INDIAN JOURNAL OF PHARMACEUTICAL SCIENCES

Evaluation of In Vitro Antioxidant Potential of Cordia retusa
Amudha M and Rani S
The present study was carried out to investigate the antioxidant potential, total flavonoid and phenolic content in extracts of aerial parts of Cordia retua (Vahl.) Masam. The samples such as ethyl acetate and ethanol extracts were tested using six in vitro models such as 2,2-diphenyl-1-picrylhydrazyl, nitric oxide radical, iron chelating, hydroxyl radical, superoxide radical scavenging activity and total antioxidant activity to evaluate the in vitro antioxidant potential of C. retusa by spectrophotometrically. Total flavonoid and phenolic content in samples were estimated using aluminum chloride colorimetric and Folin-Ciocalteu method. The results were analyzed statistically by the regression method. Half maximal inhibitory concentration (IC50) of the ethanol extract was found to be 596 μg/ml for DPPH, 597 μg/ml for nitric oxide radical, 554 μg/ml for iron chelating, 580 μg/ml for hydroxyl radical, 562 μg/ml for superoxide radical and 566 μg/ml for total antioxidant capacity. Furthermore, the total flavonoid content and total phenolic content of the ethanol extract were found to be 2.71 mg gallic acid equivalent per gram of extract and 1.86 mg quercetin equivalent per gram of extract, respectively. In all the testing, a significant correlation existed between concentrations of the extract and percentage inhibition of free radicals. The results of the present comprehensive analysis demonstrated that C. retusa possess potent antioxidant activity, high flavonoid and phenolic content. The antioxidant property may be related to the polyphenols and flavonoids present in the extract. These results clearly indicated that C. retusa is effective against free radical mediated diseases as a natural antioxidant.
Stereoselective Reduction of Prochiral Ketones by Plant and Microbial Biocatalysts
Javidnia K, Faghih-Mirzaei E, Miri R, Attarroshan M and Zomorodian K
Chiral alcohols are the key chiral building blocks to many enantiomerically pure pharmaceuticals. The biocatalytic approach in asymmetric reduction of corresponding prochiral ketones to the preparation of these optically pure substances is one of the most promising routes. The stereoselective reduction of different kinds of prochiral ketones catalyzed by various plants and microorganisms was studied in this work. Benzyl acetoacetate, methyl 3-oxopentanoate, ethyl 3-oxopentanoate, and ethyl butyryl acetate were chosen as the model substrates for β-ketoesters. Benzoyl acetonitrile, 3-chloro propiophenone, and 1-acetyl naphthalene were chosen as aromatic aliphatic ketones. Finally, 2-methyl benzophenone and 4-chloro benzophenone were selected as diaryl ketones. Plant catalysis was conducted by Daucus carota, Brassica rapa, Brassica oleracea, Pastinaca sativa, and Raphnus sativus. For microbial catalysis, Aspergillus foetidus, Penicillum citrinum, Saccharomyces carlbergensis, Pichia fermentans, and Rhodotrula glutinis were chosen. Chiral alcohols were obtained in high yields and with optical purity. A superiority in the microorganisms' performance in the bioreduction of prochiral ketones was detected. Among microorganisms, Rhodotrula glutinis showed remarkable results with nearly all substrates and is proposed for future studies.
Evaluation of Parmotrema reticulatum Taylor for Antibacterial and Antiinflammatory Activities
Jain AP, Bhandarkar S, Rai G, Yadav AK and Lodhi S
Lichens produce variety of secondary metabolites including depsides, depsidones and dibenzofurans having multifunctional activity in response to external environmental condition. Present study provides evidence for in vitro antibacterial and in vivo antiinflammatory activity of acetone and ethanol extracts of Parmotrema reticulatum. In vitro antibacterial activity was investigated against gram positive and gram negative bacteria. Cotton pellet-induced granuloma, xylene-induced ear swelling, carragennan-induced edema, histamine-induced and carboxymethylcellulose sodium-induced leukocyte emigration in mice models were used to quantify the antiinflammatory activity. Acetone and ethanol extracts were showed antibacterial activity against Bacillus subtilis (minimal inhibitory concentration: 100 and 150 μg/ml) and Staphylococcus aureus (minimal inhibitory concentration: 100 and 200 μg/ml), Escherichia coli (minimal inhibitory concentration: 200 and 250 μg/ml), and Pseudomonasa eruginosa (minimal inhibitory concentration: 200 and 300 μg/ml). Acetone extract was inhibited edema significantly at 200 mg/kg with xylene, cotton pellet, carragennan and histamine induced edema in vivo models. Ethanol extract was found effective at dose of 300 mg/kg with all in vivo antiinflammatory models. The results showed significant (P<0.01) antiinflammatory effects at 200 and 300 mg/kg dose of acetone and ethanol extracts, respectively, which can be concluded that significant activity may be due to presence of flavanoids in ethanol extract and usnic acid in acetone extract.
Molecular and Computational Studies on Apoptotic Pathway Regulator, Bcl-2 Gene from Breast Cancer Cell Line MCF-7
Tiwari P and Khan MJ
Cancer is a dreadful disease constituting abnormal growth and proliferation of malignant cells in the body. Next to lung cancer, breast cancer is the most common form of cancer affecting women. The apoptotic pathway regulators, B cell lymphoma family of protein, play a key role in various malignancies defining cancer and their constitutive expression plays an integral role in breast cancer chemotherapy. The research work discusses the identification and molecular cloning of a B cell lymphoma like gene from human breast cancer cell line. The open reading frame of the gene consisted of 965 nucleotides, encoding a protein of 380 amino acids with a predicted molecular weight of 42.5 kilodalton. The predicted physiochemical properties of the gene were as follows: Isoelectric point - 9.49, molecular formula - C1893H3004N534O548S16, total number of negatively charged residues, (Aspartate+Glutamate) - 26, total number of positively charged residues, (Arginine+Lysine)-39, instability index-42.08 (unstable protein) and grand average of hydropathicity is -0.202. Additionally, phobius prediction suggested non-cytoplasmic localization of the putative protein. The presence of secondary structure in the protein was determined by Memsat program. A 3 dimensional protein homology model was generated using threading based method of protein modeling for structural and functional annotation of the putative protein. Future prospects accounts for the biochemical characterization of the enzyme including in vitro assays on breast cancer cell line would establish the functional characteristics of the protein and its physiological mechanisms in breast cancer development and its therapeutic-target role in future.
Phytochemical, Antioxidant and Anticancer Activities of Extracts of Seven Fruits Found in the Southern Brazilian Flora
Bagattoli PC, Cipriani DC, Mariano LN, Correa M, Wagner TM, Noldin VF, Filho VC and Niero R
Methanol extracts of seven edible fruits found in southern Brazil: Garcinia achachairu, Rubus imperialis, Rubus rosaefolius, Solanum quitoense, Solanum sessiliflorun, Diospyros inconstans and Plinia glomerata, were evaluated for their total phenol content and antioxidant activity in different in vitro free radical scavenging models. In addition, studies were performed on cell viability of extracts of the seeds of G. achachairu against murine melanoma cells. The fruits peel and seeds of G. achachairu were very promising in terms of total phenol content (data in gallic acid equivalent per gram), as assessed by the Folin-Ciocalteu method, with values of 9.70±3.2 and 8.40±1.1, respectively. On the other hand, antioxidant activity using the 2,2-diphenyl-1-picrylhydrazyl scavenging assay showed that the fruit pulp and peel of P. glomerata presented the best profile, with values of the 16.3±1.8 and 15.9±2.4 μg/ml, respectively. Regarding the cytotoxic effect of methanol extract and guttiferone A from G. achachairu, we have observed that both inhibit the growth of B16F10 tumor cells, with calculated IC50 values of 49.6±2.1 mg/ml and 48.6±5.4 mM, respectively.
Estimation Based on Emission Wavelength of Dabigatran Etexilate Mesylate in Bulk and Capsule Dosage Form
Anumolu PD, Satyanarayana M, Gayatri T, Praveena M, Sunitha G and Subrahmanyam CV
A simple, rapid, specific and highly sensitive spectrofluorimetric method has been developed for the quantification of dabigatran etexilate mesylate in bulk and capsule dosage form. A linear relationship was found between fluorescence intensity and concentration in the range of 0.01-1.0 μg/ml in dimethyl sulphoxide as solvent at an emission wavelength of 391 nm after excitation at 334 nm, with a good correlation coefficient (0.989). The detection and quantification limits were found to be 0.005 and 0.015 μg/ml, respectively. The proposed method was applied for dabigatran etexilate mesylate capsules, results reveal with percentage recovery of 102% and percentage relative standard deviation values were found to be less than 2 for accuracy and precision studies. The proposed method was validated for linearity, range, accuracy, precision, limit of detection and quantification according to International Conference on Harmonization guidelines. Statistical analysis of the results revealed high accuracy and good precision. The suggested procedures could be used for the determination of dabigatran etexilate mesylate in bulk and capsule dosage form in quality control laboratories of industries as well as in academic institutions.
Determination of Quality Standards for Draksharishta, a Polyherbal Ayurvedic Formulation
Pillai D and Pandita N
Draksharishta is an ayurvedic polyherbal formulation is prescribed for digestive impairment, respiratory disorders and weakness. Though the formula composition and therapeutic claims of draksharishta are part of the Ayurvedic Formulary of India, the scientific methods for its quality and safety evaluation are yet to be documented. The current work is an attempt to evaluate the quality parameters of draksharishta which has been checked vis a vis herbs used in the formulation by modern scientific control procedures like macroscopic and microscopic study, physico-chemical analysis, preliminary phytochemical analysis, thin layer chromatography and high performance thin layer chromatography to fix the quality standard of this formulation with reference to two marketed formulations i.e. M1 and M2, respectively. The quality control parameters were within the limit as per the Ayurvedic Pharmacopeia of India which signifies good quality and purity of the plant materials. Thin layer chromatography profiles showed the presence of gallic acid, catechin and resveratrol and further it was confirmed by HPTLC fingerprints. The results obtained can be used by pharmaceutical companies as quality control parameters in order to have a proper quality check during processing.
Antitarget Interaction, Acute Toxicity and Protein Binding Studies of Quinazolinedione Sulphonamides as GABA1 Antagonists
Ajeet , Verma M, Rani S and Kumar A
Diseases characterized by recurrent seizures are known as epilepsy. One of the most important mechanisms for handling it is GABA1 receptor mediated inhibition. In the same context while studying the treatment of epilepsy we observed significant effects by derivatives of sulfonamides, which prompted us to design novel derivatives by means of in silico resources with antiepileptic effects. Molecular docking approaches are routinely used in modern drug design to help understand drug-receptor interaction. This study has been performed with the help of Chemdraw Ultra 7.0, GUSAR online tool for IC50 and LD50 predictions, AutoDock Vina (Python Prescription 0.8), and PaDEL software. Results revealed that ligand-protein interaction affinity of all 10 designed molecules ranges from -5.7 Kcal/mol to -5.2 Kcal/mol, which is approximately comparable to pre-existing GABA1 inhibitor i.e. phenytoin (CID: 1775, ligand-protein interaction affinity is -6.5 Kcal/mol).
A Strategy for Quality Control of Menispermum dauricum DC Based on Cytotoxic Activity and HPLC Fingerprint Analysis
Liu LJ and Liu JN
The rhizome of Menispermum dauricum DC known as a traditional Chinese medicine, with high content of alkaloids, has been found to possess antitumor activity. In this research, an attempt to correlate fingerprinting with bioactivity was made for quality control of M. dauricum. Firstly, the cytotoxicity of extracts from ten batches of samples against human breast MCF-7 cancer cells was estimated by [3-(4, 5-dimethylthiazole-2-yl)-2, 5-diphenyltetrazoliumbromide] assay. Then, cytotoxic activity-integrated fingerprints were established by high performance liquid chromatography. Eight peaks were selected as the common peaks to evaluate the similarities of samples and hierarchical clustering analysis was used to identify and classify different samples into groups. Assays for determinations of total alkaloids and dauricine contents enabled cytotoxicity coefficient of each extract. The potential usefulness of employing cytotoxicity coefficient was investigated by a combination of Pearson correlation coefficients and multiple linear regression analysis as being the reliable parameter to evaluate the herbal extracts. The results indicated that the level of dauricine (peak 8 in the fingerprint) correlated closely with cytotoxicity and played a significant role in the cytotoxicity of Bei Dou-Gen and could be related to its antitumor properties. It is proposed that the cytotoxicity coefficient value with a cytotoxic activity-integrated fingerprint of key biomarkers (dauricine) may be useful indicators to adopt for the quality control of M. dauricum. The analysis of cytotoxic-activity-integrated fingerprint could correlate fingerprinting with bioactivities and would provide a reasonable strategy for quality control of complex mixture of herbal medicines.
Development of an Inhaled Sustained Release Dry Powder Formulation of Salbutamol Sulphate, an Antiasthmatic Drug
Kumaresan C and Sathishkumar K
The present research was aimed to develop and characterize a sustained release dry powder inhalable formulation of salbutamol sulphate. The salbutamol sulphate microparticles were prepared by solvent evaporation method using biodegradable polymer poly (D,L-lactic-co-glycolic acid) to produce salbutamol sulphate microparticle mixed with carrier respirable grade lactose for oral inhalation of dry powder. The drug content were estimated to produce 1 mg sustained release salbutamol sulphate per dose. Total four formulations K1, K2, K3 and K4 were prepared with 1:1, 1:2, 1:3, 1:4 ratio of salbutamol sulphate:poly (D,L-lactic-co-glycolic acid). The developed formulations were studied for physicochemical properties, in vitro drug relase and Anderson cascade impaction studies. The prepared formulations effectively releases drug for 12 h in diffusion bag studies. Based on dissolution performance the 1:1 ratio of salbutamol sulphate:poly (D,L-lactic-co-glycolic acid) produces in vitro release 92.57% at 12 h and having particle size of microparticles (D0.5μm) 5.02±0.6 and the pulmonary deposition of dry powder 34.5±3.21 (respiratory fraction in percentage).
Sensitivity of Interfibrillar and Subsarcolemmal Mitochondria to Cobalt Chloride-induced Oxidative Stress and Hydrogen Sulfide Treatment
Ayswarya A and Kurian GA
Oxidative stress plays a significant role not only in cardiovascular disease but also in non-communicable diseases, where it plays a significant role the mortality rate. Hydrogen sulfide, the biological gaseous signaling molecule that preserves mitochondria in its mode of action, is an effective cardioprotective drug. However, cardiac mitochondria comprise of two distinct populations, namely interfibrillar and subsarcolemmal mitochondria, which respond distinctly in cardiovascular disease. This study was designed to determine the direct impact of cobalt chloride-induced oxidative stress in isolated mitochondrial subpopulations with an intention to examine the efficacy of hydrogen sulfide in preserving interfibrillar and subsarcolemmal mitochondria functional activities when they were incubated as pretreated, co-treated and post-treated agent. Mitochondrial subpopulations were isolated from the heart of male Wistar rats and subjected to cobalt chloride treatment (500 μM) for 20 min, followed by incubation with 10 μM sodium hydrosulfide in three different ways (Pre, Co, and Post-cobalt chloride treatment). Mitochondrial oxidative stress was measured by the concentration of thiobarbituric acid reactive species, reduced glutathione and the activities of enzymes like superoxide dismutase, catalase and glutathione peroxidase. Mitochondrial membrane potential, swelling behavior and enzyme activities were measured to assess its function. The increased level of lipid peroxidation and the decreased level of reduced glutathione in cobalt chloride-induced group confirm the induction of oxidative stress and were more predominant in the subsarcolemmal mitochondria. Hydrogen sulfide treatment to interfibrillar and subsarcolemmal mitochondria preserved their functional activities, but the effect was prominent only with co-treated group. In conclusion, the present study demonstrated that subsarcolemmal mitochondria are more prone to oxidative stress and the co-treatment of the mitochondria with hydrogen sulfide preserved the enzyme activity in the in vitro conditions.
Can Analgesic-abuse Nephropathy is a Fertile Groundfor for Rare Collecting Duct (Bellini Duct) Renal Cell Carcinoma or Merely a Coincidence?
Jhorawat R, Beniwal P and Malhotra V
Nonsteroid antiinflammatory drugs have been implicated as nephrotoxic drugs, causing both acute and chronic adverse effects that range from reversible ischemia to chronic kidney disease and urothelial tumors to renal cell carcinoma specially papillary subtype. We report one case of collecting duct (Bellini duct) renal cell carcinoma in patient with analgesic-abuse nephropathy. This young individual was suffering from ankylosing spondylitis since the age of 16 years and was consuming diclofenac and paracetamol (acetaminophen) combination for >15 years. He developed hypertension, secondary glomerulopathy, chronic kidney disease and collecting duct renal cell carcinoma.
Evaluation of Immunomodulatory Activity of the Alkaloid Fraction of Trichopus zeylanicus Gaertn on Experimental Animals
Bachhav RS and Sambathkumar R
Trichopus zeylanicus Gaertn, (Trichopodaceae) is also known as "Arogyappacha" meaning the greener of health by tribal inhabitants (Kani tribes). This plant used as health tonic and rejuvenator. The whole plant material of Trichopus zeylanicus is defatted and successively extracted with methanol. The alkaloid fraction of Trichopus zeylanicus was obtained from methanol extract. Up to the dose of 2000 mg/kg b.w. per orally alkaloid fraction of Trichopus zeylanicus did not show any mortality or toxicity. Immunomodulatory activity of alkaloid fraction of Trichopus zeylanicus Gaertn was evaluated using various in vivo models including neutrophil adhesion test, delayed type hypersensitivity reaction, and effect on hematological parameter like, total white blood cell's, red blood cell's and hemoglobin and cyclophosphamide induce immunosupression. Sheep red blood cells were used to immunized the animals. The percentage of neutrophils adhesion to the nylon fiber was dose dependently increased in alkaloid fraction of Trichopus zeylanicus75, 150 and 300 mg/kg, p.o treated groups (50.57, 52.99 and 54.21%), respectively compared to control group. A dose dependent potentiating of delayed type hypersensitivity reaction induced by sheep red blood cells was also observed from the alkaloid fraction of Trichopus zeylanicus. On chronic administration of alkaloid fraction of Trichopus zeylanicus (75, 150 and 300 mg/kg. p.o.) caused significant (P<0.001) increased in hematological parameter like, total white blood cell's, red blood cell's and hemoglobin. Alkaloid fraction of Trichopus zeylanicus also prevented the myelosupression in mice treated cyclophosphamide (30 mg/kg, p.o.). The result of present investigation suggested that alkaloid fraction of Trichopus zeylanicus stimulate defense system by modulating several immunological parameters.
Preparation and Characterization of PEG-albumin-curcumin Nanoparticles Intended to Treat Breast Cancer
Thadakapally R, Aafreen A, Aukunuru J, Habibuddin M and Jogala S
The aim of present research was to prepare novel serum stable long circulating polymeric nanoparticles for curcumin with a modification to the well known and novel nanoparticle albumin bound technology. polyethylene glycol-albumin-curcumin nanoparticles were prepared using serum albumin and poly ethylene glycol using desolvation technique. Nanoparticles were characterized for encapsulation efficiency, particle size and surface morphology. Drug excipient compatibility was determined using fourier transform infrared spectroscopy. Physical state of the drug in the formulations was known by differential scanning colorimetry. In vitro release and solubility of the drug from nanoparticles were determined. In vivo Drug release, tissue uptake and kupffer cell uptake was determined with optimized nanoformulation in rats after intravenous administration. Cell viability assay was determined using breast cancer cell line MD-MB-231. Entrapment efficiency for prepared nanoparticle was above 95%. The polyethylene glycol-albumin-curcumin nanoparticles exhibited an interesting release profile with small initial burst followed by slower and controlled release. Solubility of the drug from the formulation was increased. A sustained release of drug from nanoparticles was observed for 35 days in both in vitro and in vivo studies with the optimized formulation. Polyethylene glycol-albumin-curcumin nanoparticles showed lesser liver and kupffer cell uptake as compared to that of curcumin-albumin nanoparticles suggesting the bestowment of stealthness to nanoparticles with pegylation. Also, the antiproliferative activity of polyethylene glycol-albumin-curcumin nanoparticle formulation was more as compared to native curcumin. Polyethylene glycol-albumin-curcumin nanoparticles thus developed can be conveniently used in breast cancer with improved efficacy compared to conventional therapies and as an alternate to nanoparticle albumin bound technology which is used in producing Abraxane, albumin based breast cancer targeting nanoparticles of paclitaxel.
Molecular Cytotoxic Mechanisms of 1-(3,4,5-Trihydroxyphenyl)-dodecylbenzoate in Human Leukemia Cell Lines
Maioral MF, Bubniak LD, Marzarotto MA, De Moraes AC, Leal P, Nunes R, Yunes RA and Santos-Silva MC
Recent studies have shown that gallic acid and its alkylesters induce apoptosis in different cell lines. Since new compounds with biological activity and less cytotoxicity to normal cells are necessary for cancer therapy, the aim of this study was to evaluate the cytotoxic effect of 1-(3,4,5-trihydroxyphenyl)-dodecylbenzoate on human acute myeloid leukemia K562 cells and on human acute lymphoblastic leukemia Jurkat cells. The cell viability was determined by MTT method. The apoptosis induction was assessed by bromide and acridine orange staining and by Annexin V-FITC Apoptosis Detection kit. The cell cycle analysis was carried out by flow cytometry using propidium iodide. Cytometric analysis was also performed to evaluate the expression of the following proteins: AIF, p53, Bcl-2 and Bax. The mitochondrial potential was also assessed by flow cytometry using MitoView633 kit. The results showed that the compound significantly reduced the cell viability of K562 and Jurkat cells in a concentration and time dependent manner (IC50 of 30 μM). The compound induced cell cycle arrest in G0/G1phase and significantly increased the proportion of cells in the sub-G0/G1phase. Apoptosis was confirmed by the sight of morphological characteristics of apoptosis and by phosphatidylserine externalization (73.47±5.71% of cells expressing annexin). The results also showed that the compound promotes a modification in Bax:Bcl-2 ratio and increases p53 expression. Thus, it is possible to conclude that 1-(3,4,5-trihydroxyphenyl)-dodecylbenzoate induces apoptosis by inhibiting the antiapoptotic protein Bcl-2 and by increasing the release of AIF, Bax and p53. In addition, it blocks the cell cycle at G0/G1, stopping cell proliferation. So far, the results suggest that this compound may have a potential therapeutic effect against leukemia cells.
CoMFA, CoMSIA, HQSAR and Molecular Docking Analysis of Ionone-based Chalcone Derivatives as Antiprostate Cancer Activity
Sharma R, Dhingra N and Patil S
Androgen receptor has been proved to be effective site for treatment of prostate cancer. Molecular modeling methods performed on forty-three ionone based chalcones derivatives as anti-prostate cancer activity. The designed comparative molecular field analysis, comparative similarity indices analysis and hologram quantitative structure activity relationship models produced statistically significant results with the cross-validated correlation coefficients (q(2)) of 0.527, 0.550 and 0.670, non-cross-validated correlation coefficients (r(2)) 0.636, 0.671 and 0.746 and predicted r(2) (Pred r(2)) of 0.621, 0.563 and 0.732, respectively. Furthermore, bioactive conformation was explored and explained by docking of the potent compound 25 into the binding site of androgen receptor. Present study deals with comparative molecular field analysis, comparative similarity indices analysis and hologram quantitative structure activity relationship and molecular docking studies of the ionone-based chalcones and their derivatives, obtained from literature. The model obtained could be effectively used as a channeling tool for further structure modification and designing of some novel potent anti-prostate cancer compounds.
Lead, Cadmium and Nickel Contents of Some Medicinal Agents
Nessa F, Khan SA and Abu Shawish KY
Thirty nine brands of pharmaceutical dosage forms (28 tablets, 4 syrups, 6 suspensions and one chewing gum) that are available in United Arab Emirates pharmaceutical markets were investigated for the presence of three heavy metals; lead, cadmium and nickel. Amongst the samples, 13 products were manufactured locally in United Arab Emirates and 26 products were imported from around the world. The samples were prepared by acid digestion procedure and the resultant solutions were analyzed for heavy metals by using a validated graphite furnace atomic absorption spectrometric method. Calibration curves were achieved using different concentration of lead, nickel and cadmium ranged from 0.001 to 0.05 μg/ml. The mean recoveries of metals from the samples were 86.4 to 97%. The %relative standard deviation for the intraassay and interday precision for the metals were <5%. Amongst the 39 samples of pharmaceutical dosage form all exhibited a positive response for lead, cadmium and nickel except three products whose Ni levels were below quantification level. The products contained variable amounts of heavy metals as of 0.0017 to 11.88 μg lead; 0.0011 to 0.5559 μg cadmium and 0.0011 to 2.6428 μg nickel, respectively. Based on maximum recommended daily dose (g) of these products, maximum daily ingested mass of lead was 0.0034 to 11.88 μg/d, 0.0013 to 0.56 μg/d for cadmium and 0.0011 to 2.64 μg/d for nickel, respectively. The results were compared with those of oral permitted daily exposure levels of United State Pharmacopeial National Formulary 2013. All the products were safe to consume and contained lower level of lead, cadmium and nickel than Oral Permitted Daily Exposure levels, except three products which showed higher level of lead than oral permitted daily exposure levels. Hence the raw materials used in manufacturing of these medicinal agents might be responsible for the presence of higher level of lead.
Vitamin D Supplements in the Indian Market
Lhamo Y, Chugh PK and Tripathi CD
It is now known that vitamin D deficiency is a worldwide health problem. In our country, as food fortification is lacking, supplementation with pharmaceutical preparations is the only means of treatment of vitamin D deficiency. We aimed to study the composition and availability of various vitamin D preparations in the Indian market, data about which was collected from annual drug compendium. The preparations were assessed for total number, different formulations, constituents and amount of each constituent present in the formulation. Vitamin D3 is available in the form of cholecalciferol, alfacalcidiol and calcitriol as single ingredient products and in combination with calcium and other micronutrients. Most of the supplements contain calcitriol (46.5%) or alfacalcidiol (43%) as tablets (51.1%) and capsules (35.2%). Cholecalciferol, the preferred form for prophylaxis and treatment of vitamin D deficient states, constitutes only 10% of the available market preparations. High market sales of calcium supplements containing calcitriol indicate increasing intake of calcitriol rather than cholecalciferol; which could predispose to toxicity. There is a need for marketing and rational prescribing of the appropriate vitamin D supplement in ostensibly healthy Indian population. Implementation of population-based education and intervention programmes with enforcement of strict regulations could generate awareness and curb unsupervised intake of vitamin D containing dietary supplements. This health challenge mandates effective nutritional policies, fortification and supplementation programmes and partnership between government, healthcare and industry to safeguard the health of Indian population at large.
Evaluation of Mosquito Repellent Activity of Isolated Oleic Acid, Eicosyl Ester from Thalictrum javanicum
Gurunathan A, Senguttuvan J and Paulsamy S
To evaluate the traditional use, the mosquito repellent property of Thalictrum javanicum and to confirm the predicted larvicidal activity of the isolated compound, oleic acid, eicosyl ester from its aerial parts by PASS software, the present study was carried out using 4th instar stage larvae of the mosquitoes, Aedes aegypti (dengue vector) and Culex quinquefasciatus (filarial vector). Insecticidal susceptibility tests were conducted and the mortality rate was observed after 24 h exposure. The chitinase activity of isolated compound was assessed by using purified β-N-acetyl glucosaminidase (chitinase). Ecdysone 20-monooxygenase assay (radioimmuno assay) was made using the same larval stage of A. aegyptiand C. quinquefasciatus. The results were compared with the crude methanol extract of the whole plant. The isolated compound, oleic acid, eicosyl ester was found to be the most effective larvicide against A. aegypti (LC50/24 h -8.51 ppm) and C. quinquefasciatus (LC50/24 h - 12.5 ppm) than the crude methanol extract (LC50/24 h - 257.03 ppm and LC50/24 h - 281.83 ppm, respectively). The impact of oleic acid, eicosyl ester on reducing the activity of chitinase and ecdysone 20-monooxygenase was most prominent in both the target species, A. aegyptiand C. quinquefasciatus than the control. The results therefore suggest that the compound, oleic acid, eicosyl ester from Thalictrum javanicum may be considered as a potent source of mosquito larvicidal property.
Moisturizing and Antiinflammatory Properties of Cosmetic Formulations Containing Centella asiatica Extract
Ratz-Łyko A, Arct J and Pytkowska K
Centella asiatica extract is a rich source of natural bioactive substances, triterpenoid saponins, flavonoids, phenolic acids, triterpenic steroids, amino acids and sugars. Thus, many scavenging free radicals, exhibit antiinflammatory activity and affect on the stratum corneum hydration and epidermal barrier function. The aim of the present study was to evaluate the in vivo moisturizing and antiinflammatory properties of cosmetic formulations (oil-in-water emulsion cream and hydrogel) containing different concentrations of Centella asiatica extract. The study was conducted over four weeks on a group of 25 volunteers after twice a day application of cosmetic formulations with Centella asiatica extract (2.5 and 5%, w/w) on their forearms. The measurement of basic skin parameters (stratum corneum hydration and epidermal barrier function) was performed once a week. The in vivo antiinflammatory activity based on the methyl nicotinate model of microinflammation in human skin was evaluated after four weeks application of tested formulations. In vivo tests formulations containing 5% of Centella asiatica extract showed the best efficacy in improving skin moisture by increase of skin surface hydration state and decrease in transepidermal water loss as well as exhibited antiinflammatory properties based on the methyl nicotinate model of microinflammation in human skin. Comparative tests conducted by corneometer, tewameter and chromameter showed that cosmetic formulations containing Centella asiatica extract have the moisturizing and antiinflammatory properties.
Phytochemical Analysis and In vitro Antioxidant Studies of Plumeria obtusa L. Leaves
Dogra NK
Plumeria (Apocynaceae) is a genus comprising mostly of lactiferous trees and deciduous shrubs. Plumeria obtusa L. is a widely available but pharmacologically lesser explored species of this genus. Thus, present research was undertaken to determine the phytochemical constituents and the antioxidant potential of the methanol extract and fractions of the plant. The antioxidant potential was determined using 1,1-diphenyl-2-picrylhydrazyl radical scavenging and inhibition of lipid peroxidation assay.