Drug Development and Therapeutics最新文献

{"title":"In vitro anticancer potential of Semecarpus anacardium Linn","authors":"Md. Nasar Mallick, W. Khan, Mhaveer Singh, Mohd. Zeeshan Najm, M. Kashif, Sayeed Ahmad, S. Husain","doi":"10.4103/2394-6555.180167","DOIUrl":"https://doi.org/10.4103/2394-6555.180167","url":null,"abstract":"Background: Keeping in view the toxicity of Semecarpus anacardium Linn. as reported in the traditional literature, the present study was carried out to evaluate the in vitro cytotoxic activity of ethanolic extract of Semecarpus on two different cell lines. Materials and Methods: The ethanolic extract of Semecarpus was prepared using cold extraction method. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay of ethanolic extract was carried out on HeLa and SiHa cell lines for determination of cytotoxicity. Results: The IC50values of ethanolic extract of S. anacardium in HeLa and SiHa cell lines were 44.0 μg/ml and 57.0 μg/ml, respectively. The extract was standardized by thin-layer chromatography and Gas chromatography-mass spectrometry. Conclusion: The results showed good cytotoxic activity in the ethanolic extract of S. anacardium in both the cell lines may be due to the presence of toxic flavones.","PeriodicalId":11347,"journal":{"name":"Drug Development and Therapeutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2016-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75606180","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":"Doxorubicin prodrug for cytoplasmic and nuclear delivery in breast cancer cells","authors":"Animikh Ray, K. Cholkar, Ravinder Earla, A. Mitra","doi":"10.4103/2394-6555.180158","DOIUrl":"https://doi.org/10.4103/2394-6555.180158","url":null,"abstract":"Purpose: The objective of this study was to develop a novel peptide prodrug of doxorubicin which can evade over-expressed efflux pumps in breast cancer cells. This approach may lead to increased uptake and higher drug accumulation in nuclei of cancer cells. Materials and Methods: L-val-L-val doxorubicin prodrug was synthesized following standard f-moc chemistry. The prodrug was analyzed for stability, cellular and nuclear uptake and interaction with efflux and peptide transporters. Breast cancer cells (T47D) were grown on polystyrene 12-well plates. Result: The prodrug Val-Val-doxorubicin was found to be very stable in breast cancer cell homogenate. It was able to evade efflux pumps. The prodrug penetrated cytoplasm and nucleus of cancer cells by interacting with peptide transporters.These transporters (pepT1 and pepT2) are expressed both on plasma and nuclear membrane of breast cancer cells. Uptake of prodrug was found to be 10 times more than parent drug. Conclusion: Peptide prodrug derivatization of doxorubicin has potential to evade efflux pumps and increase availability and nuclear accumulation of doxorubcin in breast cancer cells.","PeriodicalId":11347,"journal":{"name":"Drug Development and Therapeutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2016-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76021314","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":"Strain improvement of Phaffia rhodozyma for astaxanthin production","authors":"H. Nangia, Mojeer Hasan, Mohd. Azhar, P. Bhatt, B. Panda","doi":"10.4103/2394-6555.180169","DOIUrl":"https://doi.org/10.4103/2394-6555.180169","url":null,"abstract":"Objective: The aim of the present study is to evaluate and optimize different carbon sources at different temperatures in shake flask for cell growth and astaxanthin accumulation in ultraviolet (UV) mutant Phaffia rhodozyma. The focus is to make the process cost-effective and fruitful with higher productivity. Materials and Methods: Adaptive strain development was carried out so that the P. rhodozyma can give the best astaxanthin at a higher temperature (35°C), increasing the process economy. P. rhodozyma was cultivated with three broad spectrum antibacterial drugs - streptomycin, gentamycin, and ampicillin (200 μL) and with antifungal drug - fluconazole (200 μL) to determine the effect on yeast growth and astaxanthin production. Rice, cane juice, and sucrose were selected as carbon source and compared with dextrose at different fermentation temperatures - 22°C, 30°C, 33°C, and 35°C for astaxanthin production. Results: P. rhodozyma was resistant to antibiotic drugs inhibiting bacterial and fungal contaminants. Rice being more economical was selected as carbon source, but the strain was not able to utilize starch-rich substrate leading to its rejection. When P. rhodozyma was grown in cane juice, biomass is highest (OD 2.77) at 30°C and 610 nm wavelength, whereas astaxanthin productivity is highest (OD 2.64) in dextrose media at 30°C and 450 nm. Comparative metabolic and growth results for UV mutants showed significantly higher biomass and astaxanthin productivity in comparison to wild strain. Conclusion: The most efficient carbon source in terms of penny-pinching and astaxanthin productivity was found to be dextrose containing media at 30°C.","PeriodicalId":11347,"journal":{"name":"Drug Development and Therapeutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2016-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85046952","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":"Standardization of Unani polyherbal formulation, Qurse-e-Hummaz: A comprehensive approach","authors":"Y. Kamal, Mhaveer Singh, Shahana Salam, S. Ahamd","doi":"10.4103/2394-6555.180161","DOIUrl":"https://doi.org/10.4103/2394-6555.180161","url":null,"abstract":"Background: An increase in the awareness about the advantages of the traditional system of medicines has led to the commercialization of the formulations used for the treatments. Manufacture of these medicines to meet this increasing demand has resulted in a decline in their quality, primarily due to a lack of adequate regulations pertaining to this sector of medicine. Hence, it is necessary to come up with a systematic approach to develop well-designed methodologies for the standardization of polyherbal formulations which are used in traditional systems of medicine. Materials and Methods: Qurs-e-Hummaz formulations were prepared by a qualified “Hakim” (Unani medical practitioner) of Faculty of Unani Medicine, Hamdard University, as per the formula and instruction given in National Formulary of Unani Medicine. Results: Various quality control parameters such as organoleptic evaluations (color, odor, taste, and consistency), physicochemical evaluations (loss on drying, disintegration time, moisture content, total ash, acid insoluble ash, water soluble ash, pH of 1 and 10% solution, extractive values, water soluble matter, alcohol-soluble matter, and total phenolic content) and thin layer chromatography fingerprint profiling have been carried out in triplicate. The evaluation of contaminants such as heavy metals, aflatoxins, pesticide residues, and microbial contamination has also been carried out in the formulation. Conclusion: Help in maintaining the quality and batch to batch consistency of many important polyherbal formulations.","PeriodicalId":11347,"journal":{"name":"Drug Development and Therapeutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2016-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76084278","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":"First in human trials: Are there any benefits of including placebo treatments?","authors":"A. Agyeman, R. Ofori-Asenso","doi":"10.4103/2394-6555.180155","DOIUrl":"https://doi.org/10.4103/2394-6555.180155","url":null,"abstract":"","PeriodicalId":11347,"journal":{"name":"Drug Development and Therapeutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2016-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88290479","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":"Quantification of vasaka alkaloids in in vitro cultures and in natural leaves from Indian subcontinents by reversed phase- high performance liquid chromatography","authors":"Sayeed Ahmad, Madhukar Garg, E. Tamboli, Y. Kamal, S. Ansari","doi":"10.4103/2394-6555.180165","DOIUrl":"https://doi.org/10.4103/2394-6555.180165","url":null,"abstract":"Background: The present study was designed to develop an efficient protocol for studying the enhancement of in vitro production of secondary metabolites in Adhatoda vasica leaves collected from the varied geographical locations of Indian sub-continents by a validated simultaneous high-performance liquid chromatography gradient method for the quantification of vasicine and vasicinone in the developed calli and crude samples. Materials and Methods: The analysis was carried out on a reverse phase C18column using 0.1% of orthophosphoric acid: Acetonitrile in gradient manner and carried out the detection at 280 nm wavelength keeping the flow rate of 1.0 mL/min. Results: The simultaneous method was found linear with regression coefficient r2 = 0.991 in a wide range (100–500 μg/mL) precise, accurate, and robust for quinazoline alkaloids in samples. Results clearly showed a significant increase in the concentration of alkaloids in in vitro cultures as compared to natural ones. The proposed method was validated as per the International Conference on Harmonization guidelines for accuracy, precision, robustness, limit of detection, and limit of quantitation. Conclusion: The developed method was found suitable for quality control of A. vasica and for the analysis of vasicine and vasicinone in any type of sample.","PeriodicalId":11347,"journal":{"name":"Drug Development and Therapeutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2016-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80199000","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":"Quality control analysis of Khamira Abresham Hakim Arshad Wala and Khamira Marwareed","authors":"M. Khan, W. Khan, W. Ahmad, Mhaveer Singh, Sayeed Ahmad","doi":"10.4103/2394-6555.180164","DOIUrl":"https://doi.org/10.4103/2394-6555.180164","url":null,"abstract":"Background: Unani system of medicine is based on the principles proposed by Galen, a Greek practitioner. Since then, many Arab and Persian scholars have contributed to the system. Among them, Ibn-e-Sina, an Arab philosopher and Physicist, who wrote “Kitab-al-shifa” are worth mentioning. This system has an extensive and inspiring record in India. Khamira Abresham Hakim Arshad Wala (KAHAW) and Khamira Marwareed (KM) are semisolid sugar-based preparations with potent cardiac tonic and well-known antioxidant properties. It has been studied that therapeutic intervention of KAHAW may be used to prevent or to decrease the deterioration of cognitive function and neurobehavioral activities, often associated with the generation of a free radical. However, no considerable attempt has been made for quality evaluation of KAHAW. Materials and Methods: In the present investigations, KAHAW and KM were evaluated for their phytochemical screening, physicochemical standards, presence of minerals, contaminants such as aflatoxins, pesticide residues, thin layer chromatography, and high performance thin layer chromatography (HPTLC) as per WHO and AYUSH guidelines for development of quality standards, which can be used by Unani industries. Results: Physicochemical parameters of the prepared compound formulation KAHAW and KM were studied such as total ash, acid insoluble ash, water soluble ash, solubility matter in alcohol and water, and loss on drying at 105°C, pH as per the methods described in WHO guidelines. The heavy metal, aflatoxins, and pesticide residues were also determined for safety evaluation. The total phenolic and flavonoid contents were estimated using catechin and quercetin as standard after preparing calibration plot, respectively. HPTLC fingerprinting of hydrolyzed chloroform extracts of KAHAW and KM was carried out to determined a number of spots present in them. Conclusions: This study on pharmacognostical standardization of KAHAW and KM will provide useful information for its identification and quality control and can be applied by different manufacturers of these formulations.","PeriodicalId":11347,"journal":{"name":"Drug Development and Therapeutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2016-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79607886","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":"Quality control of an antipsoriatic ayurvedic herbal Formulation: Lajjalu Keram","authors":"M. Athar, S. Musthaba, A. Al-Asmari, S. Baboota, J. Ali, Sayeed Ahmad","doi":"10.4103/2394-6555.180162","DOIUrl":"https://doi.org/10.4103/2394-6555.180162","url":null,"abstract":"Background: Psoriasis is an autoimmune disorder, which affects a large group of human population of world (3%). Till date, there is no treatment for psoriasis except some herbal drugs and its constituents. Since Ayurveda is the main traditional system of medicine in India, here, we have selected one ayurvedic formulation - Lajjalu Keram, which has been used since long for their quality control. Methods: Total microbial load of formulations were carried out for total fungal count and total bacterial count. Lajjalu Keram was also tested by high-performance liquid chromatographic (HPLC) for aflatoxins (B1, B2, G1, and G2), which showed its presence below the permissible limit; similarly, pesticides residues were analyzed using gas chromatography/mass spectrometry for organophosphates and organochlorides, which showed that pesticides were below detection limit (0.1 ppb). The content of heavy metals was analyzed using AAS, which demonstrated the presence of cadmium, lead, and arsenic below permissible limit, whereas mercury was found absent. Results: The result of quality control analysis showed the presence of alkaloids, tannins, carbohydrate, saponins, proteins and amino acids, lipid/fats, phenolic compounds, and flavonoids in formulation. The dermal toxicity (LD50) of Lajjalu Keram in Wistar rats was found more than 2000 mg/kg (safe for the management of psoriasis). Formulation was also analyzed for their composition of fatty acids. It was found to have 13 fatty acids, out of which, seven were saturated fatty acids (95.2%) and the rest were unsaturated fatty acids (3.27%). A rapid HPLC method for quantification of mimosine (an unusual amino acid present in formulation) has been developed and validated. The mimosine content in Lajjalu Keram was found to be 0.0070% w/w with % relative standard deviation of 0.41. Conclusion: The formulation afforded significant and better protection of carrageenan-induced rat paw edema (72.11% inhibition) as compared to control. The shelf life studies on antipsoriatic herbal formulations were carried out for 6 months at different time intervals. No significant variation in analysis parameters was observed on the storage of formulations up to 6 months. The assay of constituents using mean curve of sigma plot showed 44.2 month of shelf life for Lajjalu Keram.","PeriodicalId":11347,"journal":{"name":"Drug Development and Therapeutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2016-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84589191","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":"Antimicrobial activity of sugar-based semisolid polyherbal ayurvedic formulation: Chyawanprash","authors":"M. Khan, Satyajyoti Kanjilal, Arun Gupta, Sayeed Ahmad","doi":"10.4103/2394-6555.180159","DOIUrl":"https://doi.org/10.4103/2394-6555.180159","url":null,"abstract":"Objective: This study evaluated the antimicrobial activity of chloroform (CHCl3) extracts of chyawanprash (Dabur India Ltd., Uttar Pradesh, India) and hydrolyzed chyawanprash against Escherichia coli and Staphylococcus aureus on nutrient agar media using cup plate method. Materials and Methods: CHCl3extracts of chyawanprash were prepared directly as well as by previously hydrolyzing with dilute HCl. Three test groups of 10, 20, and 50 mg/ml were prepared for each CHCl3extract, whereas ampicillin 20 mg/ml was used as standard group. Further, six agar plates were prepared for each group, i.e., three for E. coli and three for S. aureus. Cups were bored on each plate with the help of steel cup borer and cups on each plate were marked for identification. Extracts of different concentrations (i.e., 10, 20, and 50 mg/ml) were poured into cups and all plates were then incubated at 37°C for 48 h. After incubation, plates were observed for bacterial growth and zone of inhibition were measured. Results: Results showed that both CHCl3as well as hydrolyzed CHCl3extract of chyawanprash showed concentration-dependent antimicrobial activity. The largest zone of inhibition was observed at the concentration of 50 mg/ml of both CHCl3extracts of chyawanprash (12.7 ± 1.5 mm for E. coli and 15.0 ± 1.0 mm for S. aureus) and hydrolyzed chyawanprash (14.3 ± 0.6 mm for E. coli and 16.3 ± 0.6 mm for S. aureus). Conclusion: Chyawanprash possesses promising potential for use as an antimicrobial agent.","PeriodicalId":11347,"journal":{"name":"Drug Development and Therapeutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2016-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91398790","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":"Simultaneous determination of 18α-glycyrrhetinic acid and 18β-glycyrrhetinic acid in Glycyrrhiza glabra root by reversed phase high-performance liquid chromatography","authors":"Ambika Chamoli, Makhmur Ahmad, Mojeer Hasan, B. Panda","doi":"10.4103/2394-6555.180168","DOIUrl":"https://doi.org/10.4103/2394-6555.180168","url":null,"abstract":"Background: The aim of the present research work is to develop a high-performance liquid chromatography (HPLC) method for simultaneous analysis of 18α-glycyrrhetinic acid (18α-GA) and 18β-GA (18β-GA) of Glycyrrhiza glabra. Materials and Methods: About 20 μL aliquots of each 18α-GA and 18β-GA were analyzed using reversed-phase C-18 column. The mobile phase was acetonitrile:tetrahydrofuran:water (10:80:10, v/v/v). The run time was 10 min at flow rate of 1 ml/min. Ultraviolet detection was carried out at 254 nm. Results: 18α-GA and 18β-GA were well resolved in reversed phase C-18 column using mobile phase acetonitrile: tetrahydrofuran: water (10:80:10, v/v/v, pH 7.9). The Rtof 18α-GA and 18β-GA was detected at 2.091 and 2.377 min, respectively. Conclusion: The developed chromatography method could be extended for potential quantification or simultaneous determination of these markers in plant as well as in herbal formulation.","PeriodicalId":11347,"journal":{"name":"Drug Development and Therapeutics","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2016-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76517915","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}