HPLC测定乳疾宁胶囊中丹酚酸B的含量

目的 建立乳疾宁胶囊中丹酚酸B的含量测定方法。方法色谱柱：Agilent ZORBAXE clispse XDB—C18柱（4．6mm×150mm,5μm）,流动相：甲醇-乙腈-甲酸-水（28：8：1：63）,检测波长：286nm。结果丹酚酸B在0．9～2．7μg内呈良好线性关系,r=0．9997,加样回收率平均为100．1％（n=9,RSD=2．2％）。结论本法灵敏度高、操作简便、结果准确,可用于乳疾宁胶囊中丹酚酸B的含量测定。     

HPLC测定心可宁胶囊中丹酚酸B的含量

目的：建立测定心可宁胶囊中丹酚酸B的HPLC含量测定方法。方法：色谱柱：kromasil^TM C18（150nm×4．6mm,5μm）;流动相：乙腈-甲醇-甲酸-水（10：30：1：59）,流速：1．0ml·min^-1,检测波长：286nm,柱温：30℃。结果：丹酚酸B在0．54—4．02μg线性关系良好,平均回收率为99．7％,RSD为0．12％（n=5）。结论：方法简便、准确、重复性好,可作为心可宁胶囊中丹酚酸B的含量测定。     

HPLC法测定首乌丹参滴丸中丹酚酸B含量

目的：拟定首乌丹参滴丸产品丹酚酸B的含量测定方法。方法：采用高效液相色谱法对供试品中的丹酚酸B进行含量测定。选用十八烷基硅烷键合硅胶为填充剂色谱柱（4．6mm×250mm,5μm）;以乙腈为流动相A,1％甲酸水溶液为流动相B,按规定进行梯度洗脱;检测波长为286nm;柱温为25℃;进样量为10μl;理论塔板数按丹酚酸B峰计算应不低于2000,分离度大于1．0。结果：被测物丹酚酸B的含量在0．0956—0．9560μg的范围内有良好的线性关系,平均回收率101．0％,精密度、重复性良好。结论：建立了首乌丹参滴丸产品中丹酚酸B的含量测定方法,该方法稳定可靠,操作简便,分析快速,可用于该产品中丹酚酸B的含量测定。     

高效液相色谱法测定脉管复康胶囊中丹酚酸B含量

目的建立测定脉管复康胶囊中丹酚酸B含量的方法。方法采用反相高效液相色谱法测定方中丹酚酸B的含量。色谱柱为Dikma C18柱（250mm×4．6mm,5μm）,流动相为乙腈-甲醇-甲酸-水（10：30：1：59）,流速为1．0mL／min,柱温为30℃,检测波长为286mm,进样量为10μL。结果丹酚酸B质量浓度在28．08～140．4μg／mL范围内与峰面积呈良好线性关系,r=0．9999（n=5）,平均回收率为100．12％,RSD=1．99％（n=9）。结论所建立的方法简便、准确,专属性强,重现性好,可作为脉管复康胶囊的质量控制方法。     

HPLC法测定精制冠心颗粒中丹酚酸B的含量

目的：建立HPLC法测定精制冠心颗粒中丹酚酸B含量的方法。方法：采用VP-ODS C18柱（150mm×4．6mm,5um）色谱柱;以乙腈-甲醇-甲酸-水（10：30：1：59）为流动相等度洗脱;检测波长286nm。结果：丹酚酸B在10．4～104．4ug·ml^-1的浓度范围内呈良好的线性关系（r=0．9991）,平均加样回收率为99．55％,RSD0．96％。结论：本法简便、灵敏、准确、可用于测定精制冠心颗粒中丹酚酸B的含量。     

复方血栓通系列品种中丹酚酸B的通用检测方法研究

目的：统一复方血栓通颗粒、片、滴丸和胶囊中丹酚酸B的含量测定方法。方法：采用高效液相色谱法,使用Thermo Syncronis（5μm,250mm×4．6mm）色谱柱,流动相为乙腈：甲醇：甲酸：水（10：25：1：64）,流速为1．0ml·min^-1,检测波长286nm。结果：丹酚酸B的量在0．0541-5．4108μg范围内与峰面积线性关系良好,r=0．9999;精密度、重复性、稳定性及加样回收率结果均能满足分析要求。结论：该方法简单可行,为复方血栓通品种中丹酚酸B含量测定方法的统一提供可靠的依据。     

高效液相色谱法测定冠脉宁片中丹酚酸B含量

目的用高效液相色谱（HPLC）法测定冠脉宁片中丹酚酸B的含量。方法采用Agilent C18色谱柱（250mm×4．6mm,5μm）,流动相为甲醇-乙腈-甲酸-水（27：9：1：63）,流速为1．0mL／min,检测波长为286nm。结果丹酚酸B进样量在0．784～7．020μg（r=0．99999）范围内与峰面积线性关系良好,平均加样回收率为99．40％,RSD=1．75％（n=6）。结论HPLC法简便、准确、灵敏,重现性好,可用于冠脉宁片中丹酚酸B含量的测定。     

丹参补益丸中丹酚酸B含量测定

目的：建立丹参补益丸中丹酚酸B的含量测定方法。方法：采用高效液相色谱法（HPLC）,色谱柱：Kromasil C18（250min×4．6mm,5μm）;流动相：乙腈-0．4％磷酸溶液（80：20）;流速：1．0ml·min^-1;检测波长：286nm。结果：丹酚酸B浓度在4．305-25．95μ范围内线性关系良好,γ=0．9999,回收率为96．99％,RSD％=1．19％（n=6）。结论：所建立的方法简便、准确、专属性强,可有效地控制制剂的质量。     

HPLC法测定丹黄颗粒中丹酚酸B的含量

目的建立测定丹黄颗粒中丹酚酸B的含量的方法。以控制丹黄颗粒的质量．保证药效。方法采用高效液相色谱法对颗粒中的丹酚酸B进行含量测定。结果丹酚酸B在0．102--15．30μg范围内呈良好的线性关系（r=0．9999），平均加样回收率为100．0％（RSD=1．55％）。结论所建方法可准确进行定量测定,干扰少,重复性好。     

HPLC法测定安神益智胶囊中丹酚酸B的含量

目的：建立高效液相色谱法测定安神益智胶囊中丹酚酸B的含量。方法：色谱柱为HypersilODS2C18柱（150mm×4．6mm,5μm）,流动相为甲醇：水：甲酸（40：60：1）,检测波长：286nm;流速：1．0ml·min-1;进样量：10μl。结果：丹酚酸B在7．75—77．51μg·ml-1的浓度范围内线性关系良好,r=0．9996,平均回收率为98．17％,RSD为1．79％（n：6）。结论：本法简便、准确,灵敏度高,重复性好,可作为控制安神益智胶囊质量的方法。     

大蒜抗氧化活性成分的测定及薄层生物自显影技术分析

目的测定和分析大蒜抗氧化活性成分。方法利用1,1-二苯基苦基苯肼法(DPPH·)测定大蒜灭酶体系和蒜酶激活体系抗氧化活性成分,利用大蒜氨基酸展开系统(正丁醇-冰乙酸-水)、大蒜辣素展开系统(甲苯-乙酸乙酯)和大蒜多糖展开系统(冰乙酸-氯仿-水)对大蒜抗氧化活性成分进行分析。结果大蒜灭酶体系中氨基酸、大蒜多糖和蒜酶激活体系中的大蒜含硫化合物的半数抑制质量浓度(IC50)分别为0.058,0.170和0.068mg·mL-1。大蒜灭酶体系中的蒜氨酸和蒜酶激活体系中的大蒜辣素有抗氧化活性,其他抗氧化活性成分有待进一步确定。结论大蒜中氨基酸和含硫化合物有一定的抗氧化活性,具有研究价值。     

Prophylactic action of garlic on the histological and histochemical patterns of hepatic and gastric tissues in rats injected with a snake venom

The present study aimed to examine the prophylactic action of oral administration of two doses of garlic on the histological and histochemical patterns of the gastric and hepatic tissues in rats envenomed with cobra snake. The study included the following groups: Group I contained control rats orally administered distilled water for ten days. Group II included rats orally administered daily for ten days with the equivalent therapeutic dose of garlic to rat (18 mg/kg body weight). Group III included rats orally administered daily for ten days with double the equivalent therapeutic dose of garlic to rat (36 mg/kg body weight). Group IV contained rats intramuscularly (i.m.) injected with 1/2 LD50 of cobra venom (0.0125 microg venom/gm body weight) and dissected after 6 hr from injection. Groups V and VI contained rats daily administered with the previous two doses of garlic for ten days, respectively, followed by a single i.m. injection of the above dose of cobra venom after 24 hr from the last garlic application. Rats of these two groups were dissected after 6 hr from venom injection. Administration of the therapeutic dose of garlic induced slight cytoplasmic granulation in some hepatic cells. However, administration of double the therapeutic dose caused swelling, necrosis, and damage of the gastric glandular epithelia together with signs of erosion, exfoliation, and necrosis of the surface mucosal cells. It also induced swelling and coalescence of the hepatic cells, loss of the normal arrangement of the hepatic cords, and hypertrophy of Kupffer cells. Injection with cobra venom caused loss of the normal characteristic appearance of the gastric glands and the epithelial lining cells of the gastric folds and the appearance of numerous inflammatory cells in the lamina properia. It also induced the occurrence of highly swollen hepatic cells, hepatic cellular necrosis and damage, as well as activated Kupffer cells. Nevertheless, pretreatment with the therapeutic dose of garlic for ten days induced a prophylactic activity against the pathogenic effects of the venom in both tissues, which appeared more or less normal except for very minor abnormalities. However, application of double the therapeutic dose of garlic for the same duration did not induce any prophylactic activity. Histochemically, slight alterations were noticed in the polysaccharide, protein, and nucleic acid contents of the gastric mucosa and the hepatic tissues due to administration of the therapeutic doses of garlic. However, severe depletions of these components were recorded in both tissues due to administration of double the therapeutic doses of garlic or injection of cobravenom or the application of both of them together. On the contrary, minor changes were noticed in the histochemical patterns of both tissues in rats pretreated with the therapeutic doses of garlic prior to venom application. It could be concluded that oral administration of the therapeutic dose of garlic for ten days has no serious side effects on gastric and hepatic tissues and could be used as a prophylactic tool against cobra snake envenomation.     

Identification and HPLC quantitation of the sulfides and dialk(en)yl thiosulfinates in commercial garlic products.

The content of dialk(en)yl thiosulfinates, including allicin, and their degradation products has been determined by high performance liquid chromatography (HPLC), using the respective determined extinction coefficients, for a number of commercially available garlic products. Quantitation has been achieved for the thiosulfinates; diallyl, methyl allyl, and diethyl mono-, di-, tri-, tetra-, penta-, and hexasulfides; the vinyldithiins; and (E)- and (Z)-ajoene. The thiosulfinates were found to be released only from garlic cloves and garlic powder products. The vinyldithiins and ajoenes were found only in products containing garlic macerated in vegetable oil. The diallyl, methyl allyl, and dimethyl sulfide series were the exclusive constituents found in products containing the oil of steam-distilled garlic. Typical steam-distilled garlic oil products contained about the same amount of total sulfur compounds as total thiosulfinates released from freshly homogenized garlic cloves; however, oil-macerated products contained only 20% of that amount, while garlic powder products varied from 0 to 100%. Products containing garlic powder suspended in a a gel or garlic aged in aqueous alcohol did not contain detectable amounts of these non-ionic sulfur compounds. A comparison of several brands of each type of garlic product revealed a large range in content (4-fold for oil-macerates and 33-fold for steam-distilled garlic oils), indicating the importance of analysis before garlic products are used for clinical investigations or commercial distribution.     

Black garlic: A critical review of its production,bioactivity, and application

Black garlic is obtained from fresh garlic (Allium sativum L.) that has been fermented for a period of time at a controlled high temperature (60–90°C) under controlled high humidity (80–90%). When compared with fresh garlic, black garlic does not release a strong offensive flavor owing to the reduced content of allicin. Enhanced bioactivity of black garlic compared with that of fresh garlic is attributed to its changes in physicochemical properties. Studies concerning the fundamental findings of black garlic, such as its production, bioactivity, and applications, have thus been conducted. Several types of black garlic products are also available in the market with a fair selling volume. In this article, we summarize the current knowledge of changes in the components, bioactivity, production, and applications of black garlic, as well as the proposed future prospects on their possible applications as a functional food product.     

Garlic [Allium sativum]: a review of its potential use as an anti-cancer agent

Garlic [Allium sativum] is among the oldest of all cultivated plants. It has been used as a medicinal agent for thousands of years. It is a remarkable plant, which has multiple beneficial effects such as antimicrobial, antithrombotic, hypolipidemic, antiarthritic, hypoglycemic and antitumor activity. In this review, we will discuss particularly the largely preclinical use of this agent in the treatment and prevention of cancer. A number of studies have demonstrated the chemopreventive activity of garlic by using different garlic preparations including fresh garlic extract, aged garlic, garlic oil and a number of organosulfur compounds derived from garlic. The chemopreventive activity has been attributed to the presence of organosulfur compounds in garlic. How this is achieved is not fully understood, but several modes of action have been proposed. These include its effect on drug metabolizing enzymes, antioxidant properties and tumor growth inhibition. Most of these studies were carried out in the animal models. Also, recent research has focused on the antimutagenic activity of garlic. Recently, it has been observed that aged garlic extract, but not the fresh garlic extract, exhibited radical scavenging activity. The two major compounds in aged garlic, S-allylcysteine and S-allylmercapto-L-cysteine, had the highest radical scavenging activity. In addition, some organosulfur compounds derived from garlic, including S-allylcysteine, have been found to retard the growth of chemically induced and transplantable tumors in several animal models. Therefore, the consumption of garlic may provide some kind of protection from cancer development.     

Effect of diallyl trisulfide-rich garlic oil on blood coagulation and plasma activity of anticoagulation factors in rats.

Diallyl trisulfide (DAT)-rich garlic oil was fed to Sprague-Dawley rats and the effects of this DAT-rich garlic oil on bleeding time, clotting time and anticoagulation factors were examined. Garlic oil supplement at 5 or 50mg garlic oil/kg bodyweight significantly prolonged bleeding time and thrombin time, and enhanced anticoagulation factor activity, such as antithrombin III and protein C (P<0.05). These results suggested that the anticoagulant action of DAT-rich garlic oil was due to inhibition and/or inactivation of thrombin. In addition, DAT-rich garlic oil benefits blood anticoagulation factors, which might further prevent the development of thrombus formation. However, the intake of garlic oil at high dose significantly increased plasma fibrinogen concentration (P<0.05), and affected the levels of several hematological parameters such as erythrocyte count, hemoglobin and platelets (P<0.05). The adverse effect of high doses of garlic oil might further influence the hemostatic balance. Therefore, the concentration of DAT-rich garlic oil should be carefully considered in its application. Supplementation of garlic oil at 5mg/kg bodyweight has anticoagulation effect in this animal study.     

大蒜油联合顺铂诱导人腺样囊性癌细胞株ACC-M凋亡

目的探讨大蒜油联合顺铂对人腺样囊性癌细胞株ACC—M细胞增殖、细胞周期及凋亡的影响。方法采用不同浓度大蒜油、顺铂、大蒜油联合顺铂分别处理人腺样囊性癌细胞株ACC—M细胞24、48、72h后,MTT法检测肿瘤细胞体外增殖抑制情况;选取2、8、32μg/mL的大蒜油、顺铂、大蒜油联合顺铂处理肿瘤细胞4、8h后,流式细胞术分析肿瘤细胞周期分布和凋亡率。结果8、16、32μg／mL大蒜油及2、4、8、16、32μg／mL顺铂、大蒜油联合顺铂作用24、韶、72h对ACC-M细胞均有明显抑制作用,随浓度及时间增加,抑制率呈上升趋势。联合组用药肿瘤细胞抑制率明显高于单一用药组。流式细胞术结果显示,不同浓度的大蒜油、顺铂、大蒜油联合顺铂作用能使ACC．M细胞发生G2/M期阻滞,诱导细胞凋亡,随浓度增高及作用时间延长,周期分布越明显,凋亡率增高,联合组用药细胞周期阻滞和促凋亡作用明显强于单一用药组,差异有统计学意义（P〈0．05）。结论不同浓度的大蒜油、顺铂、大蒜油联合顺铂均能有效抑制ACC-M细胞生长．阻滞细胞于G2／M期并诱导肿瘤细胞凋亡,大蒜油联合顺铂对ACC—M细胞生长抑制作用明显强于大蒜油、顺铂单独应用。     

Garlic flavonoids and organosulfur compounds: impact on the hepatic pharmacokinetics of saquinavir and darunavir

The therapeutic efficacy of saquinavir and darunavir is affected by the presence of xenobiotics (such as garlic compounds) capable of modifying transporter-enzyme interplay. To ascertain the mechanism of interactions between antiretroviral drugs and garlic supplements and to identify the garlic constituents responsible, the hepatic pharmacokinetics of two antiretroviral drugs was investigated in the presence of garlic phytochemicals and aged garlic extract. For this purpose, rat liver slices and isolated rat hepatocytes were used. Aged garlic extract significantly inhibited saquinavir efflux from rat hepatocytes, while the efflux of darunavir significantly increased. Phytochemicals inducing distribution changes of saquinavir and darunavir were most probably flavonoids and lipophilic organosulfur compounds, respectively. All tested phytochemicals (except S-allyl L-cysteine) and aged garlic extract inhibited CYP3A4 metabolism of both drugs and modulated hepatic distribution of the corresponding saquinavir and darunavir metabolites. The competition between saquinavir and garlic constituent(s) for the same binding site on the efflux transporter and the positive cooperative effect between darunavir and garlic phytochemical(s), which bind to separate binding places on transporter, are the most probable mechanisms explaining the plasma profile changes, which could occur in vivo during concomitant consumption of antiretrovirals and garlic supplements.     

Comparative pharmacological investigations of Allium ursinum and Allium sativum.

Extracts of wild garlic (Allium ursinum) and garlic (A. sativum) with defined chemical compositions were investigated for their in vitro inhibitory potential on 5-lipoxygenase (LO), cyclooxygenase (CO), thrombocyte aggregation (TA), and angiotensin I-converting enzyme (ACE). The inhibition rates as IC50 values of both extracts for 5-LO, CO, and TA showed a good correlation with the %-content of the major S-containing compounds (thiosulfinates and ajoenes) of the various extracts. In the 5-LO and CO test the garlic extracts are slightly superior to the wild garlic extracts whereas, in the TA test, no differences could be found. In the ACE test the water extract of the leaves of wild garlic containing glutamyl-peptides showed the highest inhibitory activity followed by that of the garlic leaf and the bulbs of both drugs. The comparative studies underline the usefulness of wild garlic as a substitute of garlic.     

大蒜油亚微乳的安全性及体外抗真菌作用

目的考察大蒜油亚微乳的安全性及体外抗真菌作用。方法急性毒性试验为小鼠尾静脉注射给药,测定LD50;采兔血配制成体积分数为2%的红细胞混悬液,进行溶血试验;新西兰大耳兔左、右耳缘静脉分别静滴大蒜油亚微乳或大蒜油注射液和5%的葡萄糖注射液,观察药物对血管的刺激性;用沙氏培养基以倍比稀释法测定大蒜油亚微乳、大蒜油注射液、氟康唑注射液对白色念珠菌、热带念珠菌、新型隐球菌、烟曲菌的最小抑菌浓度(MIC)。结果大蒜油亚微乳的LD50为282.0 mg.kg-1,大蒜油注射液为167.2 mg.kg-1;大蒜油亚微乳无溶血作用,无血管刺激性;大蒜油亚微乳对白色念珠菌、热带念珠菌、新型隐球菌及烟曲菌的最小抑菌浓度(MIC)分别为50、25、502、5 mg.L-1,大蒜油注射液对上述4种菌的MIC分别为50、50、100、25 mg.L-1。结论大蒜油亚微乳的LD50是大蒜油注射液的1.7倍,安全性好于大蒜油注射液;大蒜油制成亚微乳后仍具有较强的抗真菌作用。