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通脉方是由葛根、丹参和川芎3味药按质量1∶1∶1组成的复方。该文研究通脉方中异黄酮类化合物大豆苷元、芒柄花素、5-羟基芒柄花苷、芒柄花苷、大豆苷、3’-甲氧基葛根素、染料木苷、葛根素、芒柄花素-8-C-β-D-呋喃芹糖基-(1→6)-O-β-D-吡喃葡萄糖苷、芒柄花素-7-O-β-D-呋喃芹糖基-(1→6)-O-β-D-吡喃葡萄糖苷、澳白檀苷、葛花宁、大豆苷元-7,4’-二-O-β-D-吡喃葡萄糖苷、泰国野葛根素、3’-羟基葛根素、3’-甲氧基大豆苷、芒柄花素-8-C-β-D-吡喃木糖基-(1→6)-O-β-D-吡喃葡萄糖苷、染料木素-8-C-β-D-呋喃芹糖基-(1→6)-O-β-D-吡喃葡萄糖苷、染料木素-7-O-β-D-呋喃芹糖基-(1→6)-O-β-D-吡喃葡萄糖苷、3’-羟基泰国野葛根素、6″-O-β-D-木糖基葛根素、鹰嘴豆芽素A-8-C-β-D-呋喃芹糖基-(1→6)-O-β-D-吡喃葡萄糖苷、3’-甲氧基大豆苷元-7,4’-二-O-β-D-吡喃葡萄糖苷、大豆苷元-7-O-β-D-吡喃葡萄糖基-(1→4)-O-β-D-吡喃葡萄糖苷和大豆苷元-7-O-α-D-吡喃葡萄糖基-(1→4)-O-β-D-吡喃葡萄糖苷在肠的吸收转运。采用人源肠Caco-2细胞单层模型,研究通脉方中上述25个异黄酮类化合物由绒毛面(AP侧)到基底面(BL侧)或从BL侧到AP侧2个方向的转运过程。应用高效液相色谱法分离、紫外检测法对化合物进行定量分析,计算表观渗透系数(P_(app)),并与阳性对照药普萘洛尔和阿替洛尔比较。大豆苷元和芒柄花素由AP侧到BL侧的P_(app)分别为(2.55±0.03)×10~(-5),(3.06±0.01)×10~(-5)cm·s~(-1);由BL侧到AP侧的P_(app)分别为(2.62±0)×10~(-5),(2.65±0.11)×10~(-5)cm·s~(-1)。与本试验中在Caco-2细胞单层模型上呈良好吸收的阳性对照药普萘洛尔的P_(app)(2.66±0.32)×10~(-5)cm·s~(-1)和呈难吸收的阳性对照药阿替洛尔的P_(app)(2.34±0.10)×10-7cm·s~(-1)比较,大豆苷元和芒柄花素与普萘洛尔在同一数量级;其他化合物与阿替洛尔在同一数量级。大豆苷元和芒柄花素的P_(app AP→BL)/P_(app BL→AP)分别为0.97,1.15。可以预测,大豆苷元和芒柄花素可以通过小肠上皮细胞被动吸收进入体内,属于良好吸收的化合物;其他化合物属于吸收不良的化合物。5-羟基芒柄花苷、染料木苷、澳白檀苷、葛花宁和染料木素-7-O-β-D-呋喃芹糖基-(1→6)-O-β-D-吡喃葡萄糖苷的P_(app AP→BL)/P_(app BL→AP)分别为0.18,0.28,0.45,0.38,0.49,推测它们在Caco-2细胞单层模型中的转运可能存在外流机制。
Tongmai side by Pueraria, Salvia and Chuanxiong 3 herbs by mass 1: 1: 1 composition. In this paper, we study the effects of Tongmai Fang, a compound of daidzein, daidzein, 5-hydroxymyristin, manganoside, daidzin, 3’-methoxy puerarin, genistein, O-β-D-glucopyranoside, formononetine-7-O-β-D-glucopyranoside, Furanosyl- (1 → 6) -O-β-D-glucopyranoside, albuterol, Gehuanen, daidzein -7,4’-di-O-β-D-glucopyranose Glucosyl- (1 → 6) -O-glucosyltransferase, puerarin, thaumatoxylin, 3’-hydroxy puerarin, β-D-glucopyranoside, genistein -8-C-β-D-furanosyl- (1 → 6) -O-β-D-glucopyranoside, -β-D-furanosyl- (1 → 6) -O-β-D-glucopyranoside, 3’-hydroxy thaumatan, 6 "-O-β-D-xylosylpuerarin , Biochanin A-8-C-β-D-furanosyl- (1 → 6) -O-β-D-glucopyranoside, ’-di-O-β-D-glucopyranoside, daidzein -7-O-β-D-glucopyranosyl- (1 → 4) -O-β-D-glucopyranoside and soybean Aglycone-7-O-α-D-glucopyranoside (1 → 4) -O-β-D-glucopyranoside in intestine.Using the human intestinal Caco-2 cell monolayer model, we studied the above 25 isoflavones From the villus surface (AP side) to the basal side (BL side) or from the BL side to the AP side of the two directions of transport.Application of high performance liquid chromatography, UV detection of compounds were quantitative analysis of apparent permeability coefficient (P_ (app)), and compared with the positive control drug propranolol and atenolol.The P app of daidzein and tomanonetin from AP side to BL side were (2.55 ± 0.03) × The average values of P app from BL to AP were (2.62 ± 0) × 10 ~ (-5), (3.06 ± 0.01) × 10 ~ (-5) cm · s -1 -5), (2.65 ± 0.11) × 10 -5 cm · s -1, respectively.Compared with propranolol, which is a good positive control in the Caco-2 cell monolayer model P (app) was (2.66 ± 0.32) × 10 ~ (-5) cm · s ~ (-1), and Pare (app) was 2.34 ± 0.10 × 10-7cm · S ~ (-1), the daidzein and the formononetin were in the same order of magnitude as those of propranolol; the other compounds were in the same order of magnitude as atenolol.Application of AP_ (app AP → BL) / P_ (app BL → AP) were 0.97 and 1.15 respectively. It can be predicted that daidzein and formononetin can passively enter the body through intestinal epithelial cells and are well-absorbed compounds; other compounds belong to malabsorptive compounds. O-β-D-furanosyl- (1 → 6) -O-β-D-D-glucosyltransferase P_ (app AP → BL) / P_ (app BL → AP) of glucopyranoside were 0.18,0.28,0.45,0.38,0.49, respectively. It is speculated that they may have efflux mechanism in Caco-2 cell monolayers.