{"title":"Agents that induce pseudo-allergic reaction.","authors":"H Wang, H S Wang, Z P Liu","doi":"10.5582/ddt.2011.v5.5.211","DOIUrl":"https://doi.org/10.5582/ddt.2011.v5.5.211","url":null,"abstract":"<p><p>Pseudo-allergic reactions may result from the activation of inflammatory or anaphylactic mechanisms independent of antigen-specific immune responses. Recent statistics show that pseudo-allergic reactions may represent as high as two thirds of all immediate hypersensitivity reactions, implying a great amount of morbidity and numerous health care costs. In this review, we concentrate on agents mediating pseudo-allergic reactions and evaluate accurately the available information on their modes of action. The agents discussed here are divided into three types: (i) Direct mast cell activators, which may activate mast cells in an IgE-independent manner, such as opioid drugs, basic secretagogues and calcium ionophore A23187; (ii) Complement activators, including liposomes, radiocontrast media and Cremophor EL, which may activate the complement system by different pathways: the classical pathway, the mannose-binding lectin pathway or the alternative pathway; (iii) Nonsteroidal anti-inflammatory drugs, which may inhibit the function of cyclooxygenase-1, resulting in the occurrence of adverse reactions. In addition, nonclinical detection methods of pseudo-allergic reactions are also reviewed in order to supply valuable information for clinical diagnosis.</p>","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"211-9"},"PeriodicalIF":3.1,"publicationDate":"2011-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5582/ddt.2011.v5.5.211","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30545244","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Targeting apoptosis pathways in cancer with magnolol and honokiol, bioactive constituents of the bark of Magnolia officinalis.","authors":"H L Xu, W Tang, G H Du, N Kokudo","doi":"10.5582/ddt.2011.v5.5.202","DOIUrl":"https://doi.org/10.5582/ddt.2011.v5.5.202","url":null,"abstract":"<p><p>Magnolol and honokiol, main active compounds from the bark of Magnolia officinalis, have been found to have various pharmacological actions, including anti-oxidative, anti-inflammatory, anti-tumor, and anti-microbial properties, without appreciable toxicity. Recently, the anti-tumor activity of magnolol and honokiol has been extensively investigated. Magnolol and honokiol were found to possess anti-tumor activity by targeting the apoptosis pathways, which have been considered as targets for cancer therapies. This review will focus on the mechanisms by which magnolol and honokiol act on apoptosis pathways in cancer that have been characterized thus far, including the death receptor mediated pathway, mitochondria-mediated pathway, caspase-mediated common pathway, and regulation of apoptosis-related proteins. These breakthrough findings may have important implications for targeted cancer therapy and modern applications of traditional Chinese medicine.</p>","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"202-10"},"PeriodicalIF":3.1,"publicationDate":"2011-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5582/ddt.2011.v5.5.202","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30545243","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Anti-Candida and radical scavenging activities of essential oils and oleoresins of Zingiber officinale Roscoe and essential oils of other plants belonging to the family Zingiberaceae.","authors":"M Takahashi, S Inouye, S Abe","doi":"10.5582/ddt.2011.v5.5.238","DOIUrl":"https://doi.org/10.5582/ddt.2011.v5.5.238","url":null,"abstract":"<p><p>Essential oils of young and mature rhizomes, air-dried and steamed rhizomes, and seed rhizomes of Zingiber officinale Roscoe (ginger) were prepared, and their inhibition of filamentation by Candida albicans was examined. Ginger essential oils, and particularly those from seed and air-dried rhizomes, had potent inhibitory activity compared to ginger oleoresins obtained by ethanol and hypercritical carbon dioxide extraction and essential oils of 5 other plants in the family Zingiberaceae. Of the constituents, [6]-shogaol was most active against filament formation and growth of C. albicans, followed by citral and [6]-gingerol. Ginger oleoresin, and especially that obtained by ethanol extraction, with a high [6]-gingerol content exhibited potent scavenging activity against 1,1-diphenyl-2-picrylhydrazyl radicals in comparison to essential oils of ginger and other Zingiberaceae plants.</p>","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"238-45"},"PeriodicalIF":3.1,"publicationDate":"2011-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5582/ddt.2011.v5.5.238","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30544148","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
G Kaushal, R Ramirez, D Alambo, W Taupradist, K Choksi, C Sirbu
{"title":"Initial characterization of D-cycloserine for future formulation development for anxiety disorders.","authors":"G Kaushal, R Ramirez, D Alambo, W Taupradist, K Choksi, C Sirbu","doi":"10.5582/ddt.2011.v5.5.253","DOIUrl":"https://doi.org/10.5582/ddt.2011.v5.5.253","url":null,"abstract":"<p><p>The purpose of this study is to characterize D-cycloserine (DCS) physicochemical properties to facilitate future formulation development of DCS for anxiety disorders. A stability-indicating HPLC assay method for the quantitation of DCS was developed and calibrated to be used for this study. The partition coefficient was determined and compared with the predicted value. The solution stability of DCS was studied under various pH (2.0-11.5) and ionic strengths of 10 and 20 mM at physiological temperature of 37°C. The 250 mg capsule was compounded to the nominal strength of 50 mg used for anxiety disorders. These capsules were then put under stability. The in vitro dissolution was also carried out at 37°C as per the United States Pharmacopeia (USP) guidelines. The partition coefficient value (Kp) determined for the DCS was log Kp = -2.89 ± 0.06 (n = 6). The pH-solution stability profile shows that DCS has maximum stability under alkaline conditions. The maximum rate of degradation was seen at pH of 4.7. The mean percent recovery of DCS from the capsules compounded to strength of 50 mg was 100.3 ± 1.4. The stability study of the reformulated capsules concluded that reformulated DCS is stable for at least one year at room temperature. The in vitro dissolution illustrates that all the DCS is released from the capsules in 10 min. The present characterization of DCS study will serve as guidance for the future directions regarding the reformulation of DCS in order to be used in anxiety disorders.</p>","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"253-60"},"PeriodicalIF":3.1,"publicationDate":"2011-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5582/ddt.2011.v5.5.253","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30544150","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
K Saeio, S Yotsawimonwat, S Anuchapreeda, S Okonogi
{"title":"Development of microemulsion of a potent anti-tyrosinase essential oil of an edible plant.","authors":"K Saeio, S Yotsawimonwat, S Anuchapreeda, S Okonogi","doi":"10.5582/ddt.2011.v5.5.246","DOIUrl":"https://doi.org/10.5582/ddt.2011.v5.5.246","url":null,"abstract":"<p><p>The aim of this study is to develop a microemulsion product from a plant essential oil having the highest anti-tyrosinase activity. The in vitro anti-tyrosinase activity of six essential oils extracted from six edible plants was compared. The oil of Cymbopogon citratus demonstrated the highest activity which was significantly nontoxic to normal human cells. The GC-MS data indicated that geranial and neral are the major compounds in the oil. The phase diagram composed of C. citrates oil, water, and surfactant mixture was conducted by a titration method. Ethyl alcohol was found to be the most suitable cosurfactant for the C. citrates oil microemulsion. The results revealed that the amount of oil and water played an important role in microemulsion conductivity and type. The most desirable o/w type of C. citratus oil microemulsion was found to be composed of 20% oil, 30% water, and 50% surfactant mixture of a 2:1 weight ratio of Tween 20 and ethyl alcohol.</p>","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"246-52"},"PeriodicalIF":3.1,"publicationDate":"2011-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5582/ddt.2011.v5.5.246","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30544149","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Matrix type transdermal therapeutic systems of glibenclamide: Formulation, ex vivo and in vivo characterization.","authors":"A Ali, A Trehan, Z Ullah, M Aqil, Y Sultana","doi":"10.5582/ddt.v5.1.53","DOIUrl":"https://doi.org/10.5582/ddt.v5.1.53","url":null,"abstract":"<p><p>Matrix type transdermal therapeutic systems (TTS) of glibenclamide were formulated using polymers Eudragit RL 100, ethyl cellulose, PVP K-30, and polyvinyl acetate, and citral was used as the penetration enhancer. The polymer films were formulated with Eudragit RL 100 and PVP K-30 in different ratios and subsequently subjected to ex vivo studies (drug permeation through rat skin) followed by interaction studies, skin irritation studies, accelerated stability analysis, and in vivo studies (determination of blood glucose level in rabbits). The drug content of the formulations was found to be 99.1-99.2%. The cumulative percentages of drug permeated through rat skin from the three selected formulations in 48 h were 95.3%, 98.8%, and 99%, respectively. A plot between cumulative percent of drug permeated and square root of time exhibited linear curves, which suggests the Higuchian matrix mechanism of drug release. The formulation containing Eudragit RL 100 and PVP K-30 showed better improvement in hypoglycemic activity in rabbits (56.2-60.8% reduction in blood glucose level, p < 0.05). There were fewer fluctuations in blood glucose level as compared to oral therapy due to controlled release of the active pharmaceutical ingredient, and no interaction was found between the drug and excipients of the formulation. Accelerated stability analysis showed that the formulation was stable up to 5.5 years, with negligible skin irritation. The formulation precluded severe hypoglycemic reactions (side effect of sulfonylureas) and was effective for management of diabetes mellitus up to 48 h, with a single TTS.</p>","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"53-9"},"PeriodicalIF":3.1,"publicationDate":"2011-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5582/ddt.v5.1.53","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30543384","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Antibacterial activities of Sesbania grandiflora extracts.","authors":"P Anantaworasakul, S Klayraung, S Okonogi","doi":"10.5582/ddt.v5.1.12","DOIUrl":"https://doi.org/10.5582/ddt.v5.1.12","url":null,"abstract":"<p><p>In this study, Sesbania grandiflora, a plant in the Leguminosae family, was investigated for its antibacterial activities. The agar well diffusion assay as well as the agar and broth dilution assays were used for determination of antibacterial activities. The crude ethanolic extracts obtained from different parts of this plant exhibited different potent activities. The stem bark has the most potential to yield an extract with the highest antibacterial action. The fractionation of the stem bark with different solvents indicated that the fractionated extracts obtained from ethyl acetate or butanol possessed the most pronounced antibacterial activity. The kinetic study of bactericidal activities revealed that the butanol fractionated extract of the stem bark was effective against Gram negative bacteria. This study suggests that the stem bark of S. grandiflora contains promising antibacterial substances for clinical purposes.</p>","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"12-7"},"PeriodicalIF":3.1,"publicationDate":"2011-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5582/ddt.v5.1.12","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30543973","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"c-Met: A potential therapeutic target for hepatocellular carcinoma.","authors":"J J Gao, Y Inagaki, X Xue, X J Qu, W Tang","doi":"10.5582/ddt.2011.v5.1.2","DOIUrl":"https://doi.org/10.5582/ddt.2011.v5.1.2","url":null,"abstract":"<p><p>The approval of receptor tyrosine kinase (RTK) targeted agent sorafenib as the first effective drug for the systemic treatment of advanced hepatocellular carcinoma (HCC) represents a milestone in the treatment of this disease. A better understanding of HCC pathogenesis will lead to development of novel targeted treatments. As a typical member of the RTK family, c-Met represents an intriguing target for cancer therapy. The c-Met signaling pathway has been shown to be deregulated and to correlate with poor prognosis in a number of major human cancers. This review discusses the possibility of c-Met as a target in HCC treatment from the following respects: i) c-Met expression and activation profile in HCC, ii) relationship between c-Met and clinicopathologic state and prognosis of HCC, iii) role of c-Met signaling activity in HCC genesis and progression, and iv) strategy of c-Met pathway targeting therapy in HCC treatment.</p>","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"2-11"},"PeriodicalIF":3.1,"publicationDate":"2011-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5582/ddt.2011.v5.1.2","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30543972","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"A comparative study of protective mechanisms of glycine and L-arginine against cisplatin-induced nephrotoxicity in rat renal cortical slices.","authors":"Y Fk Mahran, A E Khalifa, E El-Demerdash","doi":"10.5582/ddt.v5.1.32","DOIUrl":"https://doi.org/10.5582/ddt.v5.1.32","url":null,"abstract":"<p><p>Amino acids exert nephroprotective effects in various forms of acute renal injury depending on their renal hemodynamic effects. The present study was designed to elucidate and compare the role of non hemodynamic mechanisms in protective actions afforded by glycine and L-arginine against cisplatin (CDDP)-induced nephrotoxicity using rat renal cortical slices (RCS). We have investigated the possible modulatory effect of glycine and L-arginine on oxidative stress and necrosis induced by CDDP as well as on CDDP uptake by kidney. After 4 h of incubation with 2 mM CDDP, nephrotoxicity was demonstrated by significant increased lactate dehydrogenase leakage, decreased ability of the slices to reduce 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, increased lipid peroxides and depleted reduced glutathione. Also, CDDP significantly inhibited pyruvate-stimulated gluconeogenesis. Histopathological examination of RCS confirmed the occurrence of tubular coagulative necrosis in cortex and corticomedullary regions. Preincubation of RCS with 1 mM glycine or L-arginine 1 h before CDDP addition significantly attenuated the oxidative stress and tubular necrotic effects of CDDP. L-Arginine showed greater antioxidant properties while glycine showed a greater antinecrotic effect. Moreover, the nephroprotective effect was mediated through lowering the platinum uptake by RCS. However, they could not counteract the inhibition of gluconeogenesis induced by CDDP. In conclusion, the present study sheds light on the mechanisms involved in glycine and L-arginine nephroprotection.</p>","PeriodicalId":520606,"journal":{"name":"Drug discoveries & therapeutics","volume":" ","pages":"32-40"},"PeriodicalIF":3.1,"publicationDate":"2011-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.5582/ddt.v5.1.32","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"30543383","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}