Osteoarthritis (OA) is an old age disease and caused by both biochemical and mechanical factors. Nitric oxide (NO), is a metabolic product of L-arginine produced by nitric oxide synthase (NOS). NO and its derivatives were found to have a number of different functions in both normal and pathophysiological joint conditions. According to recent studies excessive production of NO by excessive iNOS (inducible nitric oxide synthase) stimulation is responsible for several pathological conditions including OA. We conducted clinical study on 150 female patients suffering from OA with age group 45 – 65 years (mean age 55.5 years) to find out whether the levels of nitric oxide are associated with OA. Nitrite levels were measured in the serum as marker of nitric oxide (NO) production by assay method based on Griess assay method. In OA patients serum nitrite levels were much higher (116.8µmol/L) as compared to control subjects (48.6µmol/L) (p<0.001). At the end of the clinical study we conducted structure based drug designing (molecular docking study) for the in silico search of new iNOS inhibitors as it is involved in the excessive formation of NO which ultimately cause osteoarthritis.
Currently, there is demand for the development of herbal sunscreen formulations to suppress harmful effects of UV rays. In this regard, this study, was conducted to investigate the sun screen potential of Sri Lankan Orthodox black tea (made from buds and top most leaves of Camellia sinensis L plant) using three grades (Dust No:1, Broken Orange Pekoe and Orange Pekoe) using UV spectroscopic technique and Mansur equation. Sun Protection Factor (SPF) value was determined using 20% aqueous extracts (Black tea brews). The results revealed that all three tea samples had markedly high absorbance values (1.4 to 4.2) at 290-320 nm range and SPF values above 15 which are considered as the threshold value for good sunscreen. The SPF value of Dust No:1, B.O.P.F and O.P were respectively 36, 23 and 22. This is a novel finding for Sri Lankan black tea. It is concluded that Sri Lankan black tea, especially, Dust No: 1 can function as an efficient sunscreen agent and has great promise to be developed as cheap, safe and effective topical botanical sunscreen acting via multiple mechanisms (considering its other reported bioactivities).
Keywords : Black tea, Dust No: 1, Broken Orange Pekoe, Orange Pekoe, sunscreen, photo-protection, sun protection factor, Camellia sinensis
A Simple sensitive and specific tandem mass spectrometric (LC-MS/MS) method for the determination of penbutolol (PEN) and its metabolite 4-Hydroxy penbutolol (4HPEN) in human plasma was developed and validated. The detection of the analytes was achieved in positive ion in selected reaction monitoring (SRM) mode. The deuterated compounds of the analytes were used as internal standards (IS). The extraction procedure involved solid phase extraction of PEN, 4HPEN and IS from plasma by using Strata-X cartridges. The chromatographic separation of PEN, 4HPEN and IS was carried out on a Chromatopak C18 column with 5mM ammonium acetate (pH 4.5) buffer and acetonitrile (15:85, v/v) as the mobile phase under isocratic conditions at a flow rate of 0.6 mL/min. The nominal retention times obtained for PEN, 4HPEN, DPEN and D4HPEN were 2.42, 1.98, 2.40 and 2.00 minutes respectively. The lower limit of quantification for PEN and 4HPEN were 0.2 and 0.1 ng/mL respectively. The standard curves were linear (r2>0.99) over the concentration range of 0.2-302.7 ng/mL for PEN and 0.1-30.0 ng/mL for HPEN. Method validation was performed as per FDA guidelines and the obtained results met the acceptance criteria. The proposed method was found to be acceptable to a pharmacokinetic study in human volunteers.
Keywords : Penbutolol, 4-Hydroxy Penbutalol LC-MS/MS, Human plasma and Pharmacokinetics.
Author : Venkata Kumar Ch, Nagamalleswara Rao K, Madhuri K , Anil Kumar Ch and Kesava Rao T KV
Title : A quantitative determination of penbutolol and its metabolite in plasma by liquid chromatography tandem mass and its application to pharmacokinetic studies
Sulfonamides are considered to be pharmaceutically important class of compounds. In the present work, N-(2,4-dimethylphenyl)-4-toluenesulfonamide (3) was synthesized by the reaction of 2,4-dimethylaniline (1) and 4-tosyl chloride (2; 4-methylbenzenesulfonyl chloride) using 10% aqueous Na2CO3 solution as reaction medium. At the second step, the synthesized molecule 3 was made to react with different alkyl/aralkyl halides (4a-o) to yield the target compounds, 5a-o, using N,N-dimethylformamide (DMF) as reaction medium and lithium hydride as an activator. The synthesis of all the compounds was verified by spectral techniques using IR, 1H-NMR and EIMS; and further examined for their anti-enzymatic activities. The synthesized compound 5f represented a suitable inhibitory potential against α-glucosidase and lipoxygenase enzymes.
The crude methanol extracts of aerial parts of Abrus precatorius L., leaf of Magnolia pterocarpa Roxb., Dracaena spicata Roxb. and Ravenala madagascariensis Sonn. as well as their hexane, carbon tetrachloride, chloroform and aqueous soluble partitionates were subjected to screenings for disc diffusion assay. Among the test samples of A. precatorius, the highest zone of inhibition (15.0mm) was exhibited by the carbon tetrachloride soluble fraction against Pseudomonas aeruginosa. The M. pterocarpa extractives exhibited significant zone of inhibition ranging from 7.0 to 23.0mm against the test organisms. The highest zone of inhibition (23.0mm) was demonstrated by the carbon tetrachloride soluble fraction against Pseudomonas aeruginosa. This fraction also exhibited 20.0mm zone of inhibition against the gram positive bacteria Staphylococcus aureus and gram negative bacteria Vibrio parahemolyticus. Among the test samples of D. spicata, the highest (18.0mm) zone of inhibition was demonstrated by the aqueous soluble fraction against Pseudomonas aeruginosa. The test samples of R. madagascariensis exhibited weak antimicrobial activity with zone of inhibition ranging from 2.0 to 9.0mm.
Keywords : Abrus precatorius L. Magnolia pterocarpa Roxb. Dracaena spicata Roxb. Ravenala madagascariensis Sonn. Disc diffusion method. Zone of inhibition. Ciprofloxacin
Author : Tasnuva Sharmin, Sharmin Reza Chowdhury, Md. Yeunus Mian, Masbahul Hoque, Md. Sumsujjaman, and Faijun Nahar
Title : Evaluation of antimicrobial activities of some Bangladeshi medicinal plants
A new economic, industrially acceptable and readily adaptable method has been developed following a complexation (acid-dye method) between antiepileptic drugs and Bromocresol green (BCG) dye and validated for determination of this drug in bulk and its pharmaceutical dosage form. Drug used during analysis i.e. Rufinamide was reacted with BCG in presence of hydrochloric acid buffer pH 1.2. The colored complex formed was extracted with chloroform and the absorbance of the solutions were noted which followed a beer’s law in concentration range of 10-50 μg/ml for Drug-BCG complex with correlation coefficient close to 0.991. The method was validated as per ICH guideline for accuracy, precision, limit of detection and limit of quantification. The developed Spectrophotometric method has the advantages of speed, simplicity, sensitivity and more affordable instrumentation and could find application as a rapid and sensitive analytical method for Rufinamide.
Keywords : Extractive Spectrophotometry, Acid-dye method, Rufinamide, Bromo cresol Green
Author : Apexa Patel, Bhanubhai Suhagia
Title : Extractive spectrophotometric method for determination of rufinamide in bulk and its pharmaceutical dosage form
Osteoporosis is a multi-factorial disease characterized by reduced bone mass and impaired micro-architecture, leading to an increased susceptibility to fractures. The objective of present study was to evaluate anti-osteoporotic activity of Bonton Active Granules in ovariectomized rat model at two different dose levels i.e. Therapeutic Effective Dose (TED) 0.9 g/kg/day and double the dose (TED×2) 1.8 g/kg/day. 24 healthy female wistar rats were divided into 4 groups where each group was containing 6 animals. Group-1 was considered as a normal control group fed with 1% Carboxy Methyl Cellulose (CMC) suspension. Group-2, a Disease control group was containing ovariectomized (OVX) rates fed with 1% CMC suspension. Group 3 and 4 were orally treated with test drug at TED (0.9 g/kg/day) and TED×2 (1.8 g/kg/day) respectively. Present study included parameters like serum alkaline phosphatase (ALP), serum calcium, femoral bone parameters, bone breaking strength, body weight and histopathological study of bone. Treatment with Bonton Active Granules at both dose levels showed significant decrease in serum ALP and significant increase in serum calcium level. It also showed significant changes in femoral parameters and histopathology of bone. Hence, it can be inferred that Bonton Active Granules at both experimented therapeutic doses provides good anti-osteoporotic activity against ovariectomized rat.
Keywords : Bonton Active Granules, ovariectomized rat, anti-osteoporotic activity
Author : Soni Hardik, Kandachia Jalak, Jani Deepti, Patel Ghanashyam
Title : Evaluation of bonton active granules for anti-osteoporotic activity in ovariectomized rat
Influence of host plants on the carotenoid profile of Loranthus longiflorus leaf and bark samples collected from Casuarina equisetifolia and Ficus religiosa host trees were determined by HPTLC method. The methanol extract of L. longiflorus leaf samples obtained from C. equisetifolia host trees showed 9 compounds while it was 8 compounds in the leaf samples collected from F. religiosa host tree. Among the compounds, 5 and 3 compound in each sample, respectively, was identified as carotinoids while the others were unknown. Four compounds from each leaf samples collected from C. equisetifolia (peak no. 4- 6 & 8) and F. religiosa (peak no. 1-3 & 6) host trees showed similar Rf values (0.15, 0.19, 0.23 & 0.53, respectively). Similarly, the methanol extract of L. longiflorus bark sample collected from C. equisetifolia and F. religiosa host trees contained 8 compounds each. Of these compounds only 3 from each sample was identified as carotenoids whereas others were unknown and none of these compounds showed any similar Rf values. One compound from leaf and park samples of L. longiflorus collected from C. equisetifolia (peak no. 6 & 4) and F. religiosa (peak no. 4 & 3) showed similar Rf values (0.23 & 0.26), respectively.