Quality evaluation of commercial extracts of Scutellaria baicalensis

Botanical products have been widely used for various illnesses and general well-being. However, quality control of botanical products is often not performed due to lack of standardization, resulting in inconsistent efficacies and sometimes serious toxicity. The goals of this study were to determine the correlation between chemical composition and biological activities and to establish a method to measure authenticity, chemical consistency, and biological potency of botanical products. A high-performance liquid chromatography method was used to analyze the authenticity and chemical composition of 10 different commercial extracts. The cell viability assay and prostaglandin E2 (PGE2) enzyme immunoassay were used to analyze biological potency and consistency. Our results showed all extracts contained marker components (baicalein and/or baicalin), confirming their authenticity. However, significant product-to-product and batch-to-batch variation of these marker components was observed with 4 products containing no baicalin at all and baicalein concentration ranging from 0 to 52.3 g/mg. The 50% growth inhibition concentration of the extracts ranged from 0.18 to 2.0 mg/ml, more than an 11-fold variation. PGE2 levels varied from 19.5 to 111.1 pg/106 cells, more than a 5.7-fold difference. These results demonstrated significant variation in chemical composition and biological activities of the commercial extracts and that the amount of marker components may not reflect biological activity levels. Therefore, chemical analysis alone is inadequate for quality control, and biological assays must be included for botanical products to ensure chemical authenticity as well as pharmacological/biological potency and consistency.     

黄芩不同部位金属元素的含量测定

用原子吸收分光光度法分别测定了黄芩根、茎、叶中１１种金属元素的含量。发现叶、茎中富含镁、铬、镍、铁、钾、锰元素；叶中镁、钾、铬、镍、钴、铁、锰、铅的含量明显高于根中，锌、钼的含量和根中接近；茎中锌、锰、钾、铅的含量远高于根中，钴、镍、铬、钼、铁的含量和根中接近。     

A medicinal extract of Scutellaria baicalensis and Acacia catechu acts as a dual inhibitor of cyclooxygenase and 5-lipoxygenase to reduce inflammation

A mixed extract containing two naturally occurring flavonoids, baicalin from Scutellaria baicalensis and catechin from Acacia catechu, was tested for cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) inhibition via enzyme, cellular, and in vivo models. The 50% inhibitory concentration for inhibition of both ovine COX-1 and COX-2 peroxidase enzyme activities was 15 microg/mL, while the mixed extract showed a value for potato 5-LOX enzyme activity of 25 microg/mL. Prostaglandin E2 generation was inhibited by the mixed extract in human osteosarcoma cells expressing COX-2, while leukotriene production was inhibited in both human cell lines, immortalized THP-1 monocyte and HT-29 colorectal adenocarcinoma. In an arachidonic acid-induced mouse ear swelling model, the extract decreased edema in a dose-dependent manner. When arachidonic acid was injected directly into the intra-articular space of mouse ankle joints, the mixed extract abated the swelling and restored function in a rotary drum walking model. These results suggest that this natural, flavonoid mixture acts via "dual inhibition" of COX and LOX enzymes to reduce production of pro-inflammatory eicosanoids and attenuate edema in an in vivo model of inflammation.     

Aldol derivatives of Thioxoimidazolidinones as potential anti-prostate cancer agents

The paper discusses the synthesis and stereochemical aspects of the anti aldol products, 3-(substituted phenyl)-5-[(substituted phenyl) hydroxy methyl]-5-methyl-4-oxo-2-thioxoimidazolidines. The stereochemistry observed in the aldol reactions with benzaldehydes was explained by transition state model of the endocyclic (E)-enolate formed from the rigid 4-oxo-2-thioxoimidazolidine skeleton. Proton NMR and ROESY spectral analyses were carried out to identify the syn and anti conformations of the aldol diastereomers. Configurations of the enantiomers of the representative anti aldol product 3-(4-chlorophenyl)-5-[(4-chlorophenyl) hydroxy methyl]-5-methyl-4-oxo-2-thioxoimidazolidine was determined by single crystal XRD studies. The compounds were screened in vitro against prostate cancer cell lines, PC-3 and LNCaP and the most potent derivatives were identified.     

Molecular Mechanism of Anti-Prostate Cancer Activity of Scutellaria Baicalensis Extract

Scutellaria baicalensis is a widely used Chinese herbal medicine historically used in antiinflammatory and anticancer therapy. The goals of the study were to 1) determine its in vitro and in vivo anti-prostate cancer activity, 2) investigate its molecular mechanism directed at cell proliferation control including cyclooxygenase-2(COX-2) prostaglandin E ₂ (PGE ₂ ) and cyclins/cdks pathways, and 3) compare it with those of PC-SPES (PC stands for prostate cancer and spes is Latin for hope), a former herbal mixture for prostate cancer treatment of which S. baicalensis is a major constituent. Two human prostate cancer cell lines (LNCaP, androgen dependent, and PC-3, androgen independent) were assessed for growth inhibition. S. baicalensis exerted dose- and time-dependent increased growth inhibition in both cell lines. However, the PC-3 cells IC₅₀ (50% growth inhibition concentration) were slightly more sensitive than LNCaP cells (IC ₅₀ = 0.15 mg/ml), although the former is androgen independent. S. baicalensis was more effective in inhibition of cell growth compared with PC-SPES (IC ₅₀ = 0.38 mg/ml for PC-3 cells). Significant reduction of PGE ₂ synthesis in both cells after treatment with S. baicalensis resulted from direct inhibition of COX-2 activity rather than COX-2 protein suppression. S. baicalensis also inhibited prostate-specific antigen production in LNCaP cells. Finally, S. baicalensis suppressed expression of cyclin D1 in LNCaP cells, resulting in a G ₁ phase arrest, while inhibiting cdk1 expression and kinase activity in PC-3 cells, ultimately leading to a G ₂ /M cell cycle arrest. Animal studies showed a 50% reduction in tumor volume after a 7-wk treatment period. This study demonstrated that S. baicalensis may be a novel anticancer agent for the treatment of prostate cancer.     

黄芩提取物联合顺铂对人卵巢癌细胞株SKOV-3凋亡的研究

目的:探讨黄芩提取物(Scutellaria Baicalensis)与顺铂(cisplatin,DDP)联合应用对卵巢癌细胞系SKOV-3增殖及凋亡的影响。方法:采用MTT比色法检测S.Baicalensis与DDP联合应用对SKOV-3细胞增殖的影响,吖啶橙染色观察诱导细胞凋亡情况,流式细胞仪分析细胞周期及凋亡并计算细胞平均凋亡率,Westernblot技术观察细胞内p53、ERK1/2、p-STAT3的表达。结果:300μg/mlS.Baicalensis联合5μg/ml DDP给药:①48h后可使肿瘤细胞抑制率由单独应用DDP的15.8%提高到37.3%;②吖啶橙荧光染色可见细胞呈现明显凋亡形态,其凋亡率与10μg/ml DDP组相当;③流式细胞检测结果显示,可使细胞凋亡率从15.1%提高到42.2%(P<0.05);④westernblot结果显示,p53、ERK1/2、p-STAT3表达较5μg/ml DDP组单独给药组降低(P<0.05)。结论:S.Baicalensis与DDP联合应用增强对卵巢癌细胞株SKOV-3的致凋亡效应,联合应用可达到减毒增效的效果。     

Molecular mechanism of apoptosis induction by resveratrol, a natural cancer chemopreventive agent

In efforts to identify naturally occurring compounds that act as protective agents, resveratrol, a phytoalexin existing in wine, has attracted much interest because of its diverse pharmacological characteristics. Considering that apoptosis induction is the most potent defense approach for cancer treatment, we have tried to summarize our present understanding of apoptosis induction by resveratrol based on the two major apoptosis pathways.     

绿茶及其有效成分对肾性高血压大鼠左室肥厚抑制作用的研究

目的研究绿茶及其提取物对肾性高血压大鼠左室肥厚的抑制作用机制。方法雄性Wistar大鼠160只,体重180~220g,随机分为5组,建立二肾一夹法大鼠肾性高血压左室肥厚模型:假手术组(SHAM)和手术组(2K1C)正常饮水;手术+绿茶组(2K1C+GT)饮用2%绿茶水;手术+茶多酚组(2K1C+TP)饮用0.1%茶多酚水;手术+EGCG组(2K1C+EGCG)饮用0.05%EGCG水,术后即给予不同浓度的绿茶及其提取物,持续8周直至实验结束。结果与假手术组比较,手术组和各饮茶组血压、左心室与体重比值(LVW/BW)和左心室壁厚度(LVWT)均显著升高(P<0.01)。而与手术组相比,不同浓度的绿茶及其有效成分(2%绿茶、0.1%茶多酚、0.05%EGCG)左心室重/体重(LVW/BW)、左心室壁厚度显著降低,抗氧化酶(SOD和GSH-Px)的活性升高,活性氧自由基(ROS)以及Ras和ERK1/2蛋白表达降低,但对大鼠收缩压无显著性影响。结论绿茶及其提取物对肾性高血压大鼠左室肥厚有抑制作用,其机制可能是由于茶及其有效成分具有抗氧化活性,能够清除ROS,以及对Ras-MAPK信号传导通路的调控有关。     

Spermicidal activity of extract from Cestrum parqui

OBJECTIVE: The leaf extract of Cestrum parqui was examined for its effects on sperm motility in vitro. METHODS: Washed sperm were prepared by discontinuous buoyant density gradient centrifugation and incubated with varying concentrations of extract from C. parqui (40-250 microg/mL) at 37 degrees C and 5% CO(2). Sperm motility and viability were assessed at different intervals ranging from 5 to 240 min. Morphological changes in human ejaculated spermatozoa after exposure to the extract were evaluated under transmission electron microscope. RESULTS: A dose- and time-dependent effect of this extract on sperm motility and viability was observed. The maximal spermicidal effect was observed with a 250-microg/mL dose of the extract. Transmission electron microscope revealed a significant damage to sperm membrane in both head and acrosomal membranes, notable swelling and disruption. CONCLUSION: The present study indicates that this natural extract has potential spermicidal effect in vitro.     

Immunomodulatory activity of aqueous extract of Actinidia macrosperma

Actinidia macrosperma (AM) is a medicinal plant in China and has been well known for its activities against cancers, especially of lung, liver and digestive system. The immunomodulatory effects of AM aqueous extract were examined using S180-bearing mice. Young adult (20 +/- 2 g) ICR mice inoculated with S180 cells were divided randomly into six groups: S180-bearing control group, normal control group, positive control group (Ginseng Radix Rubra 2000 mg/kg) and 50, 100, 250 mg/kg AM treatment groups. Each group consisted of ten mice. Body and tumor weights were obtained after 12 consecutive days, and their humoral, cellular and nonspecific immune functions were also determined by relative assays. The results showed that the aqueous extract of AM was lack of significant inhibit on transplantable sarcoma S180, with a inhibit rate of 1.5% -14.8% (dose at 250 mg/kg was the best), but significantly increased the overall immune functions (especially at 100 and 250 mg/kg). The immunomodulatory effect was dose-dependent in a nonlinear fashion with the optimal dose of 100 mg/kg. The AM-induced antitumor effects were at least partially indirect and were associated with the modulation of immune functions.     

Molecular basis of cancer

Cancer is a group of diseases characterized by an autonomous proliferation of neoplastic cells which have a number of alterations, including mutations and genetic instability. Cellular functions are controlled by proteins, and because these proteins are encoded by DNA organized into genes, molecular studies have shown that cancer is a paradigm of acquired genetic disease. The process of protein production involves a cascade of several different steps, each with its attendant enzymes, which are also encoded by DNA and regulated by other proteins. Most steps in the process can be affected, eventually leading to an alteration in the amount or structure of proteins, which in turn affects cellular function. However, whereas cellular function may be altered by disturbance of one gene, malignant transformation is thought to require two or more abnormalities occurring in the same cell. Although there are mechanisms responsible for DNA maintenance and repair, the basic structure of DNA and the order of the nucleotide bases can be mutated. These mutations can be inherited or can occur sporadically, and can be present in all cells or only in the tumor cells. At the nucleotide level, these mutations can be substitutions, additions or deletions. Several of the oncogenes discussed below, including the p53, c-fms, and Ras genes, can be activated by point mutations that lead to aminoacid substitution in critical portions of the protein. This article examines the current concepts relating to cellular mechanism that underlie the molecular alterations that characterize the development of cancer.     

Mitogenic activity of an extract of Trypanosoma gambiense.

An extract obtained by repeated freeze/thawing of a freshly isolated strain of Trypanosoma gambiense caused stimulation of lymphocytes obtained from healthy adult donors and from cord blood. The active factor had some stimulatory effect on purified B and T lymphocytes and in two of five subjects increased IgM production by lymphocytes cultured in vitro. A trypanosome-derived mitogenic factor may play some part in the pathogenesis of the hypergammaglobulinaemia characteristic of African trypanosomiasis.     

Benefits of whole ginger extract in prostate cancer

It is appreciated far and wide that increased and regular consumption of fruits and vegetables is linked with noteworthy anticancer benefits. Extensively consumed as a spice in foods and beverages worldwide, ginger (Zingiber officinale Roscoe) is an excellent source of several bioactive phenolics, including non-volatile pungent compounds such as gingerols, paradols, shogaols and gingerones. Ginger has been known to display anti-inflammatory, antioxidant and antiproliferative activities, indicating its promising role as a chemopreventive agent. Here, we show that whole ginger extract (GE) exerts significant growth-inhibitory and death-inductory effects in a spectrum of prostate cancer cells. Comprehensive studies have confirmed that GE perturbed cell-cycle progression, impaired reproductive capacity, modulated cell-cycle and apoptosis regulatory molecules and induced a caspase-driven, mitochondrially mediated apoptosis in human prostate cancer cells. Remarkably, daily oral feeding of 100?mg/kg body weight of GE inhibited growth and progression of PC-3 xenografts by approximately 56?% in nude mice, as shown by measurements of tumour volume. Tumour tissue from GE-treated mice showed reduced proliferation index and widespread apoptosis compared with controls, as determined by immunoblotting and immunohistochemical methods. Most importantly, GE did not exert any detectable toxicity in normal, rapidly dividing tissues such as gut and bone marrow. To the best of our knowledge, this is the first report to demonstrate the in vitro and in vivo anticancer activity of whole GE for the management of prostate cancer.     

葡萄籽提取物抗实验性动脉粥样硬化作用及其机理研究

为探讨葡萄籽提取物抗实验性动脉粥样硬化作用及机理 ,将 5 0只动脉粥样硬化敏感株近交系C5 7BL 6J小鼠 ,随机分为正常对照组、高脂模型组、葡萄籽提取物低、高剂量组和药物对照组 ,正常对照组和高脂模型组 ,每日分别给予普通饲料和高脂饲料 ,葡萄籽提取物组和药物对照组 ,在每日给予高脂饲料的同时 ,分别添加葡萄籽提取物 (0 2mg g、0 6mg g体重 )和普托罗考片 (0 2mg g体重 ) ,实验至第 2 1周末 ,眼球放血处死小鼠 ,检测血清氧化型低密度脂蛋白 (OX LDL)、细胞粘附因子 1(ICAM 1)和一氧化氮 (NO)含量 ,同时取主动脉作病理形态学观察。结果发现 ,葡萄籽提取物组 ,血清OX LDL和ICAM 1水平均高于正常对照组 ,但明显低于高脂模型组 ,血清NO水平 ,则低于正常对照组而高于高脂模型组。观察主动脉部位的形态显示 ,葡萄籽提取物组其血管壁增厚程度、玻璃样改变和泡沫细胞数量均轻于模型组 ,高剂量组效果为佳 ,但仍重于正常对照组。实验结果提示 ,葡萄籽提取物具有减缓C5 7BL 6J小鼠动脉粥样硬化形成的作用 ,这可能与阻抑OX LDL、ICAM 1含量升高减低对血管内皮细胞损伤及保护血管内皮功能等作用有关     

中药仙鹤复方水提取物对肝癌H22细胞增殖与凋亡的影响及其作用机制

目的：观察中药仙鹤复方水提取物（aqueousextract of Xian-he Compound,XHC）对肝癌H22细胞增殖与凋亡的影响度对炎症因子COX-2的影响。方法：栗用四甲基偶氮唑盐（MTT）比色法检测不同浓度的H22肝癌细胞增殖情况;Hoechst33342染色观察细胞形态学变化;western blot检测COX-2蛋白质表达;RT-PCR法检测COX-2mRNA水平表达的变化。结果：XHC各剂量组较空白对照组对肝癌H22细胞均有明显的抑制作用,以作用24h后的1．8g／mL XHC组作用最显著,抑制率为71．25％±0．32％;与空白对照组相比,LPS诱导后加1．8g／m LXHC组有较显著的凋亡率．凋亡率由1．91％±0．45％增加至8．53％±0．13％;同样作用条件下与空白对照组及阳性对照组相比COX-2蛋白质及mRNA的表达明显下调。结论：XHC的抑瘤作用与下调COX-22蛋白质及mRNA的表达有密切关系。     

Molecular mechanisms of cancer cachexia

Molecular mechanisms of cancer cachexia. Cancer cachexia is a complex, multifactorial syndrome characterised by a critical weight loss, anorexia, asthenia and anaemia. Most of the patients with advanced cancer suffer from cancer cachexia. The cachectic state is closely associated with progressive expansion of the tumour and leads to a malnutrition status due to the induction of anorexia and decreased food intake. In addition, the competition for nutrients between the tumour and the host leads to malnutrition state, too, which promotes severe metabolic disturbances in the host, including hypermetabolism which leads to an increased energetic inefficiency. Although, the search for the cachectic factors has a long history, we are still far away from knowing the complete answer. The main aim of the present paper is to summarise the different catabolic mediators involved in cancer cachexia. Better understanding of the pathomechanism of cancer cachexia can lead to the discovery of new, effective strategies of the therapy for the future.     

香椿叶水提物对小鼠炎症抑制作用

目的 研究香椿叶水提物抗炎作用机制。方法 观察香椿叶水提物对二甲苯所致小鼠耳廓肿胀、角叉菜胶所致大鼠足肿胀、炎症组织和血清中前列腺素E₂(PGE₂)、一氧化氮(NO)含量的影响。结果 0.5,1.5 g/kg香椿叶水提物灌胃给药能明显抑制对二甲苯所致小鼠耳廓肿胀,抑制率分别为33.85%和46.98%;对照组大鼠注射角叉菜胶2,4 h后,足跖肿胀度为(0.68±0.19),(1.12±0.10)mL,6 h时开始恢复;对角叉菜胶所致正常大鼠足肿胀,香椿叶水提物高、低剂量组注射3和2 h后与对照组比较可明显抑制;低、高剂量香椿叶水提物可降低肿胀足爪组织中NO及PG E₂含量;低剂量香椿叶水提物可降低血清中NO含量。结论 香椿叶水提物可能通过影响炎症介质释放和减少NO的生成而起到抑制角叉菜胶性大鼠足肿胀作用。