60Co辐照对睾丸酮/乳酸-乙醇酸共聚物微球理化特性及体外释放的影响

目的 :睾丸酮 (T) /乳酸 -乙醇酸共聚物 (PLGA)微球6 0 Co辐照灭菌可行性研究。方法 :T/PLGA微球在6 0 Co源下 ,以 2 5kGy的剂量进行辐照 ,对微球辐照前后主药T、载体PLGA的理化特性和微球体外释药速率的变化进行比较 ,考察6 0 Co辐照对T/PLGA微球理化特性及药物体外释放的影响。结果 :6 0 Co辐照引起PLGA分子量一定程度的下降 ,但对T/PLGA微球的理化特性及体外释药速率没有影响。结论 :初步的可行性研究表明T/PLGA微球可用6 0 Co辐照灭菌     

60Co辐照对乌金丸中益母草碱的影响

目的 考察不同剂量60 Co辐照(0、2、6和10 kGy)对乌金丸有效成分益母草碱含量的影响.方法 采用梯度高效液相色谱(HPLC)法检测益母草碱的含量,应用SPSS软件对试验结果进行统计分析.结果 益母草碱在0、2、6和10 kGy的辐照处理后含量分别为0.138、0.135、0.139和0.137 mg·g-1.统计学分析发现,经不同剂量辐照灭菌后乌金丸中益母草碱的含量与无辐照相比无显著性差异(P>0.05).结论 60 Co辐照灭菌对乌金丸中益母草碱的含量无影响.     

采用特征图谱分析~(60)Co-γ射线辐照灭菌技术对丁香质量的影响

目的评价~(60)Co-γ射线辐照灭菌技术对丁香药材质量的影响。方法建立10批丁香的GC特征图谱,比较辐照前后(5或10kGy辐照10h)丁香样品特征图谱色谱峰的变化,并利用GC-MS法对共有峰成分进行确认,利用SPSS 17.0对共有峰面积进行方差分析及配对t检验。结果 GC特征图谱分析显示,10kGy辐照剂量辐照10h对4个共有峰面积无影响。结论辐照剂量在10kGy以下对丁香药材质量无影响。     

~(60)Co—γ射线辐照中药材杀虫灭菌效果及主要有效成分变化的研究

本文为应用~(60)Co—γ射线辐照边条红参(Radix Ginseng)、当归(Radix AnselicaeSinensis)、槟榔(Semen Arecae)等21种中药材杀虫、灭菌效果及其主要有效成分变化的研究。结果表明,辐照杀虫剂量范围为1.5～2.3kGy;灭菌剂量范围为3.8～7.6kGy;以3.7～20.6kGy剂量辐照边条红参、当归头、槟榔、其主要有效成分人参总皂甙、人参单体皂甙Rg_1,当归挥发油以及榔槟生物碱的颜色和百分含量均无明显变化,杀虫、灭菌效果显著,防止二次感染、辐照后贮藏一年仍可达到色鲜、味正、不生虫、不发霉的良好效果。     

PLA/CoFe_2O_4载药微球的制备、表征及释药性能

采用 乳化-溶剂挥发法制备了聚乳酸(polylactie acid,PLA)载硫酸庆大霉素复合微球.通过正交设计实验优选PLA载药微球的最佳实验条件.在此基础上利用微乳法制备的铁酸钴(CoFe2O4)制备了PLA/CoFe_2O_4载硫酸庆大霉素复合微球.通过透射电子显微镜(TEM)、X-射线衍射(XRD)、振动样品磁强计(VSM)对铁酸钴进行微观结构表征和性能分析.采用傅立叶变换红外光谱(FT-IR),扫描电子显微镜(SEM)、生物数码显微镜对聚乳酸载药微球和PLA/CoFe_2O_4载药微球进行了微观结构的表征和分析.结果 表明两种载药微球呈规则球形,表面光滑,分布较均匀,平均粒径约为20μm.通过体外模拟释药试验考查了PLA载药微球和PLA/CoFe_2O_4载药微球的释药性能.结果 表明聚乳酸作为药物载体具有明显的药缓控释作用,PLA/CoFe_2O_4载药微球药物释放持续的时间最长.     

60Co-γ射线辐照对赤芍和黄芩有效成分的影响

目的:考察60Co-γ射线辐照灭菌效果及对中药赤芍和黄芩有效成分的影响。方法:选择5,8,10kGy3种辐照剂量对黄芩、赤芍饮片进行辐照。比较辐照前后饮片的杂菌和霉菌总数及其有效成分黄芩苷和芍药苷的含量。结果:两味中药在经过5kGy的辐照后,都能达到卫生学标准要求,且有效成分较辐照前无明显变化;经过8kGy、10kGy辐照后,赤芍所含的成分芍药苷有明显变化。结论:60CO-γ射线辐照灭菌的效果理想,但要慎重选择辐照的剂量。     

辐射灭菌不同剂量设定方法的比较

摘要 目的：比较分析3种常用灭菌剂量设定方法的适用性,为企业选择剂量设定方法提供参考。方法：本文采用系列辐射剂量对定量菌球进行辐射处理,根据辐射结果获得菌球的D10值,然后通过D10值计算理论剂量,最后与3种设定方法获得的剂量进行比较。结果：方法1、方法2、VDmax法的灭菌剂量分别为24.5kGy,19.2kGy,25kGy,与理论灭菌剂量的偏差分别为97.6%、54.8%、101.6%。结论：使用方法2设定的灭菌剂量最接近于产品微生物辐射抗力所需的灭菌剂量,但其所需样本量最大,其灭菌剂量设定成本最高,在日常实践中,需要考量日常辐照灭菌成本与剂量设定成本的平衡;使用VDmax法设定的灭菌剂量是较为保守的,由于样本量小,其灭菌剂量设定成本最低,适用于风险较高、附加值较高且样本不易获得的产品的;由于方法1要求的样本适中且兼具有一定的保守性,使用方法1进行灭菌剂量设定是医疗器械行业较为通行做法,企业需要根据实际需求兼顾产品风险选择合适的剂量设定方法。     

60Co-γ辐照对红花药材及醇提取物羟基红花黄色素A的影响

目的 考察60Co-γ射线辐照灭菌效果及对中药红花和红花25％乙醇提取物中有效成分羟基红花黄色素A的影响.方法 选择5、10kGy 2种辐照剂量对红花和红花25％乙醇提取物进行辐照.比较辐照前后杂菌和霉菌总数及其有效成分羟基红花黄色素A的含量.结果 红花药材及红花25％乙醇提取液在经过5kGy的辐照后,都能达到卫生学标准要求.红花药材经过5kGy辐照后,红花所含有效成分羟基红花黄色素A不发生明显的变化,10kGy辐照后,红花所含有效成分羟基红花黄色素A降低34％;而红花25％乙醇提取液经5、10kGy辐照后,羟基红花黄色素A分别降低44％、71％.结论 60Coγ射线辐照灭菌的效果理想,但不是任何药材和制剂都能采用这种灭菌方法.     

60Co辐照对睾丸酮/乳酸-乙醇酸共聚物微球理化特性及体外释放的影响

目的：睾丸酮（Ｔ）／乳酸－乙醇酸共聚物（ＰＬＧＡ）微球＾６０Ｃｏ辐照灭菌可行性研究,方法：Ｔ／ＰＬＧＡ微球在＾６０Ｃｏ源下,以２５ｋＧｙ的剂量进行辐照,对微球辐照前后主药Ｔ,载体ＰＬＧＡ的理化特性和现球本外释药速率的变化进行比较,考察＾６０Ｃｏ辐照对Ｔ／ＰＬＧＡ微球理化性及药物体外释放的影响。结果：＾６０Ｃｏ辐照引起ＰＬＧＡ分子量一定程度的下降,但对Ｔ／ＰＬＧＡ微球的理化特性及体外释药速率没有影响     

转移因子经60Co-γ射线辐照前后活性的比较研究

目的考察转移因子干粉采用60Co-γ射线辐照灭菌的可能性.方法将样品分别用2,4,8 kGy的剂量进行辐照,对其辐照前后微生物限度及活力的结果进行比较.结果经2 kGy的剂量辐照后效果最理想,细菌数从800个·g-1下降到33个·g-1,而活力只从22.3%下降到19.4%.结论转移因子干粉可以采用辐照的方法进行灭菌,但要控制好辐照剂量.     

Effects of water-soluble antioxidant from spinach, NAO, on doxorubicin-induced heart injury.

Doxorubicin (DOX) produces clinically restorative responses in numerous human cancers, but its cardiotoxicity has limited its usefulness. Because reactive oxygen species may affect DOX-induced antitumor activity and cardiotoxicity, we evaluated the prophylactic effect of spinach natural antioxidant (NAO) on DOX-induced cardiotoxicity and oxidative stress in female Balb/c mice using histological, electron microscopical and biochemical parameters. Mice were treated with NAO for 7 days prior to and/or for 6 days after DOX administration. Pretreatment with NAO (cumulative dose: 130 mg/kg) did not hinder the effectiveness of DOX. Light and electron microscopy of DOX-treated heart revealed myocardial degeneration. When administered combined before and after DOX, NAO conferred the most significant cardiac protection. The effects of NAO on the lipid peroxidation product, malondialdehyde, and on H2O2/ hydroperoxides were examined on day 6 following DOX administration; levels of both were elevated in DOX-treated mice, compared to control. Pretreatment with NAO prevented these changes. Pretreatment with NAO before DOX administration decreased catalase and increased superoxide dismutase activities compared to the DOX group. Our results suggest usage of NAO in combination with DOX as a prophylactic strategy to protect heart muscle from DOX-induced cellular damage.     

Effect of natural antioxidants and apocynin on LPS-induced endotoxemia in rabbit

The objective of this study was to compare the prophylactic effects of the natural antioxidant from spinach (NAO) and apocynin, on the hepatic oxidative stress and liver damage induced by lipopolysaccharide (LPS). Male New Zealand rabbits were challenged with LPS with or without 8 days of antioxidant pretreatment. Pretreatment with NAO, but not apocynin, significantly (p < 0.05) decreased the levels of hydroperoxides and malondialdehyde (MDA) in the liver cytosolic fraction and the activity of NADPH oxidase-generated superoxide in the microsomal fraction, compared to LPS alone. The activity of glutathione peroxidase (G-POX) was significantly (p < 0.05) increased in the LPS-treated group, whereas treatment with NAO, but not apocynin, significantly (p < 0.05) decreased G-POX activity. Pretreatment with the same antioxidants had no significant effects on superoxide dismutase (SOD) activity, whereas an increased level of catalase (CAT) was obtained in all LPS-treated groups. TUNEL immunohistochemical staining in the LPS-treated animals indicated that there was no increase in apoptosis outside of necrotic foci. However, apoptotic hepatocytes were observed within areas of focal necrosis in animals exposed to LPS alone or LPS plus apocynin. Hepatocyte cell proliferation was tested by the proliferating-cell nuclear antigen (PCNA) tool, which indicated a proliferative effect in the LPS group, whereas the effect disappeared in the antioxidant-treated groups. The prophylactic effect of NAO on liver pathology and the significant decreases in lipid peroxidation products and NADPH oxidase activity suggest the use of NAO as an efficient strategy for treatment of endotoxemia.     

中性氧化铝在中药含量测定样品前处理中的应用

中性氧化铝在食品、保健食品、化妆品和药品等领域的含量测定中广泛用于样品的前处理。综述中性氧化铝在中药材及其饮片、中药制剂的含量中测定样品前处理的使用情况,有关粒度、pH值、含水量、装柱量等对测定结果的影响,对中性氧化铝在中药含量测定样品前处理中存在的问题及其对策进行探讨,以期为药检工作者提供参考。     

Topical and oral administration of the natural water-soluble antioxidant from spinach reduces the multiplicity of papillomas in the Tg.AC mouse model

The Tg.AC mouse carrying the v-Ha-ras structural gene is a useful model for the study of chemical carcinogens, especially those acting via non-genotoxic mechanisms. This study evaluated the efficacy of the non-toxic, water-soluble antioxidant from spinach, natural antioxidant (NAO), in reducing skin papilloma induction in female hemizygous Tg.AC mice treated dermally five times over 2.5 weeks with 2.5 microg 12-O-tetradecanoylphorbol-13-acetate (TPA). The TPA-only group was considered as a control; the other two groups received, additionally, NAO topically (2 mg) or orally (100 mg/kg), 5 days/week for 5 weeks. Papilloma counts made macroscopically during the clinical observations showed a significant decrease in multiplicity (P<0.01) in the NAO topically treated group. According to histological criteria, papilloma multiplicity were lower in both topical-NAO and oral-NAO groups, but significantly so only in the oral-NAO mice (P<0.01). The beneficial effect of NAO in the Tg.AC mouse is reported.     

蜂毒磷脂酶A_2的降压作用

iv蜂毒磷脂酶A_2(PLA_2)可使麻醉大鼠和猫的血压产生快速而明显的下降,降压作用主要与释放组胺有关,合用组胺H_1、H_2受体拮抗剂,可以显著减弱蜂毒PLA_2的降压作用。     

Melatonin reduces early changes in intramitochondrial cardiolipin during apoptosis in U937 cell line.

Cardiolipin (CL) is found exclusively in the inner mitochondrial membrane. CL deficiency leads to an alteration in the stability of mitochondrial membranes, to an increased permeability as well as a decreased respiratory rate, and therefore to mitochondria which are completely dysfunctional. It is known that reactive oxygen species (ROS) cause a decrease and a variation in CL content, concomitantly the formation of the mitochondrial permeability transition pore facilitates the release of cytochrome c (cyt c) into the cytosol. Melatonin (Mel), the secretory product of the pineal gland, is a potent and efficient endogenous radical scavenger. It has been shown to protect, various biomolecules, such as DNA, membrane lipids, and cytosolic proteins from oxidative damage. To evaluate the protective role of Mel, we have studied U937 cells treated with UV-B irradiation. In our model, the administration of 1mM Mel before UV-B irradiation showed a significant protection from apoptotic cell death, in particular, mitochondrial structure and function were preserved through apoptotic pathways when cells were preincubated with 1mM Mel before UV-B exposure. The cardiolipin-sensitive probe 10-nonyl acridine orange (NAO) was used to monitor changes in mitochondrial lipids. Our data suggest that the Mel treatment protects CL from ROS and this suggests a possible link with the reduction of the apoptotic phenomenon.     

The effect of natural antioxidants, NAO and apocynin, on oxidative stress in the rat heart following LPS challenge

Oxidative damage plays a key role in septic shock induced by lipopolysaccharide (LPS) which is known to enhance the formation of reactive oxygen species (ROS). In this study, biochemical parameters indicative of oxidative stress were tested in the rat heart following LPS challenge, with and without pretreatment with the antioxidants NAO (natural antioxidant) and apocynin. NAO is a natural antioxidant isolated and purified from spinach and its main components are flavonoids and coumaric acid derivatives. Treatment with LPS alone significantly (P<0.05) increased the malondialdehyde (MDA) level in heart, both in cytosolic and mitochondrial fractions by 1.5- and 2.4-fold, respectively, and in plasma (2.66 fold). In the heart homogenate, the level of hydroperoxides also increased significantly (P<0.05). In addition, LPS treatment significantly (P<0.05) increased NADPH oxidase activity in the heart microsomal fraction by approximately 10-fold compared to control. Pretreatment for 7 days with either apocynin or NAO prior to the LPS challenge significantly (P<0.05) improved rat survival, decreased MDA levels in both fractions and decreased microsomal NADPH-oxidase activity, compared to LPS alone. Catalase (CAT) activity slightly increased at 24 h post-LPS injection in LPS group and returned to the control level in the apocynin treated group. No meaningful changes were indicated for glutathione peroxidase activity among all the treatment groups. The activities of cytosolic and mitochondrial superoxide dismutase (SOD) enzymes significantly (P<0.05) increased approximately 20% in the LPS-treated group, compared to control. Apocynin significantly (P<0.05) decreased SOD level in the mitochondrial fraction with no effect on the cytosolic fraction; whereas, NAO had no important effect on SOD level in both fractions. The beneficial pretreatment effects of the antioxidants against oxidative stress in the rat heart presented in this study may suggest a potential chemopreventive effect of this compound in sepsis prevention.     

丁基苯酞对大脑中动脉阻断后皮层组织中花生四烯酸释放及磷脂酶A2基因表达的影响

目的　研究丁基苯酞 (dl NBP) ,d NBP和l NBP对大脑中动脉阻断 (MCAO) 6h后缺血区皮层中花生四烯酸 (AA)释放及磷脂酶A2 (PLA2 )基因表达的影响。方法　阻断大脑中动脉起始部造成局灶性脑缺血模型。HPLC检测AA。Northernblot检测皮层中PLA2 基因表达。结果　MCAO后 6h ,皮层中AA释放明显增加。于脑缺血后 5min和 12 0min ,给dl NBP(10或 2 0mg·kg- 1)和尼莫地平 (0 5mg·kg- 1)可显著抑制AA的释放。d NBP和l NBP作用比较 ,显示d NBP有与dl NBP相似的作用 ,而l NBP则无明显影响。Northern印迹结果表明 ,脑缺血 6h ,皮层中PLA2 的基因表达增强。dl NBP和d NBP(10 ,2 0mg·kg- 1,ip)皆可使表达降低 ,而l NBP对缺血脑组织中PLA2 的基因表达的升高无明显影响。结论　dl NBP和d NBP可抑制MCAO后脑组织中AA释放和PLA2 的基因表达。     

The application of rational design on phospholipase A(2) inhibitors

The phospholipase A(2) (PLA(2)) superfamily consists of different groups of enzymes which are characterized by their ability to catalyze the hydrolysis of the sn-2 ester bond in a variety of phospholipid molecules. The products of PLA(2s) activity play divergent roles in a variety of physiological processes. There are four main types of PLA(2s): the secreted PLA(2s) (sPLA(2s)), the cytosolic PLA(2s) (cPLA(2s)), the calcium-independent PLA(2s) (iPLA(2)) and the lipoprotein-associated PLA(2s) (LpPLA(2s)). Various potent and selective PLA2 inhibitors have been reported up to date and have provided outstanding support in understanding the mechanism of action and elucidating the function of these enzymes. The current review focuses on the implementation of rational design through computer-aided drug design (CADD) on the discovery and development of new PLA(2) inhibitors.     

Phospholipase A2 as targets for anti-cancer drugs

Phospholipase A(2) (PLA(2)) are esterases that cleave glycerophospholipids to release fatty acids and lysophospholipids. Inhibition of PLA(2) alters cancer cell growth and death in vitro and PLA(2) expression is increased in breast, lung, and prostate cancers compared to control tissues. Thus, PLA(2) may be novel targets for chemotherapeutics. However, PLA(2) are a diverse family of enzymes, encompassing 19 members. The selectivity of these individual PLA(2) for phospholipids varies, as does their location within the cell, and tissue expression. Thus, their role in cancer may also vary. This review summarizes the expression of individual PLA(2) in cancers, focuses on the potential mechanisms by which these esterases mediate carcinogenesis, and suggests that select PLA(2) isoforms may be targets for anti-cancer drugs.