大蒜油β-环糊精包合物的稳定性考察

 目的:考察大蒜油β-CD包合物的稳定性。方法:以大蒜油为测定指标，分别对包合物和混合物进行强光照射、高温、高湿、挥发性试验及恒温加速实验。结果:在光、热、湿等因素影响下，包合物中大蒜油含量没有明显变 化，而混合物中大蒜油含量均明显下降，说明大蒜油包合后增加了对光、热、湿的稳定性;挥发性试验结果，包合物的热失重比混合物小，说明包合物降低了大蒜油的挥发性。结论:大蒜油β-CD包合物具有一定的杭光照性、热稳定性和湿稳定性，其稳定性明显优于单纯大蒜油。     

大蒜油联合益生菌的抗菌活性研究

目的:联合应用大蒜油与益生菌,研究其共同抗菌活性。方法:采用最小抑菌浓度(MIC)、最低杀菌浓度(MBC)、抑菌圈直径测量法,测定联合抗菌指标。结果:大蒜油单体的抗菌活性明显,联合应用大蒜油与益生菌的抗菌活性无明显变化。结论:大蒜油与益生菌的抗菌作用机理存在差异,抗菌效果不同于单体抗菌效果的简单加和,联合使用未能达到明显的辅助增强效应。     

大蒜渣ACEI活性肽的制备及其稳定性研究

目的以蒜渣为原料,对制备ACEI(血管紧张素转化酶抑制剂)活性肽的工艺及酶解产物的稳定性进行研究。方法以水解液的抑制活性为试验指标,从9种蛋白酶中筛选出4种较佳蛋白酶单独或联合水解蒜渣。结果蛋白酶1单独水解效果较好。通过单因素和正交试验得出最佳水解条件:加酶量(E/S)6%、底物浓度8%、pH 7、50℃、3 h,在上述条件下酶解产物对ACE的抑制率为88.81%。考察了大蒜渣ACEI活性肽的热稳定性、耐酸碱性和抗肠道酶降解能力,结果表明,该活性肽具有良好的耐高温性能;在酸性条件下活性下降较快,当pH≥8.3时活性稳定;在模拟的胃肠道环境中具有良好的抗胃蛋白酶和胰蛋白酶裂解的能力。结论大蒜渣ACEI活性肽经口服或者静脉注射后很可能具有良好的降血压效果。     

Role of oil extract of garlic (Allium sativum Linn.) on intestinal transference of calcium and its possible correlation with preservation of skeletal health in an ovariectomized rat model of osteoporosis

The present study was undertaken to examine the effects of an oil extract of garlic on the in vivo intestinal transference of calcium, and also to verify its role in maintaining the bone mineral content and bone tensile strength in an ovariectomized rat model of osteoporosis. The results suggest that, in this experimental model, oil extract of garlic promotes intestinal transference of calcium by modulating the activities of both intestinal alkaline phosphatase and Ca(2+) activated ATPase. Also the observed low bone mineral content and low bone tensile strength in these rats were significantly restored by garlic oil supplementation. Further, garlic oil supplementation was able to revive partially the bilateral ovariectomy-induced decrease in the serum estrogen titer. The serum parathyroid hormone level, however, was found unaltered in these rats. The garlic oil supplemented partial recovery in serum estrogen titer in bilaterally ovariectomized rat was found to be persistently associated with enhanced calcium transference and better preservation of bone mineral content. The results of this study propose that the phytoestrogenic efficacy of an oil extract of garlic prevents ovarian hormone deficiency induced bone mineral loss possibly by promoting intestinal transference of calcium through the partial revival of the serum estrogen titer.     

静脉注射用大蒜油亚微乳的制备

 目的制备静脉注射用大蒜油亚微乳。方法采用高压匀质法制备大蒜油亚微乳。以离心稳定性参数、外观、药物含量作为评价指标,通过正交设计实验对处方进行了优化。在最佳处方的基础上,考察了工艺因素对乳剂的影响。结果在优化处方及工艺条件下,所制备的大蒜油亚微乳稳定性良好,平均粒径为(150.4±14.6)nm。结论该处方及工艺可行,制得的大蒜油亚微乳可达到静脉注射使用的目的。     

Prevention of bone loss by oil extract of garlic (Allium sativum Linn.) in an ovariectomized rat model of osteoporosis

The effects of oil extract of garlic (Allium sativum Linn.) on different primary and secondary osteoporotic marker changes were tested in an ovariectomized rat model of osteoporosis. Experiments were performed on three different rat models: sham-operated control, ovariectomized and ovariectomized supplemented with garlic oil. In ovariectomized group, there has been a significant increase in different relative organ weights compared to sham-operated control, while the uterine weight was found to be decreased. Supplementation with oil extract of garlic could effectively reverse these changes. Also low bone densities that developed in the ovariectomized group were significantly recovered in the garlic oil supplemented group. In our study, the development of high rate of bone turnover and osteoporosis in the ovariectomized animals were confirmed by significant alteration of serum alkaline phosphatase activity, serum tartrate resistant acid phosphatase activity, urinary excretion of calcium, phosphate, hydroxyproline and urinary calcium to creatinine ratio, when compared with the sham-operated control group. Garlic oil extract supplementation, apart from its unique influence in lowering blood cholesterol, could also prevent ovariectomy-induced rise in all the above-mentioned marker changes. The results of this study emphasize that oil extract of garlic possibly has a positive role in suppressing ovariectomy-induced bone resorption.     

Effect of garlic oil on ethanol induced gastric ulcers in rats

Garlic oil was evaluated for gastroprotective activity against ethanol induced ulcers. Reactive oxygen species are involved in the pathogenesis of these ulcers. The possible involvement of garlic oil in restraining the oxidation process produced in gastric tissue was also investigated. The ulcer index, lipid peroxidation and antioxidant enzyme activity (GPx, catalase, SOD) were determined. Pretreatment with garlic oil in doses of 0.25 and 0.5 mg/kg, 30 min before administration of ethanol (1 mL of 100%) caused a decrease in ulcer index and lipid peroxidation and ameliorated the decrease in antioxidant enzyme levels caused by ethanol. The result suggests that garlic oil possesses antioxidant properties and provides protection against ethanol induced gastric injury.     

胶体磨法包合大蒜油及包合物稳定性考察

目的考察胶体磨法包合大蒜油及包合物的稳定性。方法采用胶体磨法、气相色谱法,以大蒜素含量为考察指标,对大蒜油β-环糊精包合物进行强光照射、高温和高湿试验。结果在光、热、湿等因素影响下,包合物中大蒜素含量没有明显变化,而单纯大蒜油混合物的含量明显下降。结论大蒜油β-环糊精包合物具有较好的抗光照性、热稳定性和湿稳定性,其稳定性明显优于单纯大蒜油混合物。     

大蒜油固体脂质纳米粒中二硫化物和三硫化物在大鼠体内的组织分布

目的：考察大蒜油固体脂质纳米粒(GO-SLN)中二硫化物(DADS)和三硫化物(DATS)在大鼠体内的组织分布。方法：建立了测定大鼠体内大蒜油中二硫化物(DADS)和三硫化物(DATS)的气相-电子捕获法，色谱条件：恒温110 ℃，检测器300 ℃，汽化室180 ℃，载气N2(纯度>99.999％)，流速 1.0 mL·min-1，分流比1∶10；尾吹60 mL·min-1；进样量1 μL。并测定大鼠颈静脉注射GO-SLN和GO注射液后组织中的药物浓度。结果：此色谱条件下各组织的标准曲线、精密度等实验结果表明，该方法适于分析大鼠体内大蒜油中DADS和DATS含量。与GO注射液相比，GO-SLN在大鼠体内的分布特性有不同程度的改变，GO-SLN在各组织中分布均相对较高。结论：SLN能一定程度上提高药物的被动靶向性并延长药物在各组织中的作用时间。     

Role of peritoneal macrophages and lymphocytes in the development of hypogonadal osteoporosis in an ovariectomized rat model: possible phytoestrogenic efficacy of oil extract of garlic to preserve skeletal health

This study was to examine whether skeletal health deterioration in the hypogonadal situation is a consequence of an alteration in the functional status of peripheral mononuclear cells and its amelioration, if any, by an oil extract of garlic. The results suggest that hypogonadism-induced oxidative stress of peritoneal macrophages and lymphocytes could be reduced by supplementation with an oil extract of garlic. However, estrogen deficiency did not cause any significant change in DNA fragmentation of peritoneal macrophages. The hypogonadism-induced increase in the serum levels of IL-6 and TNF-alpha were significantly reduced by an oil extract of garlic. Further, such supplementation could revive the hypogonadism-induced decrease in serum estrogen titer and counter-balance the increase in bone turnover as determined by low bone tensile strength and alterations in bone related biochemical variables such as urinary calcium, hydroxyproline, calcium to creatinine ratio and serum tartrate resistant acid phosphatase activity (TRAP). The garlic oil supplemented partial recovery of the serum estrogen titer in hypogonadal rats was found to be persistently associated with reduced oxidative stress of peritoneal macrophages and lymphocytes, reduced serum interleukins and better preservation of bone mass. This study proposes that the hypogonadism-induced bone loss has a direct correlation with the functional status of lymphocytes and peritoneal macrophages, and garlic can prevent this.     

大蒜油固体脂质纳米粒大鼠体内药动学的研究

 目的研究大蒜油的血药浓度测定方法及其在大鼠体内的药动学。方法12只健康大鼠,单剂量(含大蒜油每只10mg)颈静脉注射给大蒜油固体脂质纳米粒和大蒜油注射液,在设计的时间点从颈静脉取血,采用气相电子捕获法同时测定大蒜油中指标性成分二烯丙基三硫化合物和二烯丙基二硫化合物在全血中药物浓度,药动学参数采用DAS2.0程序进行统计矩处理。结果大鼠颈静脉注射给药后,大蒜油的指标性成分DATS首先快速转化成DADS,然后继续降解;大蒜油固体脂质纳米粒中的DATS和DADS的MRT_0-t分别为7.3和16.9min,ρ_max分别为3574.3和21416.7μg·L^-1;大蒜油注射液的DATS和DADS的MRT_0-t分别为19.4和19.5,ρ_max分别为3692.8和9335.8μg·L^-1。t_max均为1min。结论本方法简单、快速,灵敏度和准确度较高,适合药动学研究。静注给药后大蒜油在大鼠体内表现为快速分布和消除,而大蒜油固体脂质纳米粒因被动靶向的关系消除比大蒜油注射液快。     

Effects of garlic oil on postmenopausal osteoporosis using ovariectomized rats: comparison with the effects of lovastatin and 17beta-estradiol

The purpose of this study was to examine the antiosteoporosis effects of garlic oil in an ovariectomized (Ovx) rat model of osteoporosis and to compare its efficacy with lovastatin (a synthetic hypocholesterolemic drug) and 17beta-estradiol (a potent antiosteoporotic agent). Animals were divided into five groups: sham-operated control, ovariectomized, ovariectomized supplemented with lovastatin, ovariectomized supplemented with garlic oil and ovariectomized supplemented with 17beta-estradiol. In our study, the development of a high rate of bone turnover and osteoporosis in the ovariectomized animals were confirmed by significant alterations of serum alkaline phosphatase activity, serum tartrate-resistant acid phosphatase activity, urinary excretion of calcium, phosphate, hydroxyproline and urinary calcium to creatinine ratio, when compared with the sham-operated control group. Supplementation of these animals with either garlic oil or lovastatin or 17beta-estradiol, in addition to their hypocholesterolemic effect, could counterbalance all these changes. The results revealed that all three compounds significantly protected the hypogonadal bone loss as reflected by higher bone densities and higher bone mineral contents than the ovariectomized group of animals. The results emphasize that, like 17beta-estradiol, the hypocholesterolemic compounds garlic oil and lovastatin are also effective in suppressing bone loss owing to estrogen deficiency and their efficacy in the order of lower to higher is garlic < lovastatin < 17beta-estradiol.     

Effects of acute and subacute garlic supplement administration on serum total antioxidant capacity and lipid parameters in healthy volunteers

Garlic has long been used for medicinal purposes. It has been shown that different forms of garlic have significant antioxidant effects. The strong flavor, odor and unwanted gastrointestinal side effects of fresh garlic has rendered the use of commercial garlic supplements as a preferable option. To investigate the effects of garlic supplementation on serum total antioxidant capacity and lipid parameters, 17 healthy volunteers were administered four standardized commercial garlic tablets every day for 30 days. Blood samples were taken at day 1 (before the first administration of tablets [control] and at 3 h after the administration of tablets), 15 and 30 days, respectively. Total antioxidant capacity (TAC), total cholesterol, low density lipoprotein cholesterol (LDL cholesterol), high density lipoprotein cholesterol (HDL cholesterol) and triglyceride (TG) were measured in sera. Serum TAC was increased significantly at 30 days compared with 15 days, 3 h and control. There was also a significant increase in serum TAC at 15 days compared with 3 h and control. Total cholesterol, LDL cholesterol, HDL cholesterol and TG were not found to be significantly different between control, 3 h, 15 and 30 days. These data suggest that garlic, used as a dietary supplementation, may be beneficial in increasing the antioxidant capacity of the body. Copyright © 2009 John Wiley & Sons, Ltd.     

大蒜油诱发瘤灶内中性粒细胞和巨噬细胞的超微结构观察

给腹水型及实体型荷瘤小鼠的瘤灶注射大蒜油后,瘤灶内的中性粒细胞、巨噬细胞和淋巴细胞数量增多,以中性粒细胞和巨噬细胞的数量最为显著。可观察到多个中性粒细胞或巨噬细胞包围一个肿瘤细胞,并有突起顶入肿瘤细胞的现象。实验结果表明,大蒜油可能具有增强中性粒细胞及巨噬细胞的抗肿瘤作用。     

Flow cytometric analysis of the garlic oil effect on DNA content of cancer cell cycle]

Flow cytometry (FCM) is a new technique developed in the recent decade. This technique may measure DNA content of 5000 cells per second and trace the dynamic changes in cell proliferation cycle and offer a hint for designing clinical treatment protocol, monitor prognosis and elucidate the mechanisms of antitumor drugs. The authors previous studies showed significant effect of garlic oil on prolongation of life expectancy and inhibition of tumor growth in mice. Using FCM the authors analysed the effect of garlic oil on cell cycle in S180 tumor cells, 2-6 hrs after single administration or multiple administration the cell number in S phase rapidly decreased, in G1 phase increased. This suggests garlic oil may blockade cells to progress from G1 phase to S phase and result in accumulation of cells in G1 phase and directly inhibit the synthesis of DNA and the cell cycle. Theoretical basis for clinical application was offered and some aspects of antitumor mechanism of garlic oil were elucidated.     

欣脉胶囊降血脂活性部位的筛选及其指纹图谱归属分析

目的：从欣脉胶囊中筛选出降血脂的主要活性部位,建立活性部位的HPLC指纹图谱,研究其与组方药材指纹图谱色谱峰的相关性。方法：利用溶剂萃取法对欣脉胶囊的不同极性部位进行分离制备,采用腹腔注射75%蛋黄乳液的方式快速建立小鼠高血脂症模型,筛选出欣脉胶囊的活性部位;建立欣脉胶囊活性部位及各药材的指纹图谱,以色谱峰保留时间为考察指标,对复方活性部位指纹图谱色谱峰归属进行分析。结果：乙酸乙酯部位和大蒜挥发油部位的降脂作用显著（P<0.01）;建立了欣脉胶囊活性部位的HPLC指纹图谱,标示出28个特征峰,对特征峰进行了归属分析,确定了27个特征峰的药材归属。结论：欣脉胶囊降血脂的主要活性部位为乙酸乙酯部位和大蒜挥发油部位,所建立的指纹图谱测定方法能较好地判别活性部位主要色谱峰与药材化学组分间的相关性,为欣脉胶囊的药效物质基础及质量标准提升提供参考。     

大蒜3个有效部位配伍对3种人胃癌细胞的杀伤作用

目的:观察大蒜3个有效部位组合物对3种人胃癌细胞的杀伤作用,筛选有效部位组合物最佳配伍比例.方法:以大蒜3个有效部位(大蒜油、大蒜总多糖、大蒜总皂苷)为研究对象,选用L16(45)正交表设计分组、给药,以胃癌细胞代谢MTT活力(抑瘤百分率)作为考察指标,采用SPSS软件对实验数据进行处理.结果:大蒜3个有效部位对MKN45细胞杀伤作用的主次顺序为大蒜油(1#)＞大蒜总多糖(2#)＞大蒜总皂苷(5#),其最佳配比为1 #∶2#∶5#=1∶20∶10.大蒜3个有效部位对AGS细胞抑制率影响无明显差别,其最佳配比为1#∶2#∶5#=1∶13.3∶3.3.大蒜总皂苷对人胃癌HGC-27细胞抑制率的影响显著(P＜0.01),影响的主次顺序为大蒜总皂苷＞大蒜油＞大蒜总多糖,其最佳配比为1#∶2#∶5#=1∶200∶50.结论:3种人胃癌细胞对大蒜3个有效部位组合物的杀伤作用的敏感性不同,3个有效部位组合对3种人胃癌细胞杀伤作用的最佳配比浓度亦不相同.     

气滞胃痛颗粒促胃肠动力有效物质组分协同关系及作用机制研究

目的：研究气滞胃痛颗粒组方中促胃肠动力有效组分协同关系及作用机制。方法：将大鼠随机分成16 组,分别灌胃给予不同配伍组合促胃肠动力有效组分,应用传统半固体糊碳末推进法观察大鼠用药后的胃肠动力变化;测定胃肠组织中NO、cGMP 及Ca2+含量变化。结果：气滞胃痛颗粒中促胃肠动力有效组分以枳壳黄酮和香附黄酮作用显著（P<0.01）,香附挥发油和柠檬烯作用明显（P<0.05）,两两交互作用表明枳壳黄酮与柠檬烯合用对胃肠动力具有显著促进作用,其次分别为枳壳黄酮与香附挥发油、香附黄酮与挥发油、柠檬烯与香附挥发油合用;各有效组分均能使胃肠组织中NO、cGMP 含量降低,Ca2+含量升高。结论：本研究确定了气滞胃痛颗粒各组分与促胃肠动力活性的相关程度及相互间协同作用,其作用机制与胃肠组织中NO、cGMP 含量降低,Ca2+含量升高有关,为进一步研究促胃肠动力药效质量控制、配伍及谱效关系提供理论依据。     

Effect of garlic (Allium sativum) on lipid peroxidation in experimental myocardial infarction in rats

The present study was conducted to elucidate the antioxidant role of garlic oil in isoproterenol (IPL)-induced myocardial infarction in rats. In myocardial necrosis induced by isoproterenol, a significant increase in serum iron content with a significant decrease in plasma iron binding capacity, ceruloplasmin activity and glutathione (GSH) level were observed. There was also a significant increase in lipid peroxides levels on isoproterenol administration. Activities of antioxidant enzymes like superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPX), glutathione-S-transferase (GST) and glutathione reductase (GRD) were decreased significantly in heart with isoproterenol-induced myocardial necrosis. Garlic oil produced a marked reversal of these metabolic changes related to myocardial infarction induced by isoproterenol. In conclusion, garlic oil exerts its effects by modulating lipid peroxidation and enhancing antioxidant and detoxifying enzyme systems.     

两个不同产地大蒜挥发油成分的比较研究

目的 利用色谱联用技术(GC—MS)对陕西兴平基地大蒜和湖南普通食用大蒜中的挥发油成分进行测定，比较挥发油成分的异同。方法 采用质谱相关色谱理论，比较了这两个不同地区大蒜挥发油成分；同时基于直观推导式演进特征投影法(HELP)对产生的二维气相色谱／质谱数据进行解析，根据得到的色谱保留时间和纯质谱在质谱库中进行相似性检索，实现对组份的鉴定。结果 鉴定并用总体积积分法定量计算了19个挥发油成分。质谱相关色谱理论和HELP方法得到了相同的定性信息。结论 采用化学计量学的方法，成功地实现了两个地区大蒜挥发油成分的比较研究，得到了两者整体组份信息的异同，为药理药效的比较研究奠定了基础。