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   2014| October-December  | Volume 5 | Issue 4  
    Online since October 15, 2014

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Antiinflammatory effects of essential oil from the leaves of Cinnamomum cassia and cinnamaldehyde on lipopolysaccharide-stimulated J774A.1 cells
Chinjarernpan Pannee, Itthipanichpong Chandhanee, Limpanasithikul Wacharee
October-December 2014, 5(4):164-170
DOI:10.4103/2231-4040.143034  PMID:25364694
Cassia oil (CO) from different parts of Cinnamomum cassia have different active components. Very few pharmacological properties of cassia leaf oil have been reported. This study investigated and compared effects of cassia leaf oil and cinnamaldehyde on lipopolysaccharide (LPS)-activated J774A.1 cells. Volatile compositions in cassia leaf oil were identified by gas chromatography-mass spectrometry (MS)/MS. Effects of CO and cinnamaldehyde on LPS-activated J774A.1 cells were investigated by determining nitric oxide (NO) production using Griess reaction assay; expression of pro-inflammatory cytokines, enzymes involve in inflammatory mediators; antiinflammatory cytokines, and iron exporter ferroportin1 (Fpn1) using reverse transcription-polymerase chain reaction; and production of tumor necrosis factor (TNF-α) and interleukin (IL)-10 using ELISA. The main component of CO was cinnamaldehyde. Both oils at 1-20 μg/ml markedly inhibited NO production in LPS-activated J774A.1 cells with IC 50 value of 6.1 ± 0.25 and 9.97 ± 0.35 μg/ml, respectively. They similarly inhibited mRNA expression of pro-inflammatory cytokines and chemokines. These mediators included TNF-α, IL-1β, IL-6, monocyte chemoattractant protein-1, and macrophage inflammatory protein-1α in LPS-activated cells. They also significantly decreased expression of inducible enzymes inducible nitric oxide synthase, cyclooxygenase-2, microsomal prostaglandin-E synthase-1. In the opposite way, they increased mRNA expression and the production of antiinflammatory cytokines IL-10 and transforming growth factor-β. In addition, they promoted the expression of Fpn1. These results demonstrated that inhibitory effects of cassia leaf oil from C. cassia mainly came from cinnamaldehyde. This compound not only inhibited inflammatory mediators but also activated antiinflammatory mediators in LPS-activated J774A.1 cells. It may also have an effect on iron regulatory proteins in activated macrophages.
  12,349 755 30
Recent advances in ocular drug delivery system
Upendra Nagaich
October-December 2014, 5(4):151-151
DOI:10.4103/2231-4040.143022  PMID:25364691
  3,082 9,336 3
In vitro evaluation of anticancer potentials of lupeol isolated from Elephantopus scaber L. on MCF-7 cell line
Daisy Pitchai, Anita Roy, Cybil Ignatius
October-December 2014, 5(4):179-184
DOI:10.4103/2231-4040.143037  PMID:25364696
Lupeol is a triterpenoid, present in most of the medicinally effective plants and possess a wide range of biological activity against human diseases. The present study aims at evaluating the anticancer potentials of lupeol, isolated from the leaves of Elephantopus scaber L. and thereby explores its action on key cancer marker, Bcl-2. The effect of lupeol on the cell viability of MCF-7 was determined by MTT and lactate dehydrogenase assays at different concentrations. The efficacy of the compound to induce cell death was analyzed using AO/EtBr staining. Phase contrast microscopic analysis provided the changes in cell morphology of the compound treated normal breast cells (MCF-10A) and MCF-7 cells. The expression of Bcl-2 and Bcl-xL proteins in the normal, cancer and lupeol treated cancer cell was analyzed by western blotting. Lupeol induced an effective change in the cell viability of MCF-7 cells with IC 50 concentration as 80 μM. Induction of cell death, change in cell morphology and population of the cancer cells was observed in the lupeol treated cells, but the normal cells were not affected. The compound effectively downregulated Bcl-2 and Bcl-xL protein expressions, which directly contribute for the induction of MCF-7 cell apoptosis. Conclusion: Thus, lupeol acts as an anticancer agent against MCF-7 cells and is a potent phytodrug to be explored further for its cytotoxic mechanism.
  5,722 590 39
Comparing the satisfaction and efficacy of Cyclofem and contraceptive pills among females in Northern Iran: A randomized controlled trial study
Bita Jamali, Azade Kiapoor, Mozhgan Firoozbakht, Fatemeh Kazeminavaei, Fatemeh Taghlili
October-December 2014, 5(4):152-157
DOI:10.4103/2231-4040.143025  PMID:25364692
Hormonal contraceptives are the most effective method for birth control, though they may have some default or complications. This research aimed to comparison of the efficacy and satisfaction of Cyclofem with oral contraceptives (OCs) among females. A descriptive-comparative method was conducted on 80 women who were selected through cluster sampling during November 2011-December 2012. The selected subjects start using OCs or Cyclofem for the 1 st time in their life. They evaluated in 2 times frames, at the beginning of the study and then 3 and 6 months after the contraceptive precautions. The data were collected by questionnaire. The data were analysed using parametric and nonparametric test in SPSS 16 software. The reasons for discontinuation of the methods were varied, in which 50% of the sample group were Cyclofem users who discontinued because of menstrual changes and the desire to use other methods, and 50% were the OC users whose reason was medical problems, and absent-mindedness was the last reason for 35.7% of the cases. The efficacy of the both (OCs and Cyclofem) was high and only one unwanted pregnancy occurred at the end of the 6 th month among OC users. There was no significant difference in term of satisfaction of two groups at the end of 3-6 months (PV = 0.433). The results indicated that Cyclofem can be well used by those women who desire for an easy and effective method which is not disturbing the sexual activity and does not also need to be used daily, but the users should be consulted before using the method.
  3,912 1,525 1
Natural polyphenols down-regulate universal stress protein in Mycobacterium tuberculosis: An in-silico approach
M Vijey Aanandhi, Debojit Bhattacherjee, P Samuel Gideon George, Anirban Ray
October-December 2014, 5(4):171-178
DOI:10.4103/2231-4040.143036  PMID:25364695
Universal stress protein (USP) is a novel target to overcome the tuberculosis resistance. Our present study enlightens the possibilities of some natural polyphenols as an antioxidant for USP. The study has shown some molecular simulations of some selected natural antioxidants with USP. We have considered USP (Rv1636) strain for homology modeling and the selected template was taken for the docking study. Curcumin, catechin, reservetrol has shown ARG 136 (1.8Ε) hydrogen bonding and two ionic bonding with carboxyl group of curcumin with LEU 130 (3.3Ε) and ASN 144 (3.4Ε) respectively. INH was taken for the standard molecule to perform molecular simulation. It showed poor binding interaction with the target, that is, −5.18 kcal, and two hydrogen bonding with SER 140 (1.887Ε), ARG 147 (2.064Ε) respectively. The study indicates possible new generation curcumin analogue for future therapy to down-regulate USP.
  4,566 467 7
Synthesis, characterization, antimicrobial, and pharmacological evaluation of some 2, 5-disubstituted sulfonyl amino 1,3,4-oxadiazole and 2-amino-disubstituted 1,3,4-thiadiazole derivatives
Dilipkumar Pal, Rohit Tripathi, Desh Deepak Pandey, Preety Mishra
October-December 2014, 5(4):196-201
DOI:10.4103/2231-4040.143040  PMID:25364699
The presence of heterocyclic structures in diverse types of compounds, this is strongly indicative of the profound effect like structure exerts on physiologic activity, and recognition of this is abundantly reflected in efforts to find useful synthetic drugs. The search for better pharmacological active drug and the importance of disubstituted 1,3,4-oxadiazole and 1,3,4-thiadiazole as active pharmacophores, prompted us to design, synthesize, characterize, and evaluate a series of differently substituted sulfonyl amino 1,3,4-oxadiazole and 1,3,4-thiadiazole for their potential antimicrobial, analgesic and antiinflammatory activity, respectively. New sulfonyl amino 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives were synthesized by intramolecular cyclization of thiosemicarbazide in alkaline medium. Reactions were carried out by the reaction between aromatic carbonyl halide and thiosemicarbazide.
  3,810 527 12
Quercetin declines plasma exposure of metoprolol tartrate in the rat model
Siva R Challa, Venkatesh R Challa, Satheesh K Ragam
October-December 2014, 5(4):185-190
DOI:10.4103/2231-4040.143038  PMID:25364697
The study was undertaken to evaluate the effect of quercetin on the pharmacokinetics of Metoprolol tartrate. A single dose in vivo pharmacokinetic study was carried out in rat models. In this study, rats were treated with quercetin (10 mg/kg) and metoprolol tartrate (20 mg/kg) orally and blood samples were collected 0, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 8, 12 h post treatment. Plasma concentration of metoprolol tartrate was estimated using reverse phase-high-performance liquid chromatography method. Area under the plasma concentration-time curve (AUC 0-12 ) of metoprolol has significantly (P < 0.001) decreased by 9.8 times in the metoprolol and quercetin combination group (9434.65 ± 3525.02) when compared with AUC 0-12 metoprolol of metoprolol-alone treated group (962.17 ± 242.81). AUC 0-∞ of metoprolol has significantly (P < 0.001) decreased by 14.9 times in the combination group (16670.79 ± 12129.06) in comparison to AUC 0-∞ of metoprolol of metoprolol-alone treated group (1113.68 ± 441.83). the results obtained herein indicate that quercetin remarkably declines the plasma exposure of metoprolol when concomitantly administered by oral route.
  3,398 301 2
Pasteurization as a tool to control the bio-burden in solid herbal dosage forms: A pilot study of formulating Ashoka tablets with an industrial perspective
Hulikal Basavarajaiah Pushpalatha, Kumar Pramod, Ramachandran Sundaram, Ramakrishnan Shyam
October-December 2014, 5(4):191-195
DOI:10.4103/2231-4040.143039  PMID:25364698
Irradiation and use of preservatives are routine procedures to control bio-burden in solid herbal dosage forms. Use of steam or pasteurization is even though reported in the literature, not many studies are available with respect to its application in reducing the bio-burden in herbal drug formulations. Hence, we undertook a series of studies to explore the suitability of pasteurization as a method to reduce bio-burden during formulation and development of herbal dosage forms, which will pave the way for preparing preservative-free formulations. Optimized Ashoka (Saraca indica) tablets were formulated and developed. The optimized formula was then subjected to pasteurization during formulation, with an aim to keep the microbial count well within the limits of pharmacopoeial standards. Then, three variants of the optimized Ashoka formulation - with preservative, without preservative and formulation without preservative and subjected to pasteurization, were compared by routine in-process parameters and stability studies. The results obtained indicate that Ashoka tablets manufactured by inclusion of the pasteurization technique not only showed the bio-burden to be within the limits of pharmacopoeial standards, but also exhibited the compliance with other parameters, such as stability and quality. The outcome of this pilot study shows that pasteurization can be employed as a distinctive method for reducing bio-burden during the formulation and development of herbal dosage forms, such as tablets.
  3,067 256 1
Ciprofloxacin monoolein water gels as implants for the treatment of chronic osteomyelitis: In vitro characterization
Bavouma Charles Sombié, Josias Gérard Yameogo, Rasmané Semdé, Viviane Henschel, Karim Amighi, Jonathan Goole
October-December 2014, 5(4):158-163
DOI:10.4103/2231-4040.143029  PMID:25364693
This work investigated the possibility of using the biodegradable gentamicin-monoolein-water gels as models, in order to obtain a similar sustained release of ciprofloxacin hydrochloride. Four gels containing antibiotics were prepared and were examined with regard to their physicochemical properties and in vitro drug release characteristics. Ciprofloxacin, unlike gentamicin, which was dissolved in the matrix, was in dispersed form. However, despite its insolubility, microscopic observation, differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), and X-ray diffraction showed that the developed gel was in the cubic liquid crystalline structure and have maintained their ability to progressively release ciprofloxacin. ciprofloxacin-monoolein-water (5:80:15% w/w), which released in vitro approximately 85% of ciprofloxacin after 16 days could possibly be considered as an alternative to a gentamicin-monoolein-water gel for the treatment of chronic osteomyelitis.
  1,367 216 3