用β-escin穿孔膜片技术研究粉防己碱对豚鼠心室肌钙电流的作用

目的 用β escin穿孔膜片 (PPR)技术研究粉防己碱 (tetrandrine ,Tet)对ICa ,L 和ICa ,T的作用。方法 用PPR和全细胞记录 (WCR)模式记录心室肌细胞ICa ,L和ICa,T。结果 2 5 μmol·L- 1 β escin可在心室肌细胞形成稳定的PPR模式 ,用此模式记录的ICa ,L衰减明显减慢。在PPR模式下 1～ 30 0 μmol·L- 1 Tet浓度依赖性地减小ICa ,L幅值。 3,30和30 0 μmol·L- 1 Tet对ICa ,T的抑制率分别为 (16± 5 ) % ,(40± 7) %和 (75± 11) %。结论 用 2 5 μmol·L- 1 β escin在豚鼠心室肌细胞能得到较稳定的PPR模式 ,在此模式下Tet浓度依赖性地抑制ICa ,L和ICa ,T。

A New Triterpenoid Oligoglycoside Escin IVe from the Seeds ofAesculus Chinensis

A new triterpenoid saponin named escin IV e was isolated from the seeds of Aesculus chinensis. Its structure was established as 28-tigloylprotoaescigenin-3 beta-O- [beta-D-glucopyranosyl (1-2)] [beta-D-glucopyranosyl (1-4)] -beta-D-glucopyranosiduronic acid.

β-escin reverses multidrug resistance through inhibition of the GSK3β/β-catenin pathway in cholangiocarcinoma

AIM: To develop a safe and effective agent for cholangiocarcinoma(CCA) chemotherapy. METHODS: A drug combination experiment was conducted to determine the effects of β-escin in c o m b i n a t i o n w i t h c h e m o t h e ra p y o n C C A c e l l s. 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay was performed to determine the effects of β-escin and common chemotherapeutics on the proliferation of human CCA cells(QBC939, Sk-Ch A-1, and MZ-Ch A-1). Immunocytochemistry was used to detect the expression of P-glycoprotein(P-gp) protein. Luciferase reporter assay was used to detect the activation of the Wnt/β-catenin pathway. The protein levels of P-gp, p S9-GSK3β, p T216-GSK3β, GSK3β, β-catenin, and p-β-catenin were further confirmed by western blotting.RESULTS: The drug sensitivity of QBC939 and QBC939/5-fluorouracil(5-FU) cells to 5-FU, vincristine sulfate(VCR), or mitomycin C was significantly enhanced by β-escin compared with either agent alone(P < 0.05). In addition, the combination of β-escin(20 μmol/L) with 5-FU and VCR was synergic with a combination index < 1. Further investigation found that the m RNA and protein expression of P-gp was downregulated by β-escin. Moreover, β-escin induced GSK3β phosphorylation at Tyr-216 and dephosphorylation at Ser-9, resulting in phosphorylation and degradation of β-catenin. Interestingly, activation of the GSK3β/β-catenin pathway induced by Wnt3 a resulted in upregulation of P-gp, which was effectively abolished by β-escin, indicating that β-escin down-regulated P-gp expression in a GSK3β-dependent manner.CONCLUSION: β-escin was a potent reverser of P-gpdependent multidrug resistance, with said effect likely being achieved via inhibition of the GSK3β/β-catenin pathway and thus suggesting a promising strategy of developing combination drugs for CCA.

Escin enhances anti-rheumatoid arthritis effects of low dose glucocorticoids through up-regulation of glucocorticoid receptor

OBJECTIVE To investigate the anti-rheumatoid arthritis(RA)effect of Escin combined with low dose of GCs(dexameth⁃asone,Dex)and its underlying mechanism.METHODS Adjuvant-induced rheumatoid arthritis rats and LPS-injured RAW 264.7 were used to investigate the anti-RA effects of Escin combined with low dose Dex in vivo and in vitro.In vivo experiment:rats were randomly divided into model group(AIA),dexamethasone high dose(Dex,0.2 mg·kg^-1)group,dexamethasone low dose(Dex,0.05 mg·kg^-1)group,Escin 10 mg·kg^-1 group,Dex 0.05+Escin group,10 rats in each group,another 10 were used as normal control group.The vehicle and the corresponding drug were administered intragastrically(ig)daily for 14 d.In vitro experiment:LPS was used to stimulate RAW 264.7 macrophages for inflammatory models,which were divided into control group,LPS group,Dex with high dose(50 nmol·L^-1)group,and Dex with low dose(12.5 nmol·L^-1)group.In the Escin 10μmol·L^-1 group and the Dex+Escin(12.5 nmol·L^-1+10μmol·L^-1)group,the corresponding drugs were added to each well.After 2 h,LPS was added to induce inflammation.RESULTS Escin combined with low dose Dex significantly decreased arthritic index,serum IL-6 and TNF-α,improved paw swelling,and ameliorated the joint pathology immune organ pathology significantly.Gene chip results revealed that Nr3c1(GR)altered significantly.And that GR activation by Escin and low dose Dex was confirmed both in vivo and in vitro.Furthermore,Escin combined with low dose Dex also significant increase GR mRNA expression.However,when suppression of GR by its specific inhibitor,the anti-RA effect of Escin combined with low dose Dex was abolished.CONCLUSION Escin combined with Dex reduces the dose of Dex,and exerts significant anti-RA effects,which could also reduce the adverse effects of Dex.This combination might be attributed to GR activation.This study might provide a new combination drugs for the treatment of RA.

Progress in anti-inflammatory effects of escin

The fraction of horse chestnut seeds was named escins,which mainly consists of A,B,C,and D escin.Accumulating evidence suggests that escin exerts potent anti-inflammatory and anti-edematous effects.The effects of escin on inflammation and edema have been confirmed in various models.In a study in 1961,intravenous administration of escin was found to reduce acute edema in a rat paw.In the same study,escin was found to inhibit the increase in vascular permeability induced by egg white injection.Escin dose-dependently reduced the capillary permeability in chloroform-induced local inflammation in the abdominal skin surface of rabbits.The anti-inflammatory and anti-edematous effects of external use of escin were studied in carrageenan-induced paw edema and histamine-induced capillary permeability in rats.Escin gel decreased the contents of PGE2,TNF-α,and IL^(-1)β,and reduced the raw edema and capillary permeability.The carrageenan-induced paw edema and pleuritis in bilaterally adrenalectomized rats were used to investigate the anti-inflammatory effects of escin and glucocorticoid alone or combined.Co-administration of escin with cortisone significantly reduced the volume of exudates and the number of white blood cells of exudates.The findings suggest escin can synergize with glucocorticoids to enhance their anti-inflammatory effect.The anti-inflammatory effect of escin was investigated in carrageenan-induced paw edema and acetic acid-induced capillary permeability in mice.Escin showed an anti-inflammatory effect,which is similar to that seen with dexamethasone treatment.However,escin showed a longer duration of the anti-inflammatory response than that of dexamethasone.Furthermore,escin had no significant effects on spleen index,thymus index,proliferative capacity of splenocytes,lymphocyte count,and phagocytic rate.The findings suggest that escin is a potent anti-inflammatory drug with long-lasting anti-inflammatory effects without any immunosuppressive effects.Traditionally the mechanism of anti-inflammatory effect of escin is supposed to be relative to release of PGF2αand corticosterone.The early studies showed that escin might promote the release of PGF2αand affect the pituitary adrenal system,stimulate the release of adrenocorticotropic hormone(ACTH)and glucocorticoid,which may explain its anti-inflammatory and anti-edema effects.Escin has glucocorticoid-like anti-inflammatory effect.However,escin did not exhibit an anti-inflammatory effect in low dose.Combination of suboptimal concentrations of escin with corticosterone inhibited the release of inflammatory factors including NO,TNF-αand IL^(-1)βin the LPS-stimulated macrophage cells.Previous studies demonstrate that escin combined with glucocorticoid produced synergistic anti-inflammatory effects.The potential synergistic mechanisms may be associated with the property which escin regulates the glucocorticoid receptor(GR)signaling pathway.Escin can upregulate the expression of GR,promote the combination of glucocorticoid and GR,then promote the activated GR transfer into the nucleus.Activated GR will inhibit the activation of NF-κB directly,thus further inhibiting the expression of TNF-αand IL^(-1)βand other inflammatory factors.Escin could inhibit 11β-HSD2 but not 11β-HSD1,thus decrease the metabolism of glucocorticoid.Escin and glucocorticoids have similar chemical structures.This indicate that one of the anti-inflammatory mechanisms of escin may be due to its stimulating GR by binding to it.Eacin might be a partial agonist of GR.A good many of researches have demonstrated the anti-inflammatory properties of escin,and shed light on the underlying mechanisms by which escin exerts these effects.Escin,as an oral or intravenous formulation,or a topical gel,inhibits inflammation,producing measurable improvements in edema and acute lung injury.Further clinical studies of escin are needed to demonstrate these properties in larger patient populations.

Escin may exert a synergistic anti-inflammatory effect with glucocorticoids

Escin is a natural mixture of triterpenoid as- ponin isolated from the seed of the horse chestnut and demonstrates anti-oedematous and anti-inflammatory effects. As yet, the pre-cise mechanisms by which escin exerts its anti- inflammatory effects remain unclear. The data from current studies indicate that the anti-in-flammatory properties of escin were attributed to its ability to reduce the adhesiveness of neu-trophils and the associated release of inflam-matory mediators;its ability to decrease hista-minic and serotoninergic activities;its ability to inhibit phospholipase A2;its ability to decrease nuclear factor-κ B activation and down-regulate the expression of tumor necrosis factor-α. All these effects are similar to glucocorticoids. Mo- reover, escin depends on adrenal glands to ex-ert its anti-inflammatory effects. Also, our recent research showed that the serum corticosterone level in mice did not increase after a 7-day in-travenous injection of escin. The results sup-port the hypothesis that escin may exert a syn-ergistic anti-inflammatory effect with glucocor-ticoids. Confirming this hypothesis will play a role in elucidating the anti-inflammatory mech- anisms of escin.

七叶皂苷对结直肠癌细胞增殖、侵袭的作用及机制研究

目的:探究七叶皂苷对氧化三甲胺(TMAO)诱导的结直肠癌细胞株增殖及迁移侵袭的影响,并探讨其作用机制。方法:取结直肠癌HCT116细胞系,分为对照组、TMAO组、观察组3组,并分别进行处理。对照组不做处理,TMAO组仅使用100μmol/L TMAO诱导,观察组使用同剂量TMAO诱导后再进行10μmol/L七叶皂苷治疗处理。随后使用四甲基偶氮唑盐比色(MTT)法、划痕愈合实验及细胞迁移侵袭试验技术(Transwell)实验分别检测细胞的增殖、迁移及侵袭行为,并使用蛋白质印迹(Western Blotting)实验检测SRC、pBTK、pTRIO蛋白表达情况。结果:TMAO诱导可增强HCT116增殖及迁移侵袭能力,并显著上调SRC-BTK-TRIO通路相关基因的mRNA水平,而七叶皂苷干预能抑制癌细胞增殖(P<0.01)并降低其迁移(P<0.001)、侵袭(P<0.01)能力,同时下调SRC(P<0.05)、BTK(P<0.01)、TRIO(P<0.05)蛋白的表达。结论:七叶皂苷可通过下调SRC-BTK-TRIO通路显著抑制HCT116细胞增殖及迁移侵袭能力。

Anti-inflammatory effect of external use of escin on cutaneous inflammation: possible involvement of glucocorticoids receptor

Escin, as an internally applied anti-inflammatory agent, has been widely used in the treatment of inflammation and edema resulting from trauma or operation in the clinic. However, the effect of its external use on cutaneous inflammation and edema remains unexplored. In the present study, the anti-inflammatory and anti-edematous effects of external use of escin were studied in carrageenan-induced paw edema and histamine-induced capillary permeability in rats, paraxylene-induced ear swelling in mice, and cotton pellet-induced granuloma in rats. Effects of external use of escin gel on prostaglandin E2(PGE2), tumor necrosis factor-α(TNF-α), and interleukin-1β(IL-1β) were determined by ELISA. The anti-inflammatory mechanism was explored by detecting the expression of glucocorticoid receptor(GR) with Western blotting and Real-time PCR analyses, with further exploration of nuclear factor-κB(NF-κB), p38 mitogen-activated protein kinase(P38 MAPK) and activator protein-1(AP-1) expressions. We demonstrated that external use of escin showed significant anti-inflammatory effects on acute and chronic inflammation in different animal models and its anti-inflammatory effects might be related to down-regulation of PGE2, TNF-α, and IL-1β. The results also showed that escin exerted its anti-inflammatory effects by promoting the expression of GR, with the possible mechanism being inhibition of the expressions of GR-related signaling molecules such as NF-κB and AP-1.

Studies on Triterpenoid Saponins of Seeds of Aesculus chinensis Bunge var. chekiangensis (Hu et Fang) Fang

Aim To study the saponin constituents of the seeds of Aesculus chinensis Bunge var. chekiangensis (Hu et Fang) Fang. Methods Compounds were separated and purified by macroreticular resin column chromatography and high-performance liquid chromatography. Their structures were elucidated by spectroscopic and hydrolysis analysis. Results Six compounds were isolated from the 70% ethanolic extracts. They were identified as escins IVc, IVd, Ia, Ib, isoescins Ia and Ib, respectively. Conclusion The above compounds were obtained from the seeds of Aesculus chinensis Bunge var.chekiangensis (Hu et Fang) Fang for the first time.

七叶皂苷对大鼠三叉神经痛的改善作用

目的:研究七叶皂苷(escin)对大鼠三叉神经痛(trigeminal neuralgia,TN)的治疗作用,并探讨其潜在的作用机制。方法:通过对大鼠行眶下神经慢性缩窄性损伤(chronic constriction injury of the infraorbital nerve,CCI-ION)的方式来构建大鼠TN模型。将大鼠随机分为假手术组(sham组)、CCI-ION组、CCI-ION+卡马西平(carbamazepine,CBZ;42 mg/kg)组和escin低、中、高剂量(6、12、24 mg/kg)组。手术当天开始灌胃给药,连续治疗14 d,sham组和CCI-ION组给予等剂量0.9%氯化钠溶液;使用Von Frey纤维细丝检测大鼠术侧口面部机械痛阈;实时定量聚合酶链反应(real-time quantitative polymerase chain reaction,RT-qPCR)检测三叉神经节(trigeminal ganglion,TG)中肿瘤坏死因子-α(tumor necrosis factor-α,TNF-α)、白细胞介素-1β(interleukin-1β,IL-1β)、Toll样受体-4(Toll like receptor-4,TLR-4)和核因子-κB(nuclear factor kappa-B,NF-κB)mRNA的表达变化;苏木精-伊红(hematoxylin and eosin,HE)染色观察TG的病理变化。结果:行为学结果显示,与sham组相比,CCI-ION组大鼠的机械疼痛阈值显著下降(P<0.01);与CCI-ION组相比,各给药组大鼠机械疼痛阈值在给药第3天后逐渐提高,至第14天时,所有给药组机械疼痛阈值均显著增高(P<0.01)。RT-qPCR结果显示,与sham组相比,CCI-ION组TNF-α、IL-1β、TLR-4及NF-κB m RNA的表达显著增加(P<0.01);与CCI-ION组相比,各给药组TNF-α、IL-1β、TLR-4及NF-κB mRNA的表达显著降低(P<0.05)。组织病理学结果显示,与sham组相比,CCI-ION组观察到TG出现明显的炎性细胞浸润、施万细胞数增多及脱髓鞘的变化;与CCI-ION组相比,各给药组光学显微镜下可见TG炎症情况有不同程度的减轻。结论:Escin对CCI-ION诱导的TN有一定的改善作用,其机制可能与促炎细胞因子释放的下调有关,并可能通过TLR4/NF-κB信号通路发挥作用。

七叶皂苷影响急性心肌梗死心肌损伤的机制研究

目的探讨七叶皂苷影响急性心肌梗死(AMI)心肌损伤的机制。方法60只雄性SD大鼠随机分为4组,假手术组、AMI组、AMI+低剂量七叶皂苷组(LE组)和AMI+高剂量七叶皂苷组(HE组),最终每组6只。建立AMI大鼠模型,其中假手术组只开胸不结扎。LE组和HE组在造模前分别2.10 mg/kg七叶皂苷灌胃7 d。建立大鼠心肌细胞H9C2株低氧损伤模型,设立对照组、低氧组、七叶皂苷组和模拟物组。除对照组外,其余各组均低氧(1%O_(2))培养,七叶皂苷组加入10μmol/L七叶皂苷,模拟物组加入10μmol/L七叶皂苷和20 nmol/L R-140-5P模拟物。通过超声检测各组大鼠心功能,采用TTC染色法检测心脏梗死面积,采用Western blot法检测大鼠心脏组织和H9C2细胞中B淋巴细胞瘤-2(Bcl-2)和B淋巴细胞瘤-2相关X蛋白(Bax)表达水平,采用qRT-PCR法检测miR-140-5p的mRNA表达水平。采用细胞增殖和毒性检测(CCK-8)法检测H9C2细胞活力,采用原位末端标记法(TUNEL)检测细胞凋亡水平。结果与假手术组比较,AMI组大鼠心脏左心室舒张末期内径(LVEDd)和左心室收缩末期内径(LVESd)均显著增大(均P<0.05),射血分数(EF)和左室短轴缩短率(FS)均显著降低(均P<0.05),同时Bax表达水平显著升高,Bcl-2表达水平均显著降低,心脏梗死面积增大,miR-140-5p表达水平显著增加(均P<0.05);与AMI组比较,LE组和HE组LVEDd和LVESd显著减小,EF和FS显著增加,Bax表达水平显著降低,Bcl-2表达水平显著升高,心脏梗死面积减小,miR-140-5p表达水平显著降低(均P<0.05),且HE组变化更显著(均P<0.05)。与对照组比较,低氧组miR-140-5p表达水平显著升高,细胞活力显著降低,Bax表达水平显著升高,Bcl-2表达水平显著降低,同时细胞凋亡水平升高(均P<0.05);与低氧组比较,七叶皂苷组细胞损伤得到明显改善(P<0.05);然而,miR-140-5p模拟物显著逆转了七叶皂苷对低氧心肌细胞损伤的改善作用(P<0.05)。结论七叶皂苷通过调控miR-140-5p表达改善AMI心肌损伤。

Three New Triterpenoid Saponins from the Seeds of Aesculus chinensis

Three new triterpenoid saponins, escins IVg (1), IVh (2) and VIb (3) were isolatedfrom the seeds of Aesculus chinensis along with two known saponins, escin IIIa (4) anddesacylescin I (5). Their structures were elucidated by spectroscopic analysis and chemicalhydrolysis.

β-七叶皂苷钠对大鼠脑出血后脑水肿及脑内精氨酸加压素含量的影响

目的 :观察 β-七叶皂苷钠治疗前后大鼠脑出血各脑区与垂体精氨酸加压素 ( AVP)含量的变化。方法 :采用立体定向于大鼠尾壳核注射胶原酶建立脑出血动物模型 ,以干湿重法测定脑组织含水量 ,放射免疫法测定 AVP含量。结果 :与正常组及对照组相比 ,脑出血组大鼠在各脑区脑组织含水量显著升高的同时 ,AVP含量也显著升高 ,而且下丘脑与垂体的 AVP含量也显著升高 ;β-七叶皂苷钠治疗后大鼠脑组织含水量显著降低 ,顶叶皮质、下丘脑及垂体 AVP含量也显著降低。各项结果均有显著性差异 ( P<0 .0 5 ,P<0 .0 1)。结论 :内源性 AVP可能参与脑出血后脑水肿的病理过程 ,β-七叶皂苷钠抗脑水肿的药理作用机制中可能有 AVP参与。

七叶树皂苷-Ia的人肠内细菌生物转化产物及其抗肿瘤活性研究

目的 :探讨人肠内细菌和短乳杆菌粗酶转化七叶树皂苷 Ia ,阐明转化产物结构 ,研究其抗肿瘤活性。方法 :采用人肠内细菌和短乳杆菌粗酶分别与七叶树皂苷 Ia共温孵方法 ,通过色谱技术分离、纯化转化产物 ,应用波谱技术确定转化产物结构。结果 :七叶树皂苷 Ia可由人肠内细菌和短乳杆菌粗酶转化产生异七叶树皂苷Ia、去酰基七叶树皂苷I、2 1 β O 巴豆酰基原七叶树皂苷元和原七叶树皂苷元。去酰基七叶树皂苷I对小鼠肉瘤S 1 80、肝癌和肺癌细胞的生长具有抑制作用。结论 :七叶树皂苷 Ia是“前药” ,人肠内细菌和短乳杆菌粗酶能够转化七叶树皂苷 Ia;转化产物去酰基七叶树皂苷I有抗肿瘤活性 。

七叶皂苷钠对大鼠脑缺血损伤中神经细胞凋亡的影响

目的 :观测七叶皂苷钠对大鼠大脑中动脉闭塞缺血半球梗死面积及凋亡细胞数目的影响。 方法 :选用健康雄性 SD大鼠 ,以头端烫圆的 4 - 0尼龙线由左侧颈总动脉插入 ,阻塞左侧大脑中动脉 ,建立缺血 2 h再灌注 2 2 h动物模型。再灌注即刻腹腔内注射七叶皂苷钠 (5 m g/ kg)为治疗组 ,注射生理盐水 (10μl/ g)为对照组。对视交叉部冠状脑组织块行 TTC染色 ,测定其吻端梗死面积百分比 ;对邻近脑组织块行原位末端转移酶标记 (TU NEL ) ,计数缺血半球凋亡细胞数目。 结果 :治疗组和对照组大鼠脑梗死面积分别为 (8.15± 5 .0 ) %和 (2 2 .14± 7.7) % (P <0 .0 1) ;细胞凋亡数目分别为 70± 2 3和 2 2 5± 78(P<0 .0 1)。结论 :再灌注即刻腹腔内注射七叶皂苷钠对大鼠短暂性、局灶性脑缺血具有保护作用 ;

急性脑梗死后白细胞介素6与神经功能缺损评分的相关性及β-七叶皂甙钠的治疗作用

目的观察急性脑梗死后血清白细胞介素6(IL-6)与神经功能缺损程度评分的动态变化,探讨IL-6对急性脑梗死后神经功能恢复的影响及β-七叶皂甙钠治疗急性脑梗死的作用机制。方法选择急性脑梗死患者63例,随机分为对照组30例和治疗组33例,对照组予以脑梗死常规治疗,治疗组在常规治疗基础上加用β-七叶皂甙钠,在脑梗死后1、5、14d进行血清IL-6测定和美国国立卫生研究院卒中量表(NIHSS)评分。另选取健康体检者30例为正常组,清晨测定血清IL-6。结果治疗组和对照组患者脑梗死后1、5、14dIL-6水平较正常组明显升高,差异有统计学意义(P<0.01);治疗组脑梗死后14d血清IL-6水平明显低于对照组[(13.33±2.82ng/L)vs(15.25±4.65)ng/L,P<0.05];对照组和治疗组脑梗死后14d神经功能缺损评分较1、5d明显改善,差异有统计学意义(P<0.01);治疗组脑梗死后14d神经功能缺损评分较对照组明显降低[(9.03±2.28)分vs(10.38±2.30)分,P<0.05];脑梗死患者血清IL-6水平与神经功能缺损评分呈正相关(r=0.888,P<0.01)。结论急性脑梗死后血清IL-6水平与神经功能缺损密切相关,β-七叶皂甙钠可能通过抑制血清IL-6的增高而改善神经功能。

HPLC法测定娑罗子中4种皂苷类成分的含量

目的:建立娑罗子药材中4种皂苷类成分的高效液相色谱测定方法。方法:色谱柱为Platinum EPS C18(4.6 mm×250mm,5μm),流动相为乙腈-水-冰醋酸(30:70:1),检测波长为210 nm,流速为1.0 mL·min-1。结果:七叶皂苷Ⅰa、七叶皂苷Ⅰb、异七叶皂苷Ⅰa和异七叶皂苷Ⅰb的线性范围分别为2.06-20.56μg,2.25-22.46μg,2.21-22.12μg,2.01-20.04μg;加样回收率分别为97.57%,96.74%,97.56%,97.50%,RSD分别为1.54%,1.18%,1.14%,1.26%(n=5)。结论:方法简便、准确,可用于娑罗子药材的质量控制。

β-七叶皂甙钠对大鼠脑出血后血SOD、NO、TNF-α的影响

目的:观察β-七叶皂甙钠对大鼠脑出血后血中超氧化物歧化酶(SOD)、一氧化氮(NO)、肿瘤坏死因子-α(TNF-α)的影响,探讨其治疗作用的机制。方法:将实验大鼠随机分为假手术1、2组;模型1、2组;七叶皂甙1、2组,采用胶原酶诱导大鼠形成脑出血模型,术后2h七叶皂甙1、2组腹腔注射β-七叶皂甙钠(2.8mg/kg),另4组注射生理盐水,分别在3、7d后取血,测定血SOD、NO、TNF-α含量。结果:与假手术组比较,模型组血SOD、NO、TNF含量明显下降和升高(P<0.01),与模型组比较,七叶皂甙组血SOD、NO、TNF含量明显升高和下降(P<0.01)。结论:β-七叶皂甙钠对脑出血后神经细胞损伤具有保护作用,其机制可能与抗自由基抑制NO和TNF毒性作用有关。

七叶树种子皂苷含量及其组分的产地变异分析

Total contents and components of escin were studied in seeds of Aesculus chinensis, A. chinensis var. chekiangensis and A. wilsonii collected from 8 origins. Results showed that total escin content ranged from 71.43 mg·g to 112.69 mg·g ,with the highest in origin of Mabian, Sichuan Province and the lowest in origin of Kangxian, Gansu Province. It was suggested that escin content was correlated with geological zone to a certain extent. A.wilsonii was richer than that of Aesculus chinensis in escin content.The proportion of 4 types of escin varied dramatically among different origins. Component A in Mabian and Cangwang origin from Sichuan Province, Kangxian origin from Gansu Province, Mianxian origin from Shanxi Province and Xixia origin from Henan Province reached 35%～41% of total escin that was much higher than that of other components, while components D was below 15% that was only 1/3 of component A. Sum of Component A and C was nearly equal in Enshi, Hubei Province and Sangzhi, Hunan Province origins, which accounted for 58% of the total content. Lin’an origins from Zhejiang Province only got (17.17%) of component A while holding much higher proportion of component D. Statistical analysis also approved that the proportion of escin was correlated to geological zone.

加速溶剂提取法提取娑罗子中的七叶皂苷

为了探讨快速溶剂提取法(ASE)提取娑罗子中七叶皂苷的可行性,并比较该方法与回流提取法和超声提取法的优越性。本文以娑罗子中的四种七叶皂苷的提取率为指标,以高效液相色谱法(HPLC)为检测方法,用单因素考察法对加速溶剂提取法从娑罗子中提取七叶皂苷的工艺条件进行优化。结果通过实验我们优选出加速溶剂提取法从娑罗子中提取七叶皂苷的最佳条件,即提取溶剂为70%甲醇,提取温度为100℃,静态提取时间为7 min,提取次数为1次。由此可以定论加速溶剂提取法可以快速、高效地提取娑罗子中的七叶皂苷类化合物。