅦ transport in mono-layer Caco-2 cell model were further investigated. Finally, the small intestinal absorption of PSⅦ was investigated in rat. In solvents of different pH, the equilibrium solubility of PSⅦ was quite low, and the dose number of PSⅦ was larger than 1. The lgP_(app) of PSⅦ was less than 0. The apparent permeability coefficient [PC_(app)(AP-BL)] of PSⅦ in mono-layer Caco-2 cell model was less than 14.96 × 10^(-6) cm·s^(-1), and the efflux ratio of PSⅦ in mono-layer Caco-2 cell model was less than 1. The transport rate of PSⅦ in mono-layer Caco-2 cell model was not affected by the inhibitors of p-glycoprotein and multidrug resistance related protein 2. After oral administration, PSⅦ could be detected in rat intestinal contents, but could not be detected in the small intestinal mucosa. PSⅦ showed low solubility and permeability,which would result in low oral bioavailability in clinic. PSⅦ belonged to Class IV compound in biopharmaceutics classification system.展开更多
北部冬麦区是我国重要的小麦主产区之一,对该麦区历年国审小麦品种进行回溯分析有助于小麦品种资源的合理利用。本研究基于产量与熟期、穗数、穗粒数、千粒重、容重、品质指数、抗病指数和抗寒指数等性状的组合,采用品种-产量×性...北部冬麦区是我国重要的小麦主产区之一,对该麦区历年国审小麦品种进行回溯分析有助于小麦品种资源的合理利用。本研究基于产量与熟期、穗数、穗粒数、千粒重、容重、品质指数、抗病指数和抗寒指数等性状的组合,采用品种-产量×性状组合(GYT,genotype by yield×trait)双标图方法对2003-2023年期间北部冬麦区47个国审小麦品种进行了综合分析和分类评价。结果表明,47个国审小麦品种可划分为4个特征显著的品种类型。其中,Ⅰ型品种综合表现优秀,在产量与早熟性、抗病性、抗寒性、千粒重和容重等性状组合上表现突出,在产量与穗数、穗粒数和品质指数组合上表现优良,在生产上推广应用价值最高,主要包括京麦179、京农16和津麦3118等8个品种。Ⅱ型品种综合表现优良,在产量与品质指数、穗数组合上表现突出,在产量与抗病指数、抗寒指数组合上表现稍差,在生产上推广应用价值较高,但应注意生产安全,主要包括京麦202、京农19和轮选158等13个品种。Ⅲ型品种的产量与抗病和抗寒指数组合最好,但在其余性状组合上表现差,综合生产应用价值有限,可作为抗性亲本。Ⅳ型品种综合表现较差,可选择单性状表现优良的品种作为育种亲本应用。根据各品种在GYT双标图ATA轴上的投影位置,筛选出综合表现优良的京麦179、京农16、津麦3118、京麦189、京麦202、京花12号、京农19、轮选158和中麦623等品种。本研究采用GYT双标图分析方法基于“产量-性状”组合水平对北部冬麦区小麦品种进行综合评价和分类研究,为其他作物和地区的类似研究提供了参考。展开更多
文摘To study the biopharmaceutics characteristics of paris saponin Ⅶ(PSⅦ). The solubility of PSⅦ was evaluated by measurement of the equilibrium solubility in different solvents and media. The permeability of PSⅦ was evaluated by measuring the oil/water partition coefficient(lgP_(app)) and determining the apparent permeability coefficient(PC_(app)) on a mono-layer Caco-2 cell model. The effects of p-glycoprotein and multidrug resistance related protein 2 on PSⅦ transport in mono-layer Caco-2 cell model were further investigated. Finally, the small intestinal absorption of PSⅦ was investigated in rat. In solvents of different pH, the equilibrium solubility of PSⅦ was quite low, and the dose number of PSⅦ was larger than 1. The lgP_(app) of PSⅦ was less than 0. The apparent permeability coefficient [PC_(app)(AP-BL)] of PSⅦ in mono-layer Caco-2 cell model was less than 14.96 × 10^(-6) cm·s^(-1), and the efflux ratio of PSⅦ in mono-layer Caco-2 cell model was less than 1. The transport rate of PSⅦ in mono-layer Caco-2 cell model was not affected by the inhibitors of p-glycoprotein and multidrug resistance related protein 2. After oral administration, PSⅦ could be detected in rat intestinal contents, but could not be detected in the small intestinal mucosa. PSⅦ showed low solubility and permeability,which would result in low oral bioavailability in clinic. PSⅦ belonged to Class IV compound in biopharmaceutics classification system.
文摘北部冬麦区是我国重要的小麦主产区之一,对该麦区历年国审小麦品种进行回溯分析有助于小麦品种资源的合理利用。本研究基于产量与熟期、穗数、穗粒数、千粒重、容重、品质指数、抗病指数和抗寒指数等性状的组合,采用品种-产量×性状组合(GYT,genotype by yield×trait)双标图方法对2003-2023年期间北部冬麦区47个国审小麦品种进行了综合分析和分类评价。结果表明,47个国审小麦品种可划分为4个特征显著的品种类型。其中,Ⅰ型品种综合表现优秀,在产量与早熟性、抗病性、抗寒性、千粒重和容重等性状组合上表现突出,在产量与穗数、穗粒数和品质指数组合上表现优良,在生产上推广应用价值最高,主要包括京麦179、京农16和津麦3118等8个品种。Ⅱ型品种综合表现优良,在产量与品质指数、穗数组合上表现突出,在产量与抗病指数、抗寒指数组合上表现稍差,在生产上推广应用价值较高,但应注意生产安全,主要包括京麦202、京农19和轮选158等13个品种。Ⅲ型品种的产量与抗病和抗寒指数组合最好,但在其余性状组合上表现差,综合生产应用价值有限,可作为抗性亲本。Ⅳ型品种综合表现较差,可选择单性状表现优良的品种作为育种亲本应用。根据各品种在GYT双标图ATA轴上的投影位置,筛选出综合表现优良的京麦179、京农16、津麦3118、京麦189、京麦202、京花12号、京农19、轮选158和中麦623等品种。本研究采用GYT双标图分析方法基于“产量-性状”组合水平对北部冬麦区小麦品种进行综合评价和分类研究,为其他作物和地区的类似研究提供了参考。
