bluuebunny/crossref_metadata_2025 huggingface dataset:
SYNTHESIS AND CHARACTERIZATION OF CYCLOHEXANE-1,3-DIONE DERIVATIVES AND THEIR IN SILICO AND IN VITRO STUDIES ON ANTIMICROBIAL AND BREAST CANCER ACTIVITY
Authors: CHINNAMANAYAKAR RAJA , MR EZHILARASI , B PRABHA , M KULANDHAIVEL
Published: October 2019

Objective: The objective of this study was to evaluate in silico and in vitro anticancer activity for synthesized cyclohexane-1,3-dione derivatives.

Methods: The new series of cyclohexane-1,3-dione derivatives were synthesized based on the Michael addition reaction. Further, the structures of the synthesized compounds were confirmed by Fourier-transform infrared spectroscopy, 1H nuclear magnetic resonance (NMR), and 13C NMR spectral data. Then, the in silico molecular docking studies were carried out using AutoDock tool version 1.5.6 and AutoDock version 4.2.5.1 docking program. The antimicrobial activity was carried out using the agar disk diffusion method, and the in vitro anticancer activity was performed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay for the synthesized compound.

Results: In silico docking study, compound 5c showed good binding score and binding interactions with selected bacterial proteins and breast cancer protein. Further, compound (5a-5h) was tested for their antimicrobial activity and compound 5c was only tested for anticancer activity (human breast adenocarcinoma 3,4-methylenedioxyamphetamine-MB-231 cell line). Compound 5c was found to be the most active one of all the tested compounds. In the MTT assay compound, 5c showed the LC50 value of 10.31±0.003 μg/ml. In antimicrobial activity, the minimum inhibitory concentration of compound 5c is 2.5 mg/ml.

Conclusion: An efficient synthesis of biologically active cyclohexane-1, 3-dione derivatives has been developed.
COUMARINS: A UNIQUE SCAFFOLD WITH VERSATILE BIOLOGICAL BEHAVIOR
Authors: GUPTA MANDEEP KUMAR , KUMAR SUSHIL , CHAUDHARY SACHIN
Published: October 2019

Benzopyrones are the club of compounds that can be coumarins or flavonoids. The hydroxyl derivatives of coumarins such as 4-hydroxycoumarins and 7-hydroxycoumarins have extensive biological activities which have employed for the synthesis of miscellaneous coumarin derivatives. These derivatives have exhibited impressive pharmacological and physiological activities such as anticoagulant, antibacterial, antiviral, antitumor, bactericidal, fungicidal, anti-inflammatory agents, and anti-HIV activity. This review comprised pharmacokinetic studies, including absorption, distribution, and metabolism of coumarin analogs along with toxicological studies. The studies of coumarins and their derivatives exhibiting immense pharmacological activity are also summarized in the current study.
EVALUATION OF ANTIPSORIATIC ACTIVITY OF AQUEOUS EXTRACT OF BRASSICA OLERACEA VAR. CAPITATA AND ETHANOLIC EXTRACT OF MENTHA SPICATA LEAVES ON IMIQUIMOD-INDUCED PSORIASIS-LIKE DERMATITIS
Authors: HUSNA S AYESHA , V JAYASANKAR REDDY
Published: October 2019

Objective: The objective of this study is to evaluate the antipsoriatic activity of aqueous extract of Brassica oleracea var. capitata leaves (BOAE) and ethanolic extract of Mentha spicata leaves (MSEE) on Imiquimod-induced Psoriasis-like dermatitis.

Methods: Imiquimod induction method for psoriasis-like dermatitis was used for the evaluation of antipsoriatic activity. Extracts were tested at a dose of 100 mg/kg body weight (b.wt.) and 400 mg/kg b.wt. in Swiss albino mice. These test doses were compared with the Retino-A (0.025%) treated group which serves as a standard group. Parameters studied in the test include changes in body weight, spleen weight and spleen index, neutrophils, lymphocytes, eosinophils, monocytes, hemoglobin, red blood cells, platelets, packed cell volume, mean corpuscular volume, mean corpuscular hemoglobin (MCH), MCH concentration, epidermal thickness, erythema, desquamation, skin thickness, superoxide dismutase, catalase, lipid peroxidation of skin and percentage orthokeratotic values, drug activity, and relative epidermal thickness.

Results: MSEE at dose of 400 mg/kg b.wt has shown more effect when compared with MSEE at low dose, BOAE topical and oral.

Conclusion: From the study, it was concluded that the above extracts have promising anti-psoriatic activity.
SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT OF EZETIMIBE BY SOLID DISPERSION AND PELLETIZATION TECHNIQUES
Authors: KUNAM VISWANADH , SURYADEVARA VIDYADHARA , RAO GARIKAPATI DEVALA , MANDAVA VENKATA BASAVESWARA RAO , SUNKARA SIVA PRASAD
Published: October 2019

Objective: In the present investigation, an attempt was made to improve the surface characters and solubility of the drug by solid dispersion and coating it on the non-pareil sugar beads as pellets.

Methods: Ezetimibe solid dispersions were prepared by solvent evaporation technique using Kollidon VA64 as binder and solubility enhancer. Crospovidone as disintegrant and ethanol was used as solvent. Ezetimibe pellets were prepared by dissolving ezetimibe, kollidonVA64, and crospovidone in ethanol in different ratios and coated on non-pareil sugar beads as a drug layer by pan coating technique.

Results: All the formulations were further evaluated for physicochemical parameters such as particle size, friability, angle of repose, and drug content. In vitro dissolution studies were carried out in 1% sodium lauryl sulfate using USP apparatus II.

Conclusion: It was observed that the dissolution rate of the solid dispersion formulation ESD5 showed better dissolution rate to the extent of 1.05 folds and 1.824 folds when compared to a marketed formulation and pure drug, respectively. Similarly, formulation EPL5 containing 1:5 ratio of ezetimibe to Kollidon VA64 showed improved dissolution rate to the extent of 1.091 folds and 1.986 folds when compared to the marketed formulation and pure drug, respectively. Majority of the formulations displayed first-order release kinetics and were found to be linear with R2 values in the range of 0.874–0.993. Fourier transform infrared analysis revealed that there was no major interaction between the drug and excipients used in the design of formulation. Scanning electron microscopy analysis was performed for solid dispersions, pellet formulations, and its polymers to determine the surface characteristics.
CORRELATIONS BETWEEN CLUSTER DIFFERENTIATION 4 COUNTS, HUMAN IMMUNODEFICIENCY VIRUS CLINICAL STAGES, AND HEMOGLOBIN LEVEL AMONG HUMAN IMMUNODEFICIENCY VIRUS PATIENTS WITH ANEMIA IN MERPATI CLINIC, WANGAYA HOSPITAL, DENPASAR, BALI, INDONESIA: A CROSS-SECTI
Authors: SURYANA KETUT , SUHARSONO HAMONG , BUDIASA GEDE , ANTARA JARWA , ASTUTI PUJI , INDAH IDA AYU , STUTI PUTRI
Published: October 2019

Objective: The objective of this study was to determine the correlation between cluster of differentiation 4 (CD4) counts, human immunodeficiency virus (HIV) clinical stages, and hemoglobin (Hb) level among HIV-infected patients with anemia.

Methods: A cross-sectional study was conducted in November 2017 at Merpati Clinic of Wangaya Hospital, Denpasar, Bali, Indonesia. We selected 79 HIV patients with anemia to participate in our study. We grouped CD4 counts into two categories: <200 cells/μL and ≥200 cells/μL, and we classified the HIV clinical stages into HIV and acquired immunodeficiency syndrome (AIDS).

Results: About 55.7% (44) of men and 44.3% (35) of women were participated in this study. As many as, 91.1% (72) of participants were AIDS patients. The mean Hb was 8.77 g/dl with SD 1.79 g/dl. 81% (64) of study participants were suffered from anemia on chronic disease or inflammatory anemia, and 19% (15) of study participants were suffered from iron deficiency anemia. The median for CD4 counts was 94 cells/μL (3–309 cells/μL) with as many as 78.5% (62) of participants were found to have low CD4 counts (<200 cells/μL). Spearman analysis revealed a positive correlation between CD4 counts and Hb level (r=0.427, p<0.001). Independent sample t-test analysis found a correlation between the HIV clinical stages and Hb level. There was a difference between the mean of Hb level in each stage with the average difference of 0.8 g/dl (95% confidence interval 0.04–1.6; p<0.04).

Conclusions: There is a correlation between CD4 counts, HIV clinical stages, and Hb level among HIV patients with anemia.
ANTIOXIDANT AND ANTI-INFLAMMATORY EFFECTS OF CURCUMIN CONTRIBUTE INTO ATTENUATION OF ACUTE GENTAMICIN-INDUCED NEPHROTOXICITY IN RATS
Authors: AL-KURAISHY HAYDER M , AL-GAREEB ALI I , RASHEED HUDA ABDULBAKI
Published: October 2019

Objectives: Nephrotoxicity is a renal-specific situation in which the excretion of toxic metabolites is reduced due to toxic agents and drugs. Gentamicin is an antibiotic belongs to aminoglycoside group which may induce nephrotoxicity due to induction of oxidative stress. Curcumin is a component of traditional medicine with significant nephroprotective effect. Therefore, the objective of the present study was to evaluate the nephroprotective effect of curcumin on gentamicin-induced nephrotoxicity.

Methods: A total of 30 male Sprague-Dawley rats were used which divided into Group 1 (n=10): Rats treated with distilled water 5 ml/kg plus normal saline 5 ml/kg for 12 days, Group 2 (n=10): Rats treated with distilled water 5 ml/kg plus gentamicin 100 mg/kg for 12 days, and Group 3 (n=10): Rats treated with curcumin 100 mg/kg plus gentamicin 100 mg/kg for 12 days. Blood urea, serum creatinine, malondialdehyde (MDA), kidney injury molecule (KIM-1), and cystatin-C were measured in both control and experimental groups.

Results: Rats treated with gentamicin showed nephrotoxicity as evident by significant elevation in blood urea, serum creatinine, KIM-1, MDA, and cystatin-C sera levels. Curcumin leads to significant reduction of blood urea and serum creatinine compared to gentamicin group, p<0.05. Curcumin also reduced MDA, KIM-1, and cystatin-C sera levels significantly compared to gentamicin group, p<0.01.

Conclusion: Curcumin produced significant nephroprotective effect on gentamicin-induced nephrotoxicity through modulation of oxidative stress and inflammatory biomarkers.
CARDIOPROTECTIVE EFFECT OF FISETIN ON LYSOSOMAL ENZYME ACTIVITIES OF NORMAL AND ISOPROTERENOL-INDUCED MYOCARDIAL INFARCTION IN MALE WISTAR RATS
Authors: PANNEERSELVAM MYTHILY , P. T DEVIKA
Published: October 2019

Objective: This study aims to evaluate the cardioprotective effect of fisetin on change in the activities of lysosomal enzymes in isoproterenol (ISO)- induced myocardial infarction (MI) in male albino Wistar rats.

Methods: Rats were orally pretreated with fisetin (30 mg/kg body weight) daily for 30 days. After the pretreatment period, ISO (100 mg/kg body weight) was subcutaneously administered to rats at intervals of 24 h for 2 consecutive days.

Results: The activities of β-glucuronidase, β-N-acetylglucosaminidase, β-galactosidase, cathepsin-B, and cathepsin-D were significantly (*p<0.05) increased in serum and the heart of ISO-induced rats. Pre-treatment with fisetin daily for 30 days to ISO-induced rats significantly prevented these activities and restored their activities to near normal. Oral treatment with fisetin (30 mg/kg body weight) to normal control rats did not show any significant effect.

Conclusion: We have concluded that fisetin protects the β-glucuronidase, β-N-acetylglucosaminidase, β-galactosidase, cathepsin-B, and cathepsin-D against ISO-induced MI. The observed effects might be due to the free radical-scavenging and membrane-stabilizing effect of fisetin.
TINOSPORA CORDIFOLIA AQUEOUS EXTRACT AMELIORATES THE SYSTEMIC INFECTION OF ASPERGILLUS FUMIGATUS IN BALB/C MICE
Authors: A KHAN MASOOD
Published: October 2019

Objective: The present study was aimed to assess the antifungal activity of Tinospora cordifolia aqueous extract (TCAE) against Aspergillus fumigatus infection.

Methods: TCAE was tested for in vitro antifungal activity against the isolates of A. fumigatus, Aspergillus flavus, and Aspergillus niger. To evaluate in vivo activity, various doses (10, 25, and 50 mg/kg) of TCAE were orally administered in A. fumigatus-infected mice for 7 days. The combination of prophylactic and therapeutic effect of TCAE was assessed by pre-treating the mice with 10 mg/kg of TCAE for 3 consecutive days before exposing them to A. fumigatus. Mice were treated with 10, 25, and 50 mg/kg doses of TCAE for 7 consecutive days’ post-A. fumigatus infection. The effectiveness of TCAE was evaluated by monitoring the survival rate and assessing the fungal burden in the kidney of the treated mice.

Results: A. fumigatus-infected mice treated with TCAE at the doses of 25 and 50 mg/kg exhibited 50% and 20% survival rate, respectively, observed on day 40 post-treatment. Like to the survival data, the fungal burden was also found to be the lowest in the kidney of mice treated with TCAE at a dose of 50 mg/kg. The results showed that pre-treatment with TCAE (10 mg/kg) followed by post-infection treatment with 10, 25, and 50 mg/kg of TCAE for 7 days resulted in 40%, 50%, and 70% survival rate, respectively.

Conclusions: These results suggest that TCAE may potentially be considered for its possible use in the treatment of the systemic infection of A. fumigatus.
EFFECTS OF SUNFLOWER SEEDS ON CHOLESTEROL AND LOW-DENSITY LIPOPROTEIN LEVELS IN PATIENTS WITH DYSLIPIDEMIA
Authors: B CHEENAM , P LEENA , K VIKAS
Published: October 2019

Objective: The present study was conducted with a goal to analyze and assess the effect of sunflower seeds on the serum cholesterol and low-density lipoprotein (LDL) levels.

Methods: A total of 60 patients comprising 34 males and 26 females were selected for the given study. The patients were divided into case and control groups. Various anthropometric measurements such as weight, height, and blood pressure along with certain biochemical parameters including cholesterol and LDL were recorded for these patients pre- and post-supplementation of 2 g of sunflower seeds for 6 months.

Results: The patients in the experimental group showed a significant and rapid difference (p<0.05) in comparison to the control intervention. The cholesterol levels in the case group reduced from 254.6±21.40 to 183.40±3.01 mg/dl, whereas, in control group, it reduced from 234.53±13.54 to 194.50±6.16 mg/dl. Similarly, the LDL levels in the case group decreased from 155.28±8.48 to 122.70±2.94 mg/dl; in contrast, in control group, it decreased from 159.53±6.04 to 140.53±1.11 mg/dl, respectively.

Conclusion: The study conducted concluded that sunflower seeds can be used as an adjuvant in treating the raised cholesterol and LDL levels in the blood serum which could otherwise lead various cardiac disorders (both major and minor).
DEVELOPMENT AND EVALUATION OF AN IN SITU THERMOGELLING SYSTEM OF OFLOXACIN FOR CONTROLLED OCULAR DELIVERY
Authors: PRABHU ANANTH , KOLAND MARINA
Published: October 2019

Objective: The purpose of this study was to develop an in situ ocular gel of ofloxacin which aimed to prolong corneal residence time while controlling drug release.
Method: In situ gelling solutions were prepared from Poloxamer 407, a temperature-sensitive gelling polymer and to which, mucoadhesive polymers such as hydroxypropyl methyl cellulose 15 cps and polyvinyl alcohol (PVA) were included to provide corneal adhesion. Drug incorporated gels were prepared and evaluated for their appearance, pH, gelation temperature, and in vitro drug release studies.
Results: Incorporation of the drug into the formulation increased the gelation temperature while the addition of mucoadhesive polymers decreased the gelation temperature. Increasing the concentration of bio-adhesive polymers retarded the release of ofloxacin from the poloxamer solutions and drug release was sustained over a period of 9 h. PVA had no significant effect on the gelation temperature and could not sustain the drug release for a longer duration. The in vitro release profiles of the drug from all the formulations could be best expressed by Higuchi’s equation which indicated that gels followed matrix diffusion process and drug release from gel formulations followed first-order process.
Conclusion: The results showed that the developed system would be promising in the treatment of ocular infections with the combined advantages of ease of administration, the accuracy of dosing, increased bioavailability, and prolonged retention time.
EFFECT OF OPUNTIA ELATIOR ON CHOLESTEROL LEVEL ALTERATIONS INDUCED BY GAMMA RADIATION IN SWISS ALBINO MICE
Authors: POONIAM KAVITA , SHARMA JAIMALA
Published: October 2019

Objectives: Radiotherapy is deleterious to patient health by making the patient more susceptible to other diseases and often causes death by weakening the immune system and also affects cholesterol level. Based on these studies, it was moved toward the selection of Opuntia elatior as a herbal remedy for serum cholesterol level induced by gamma radiation.

Methods: The modulatory effect of O. elatior stem extract was studied in Swiss albino mice at dose, i.e., 6 Gy of gamma radiation in the presence (experimental) or absence (control) of O. elatior extract (OEE) (10 mg/kg body weight) to observe in blood cholesterol level alterations. The animals were scarified and their blood was collected at days 1, 15, and 30 post-irradiation from heart puncture. Cholesterol level was estimated by the modified method of Roeschlau et al., 1974, using kit.

Results: The cholesterol level was found almost constant in the control group (without any treatment) and increased in gamma radiation-treated group and decreased in only plant extract-treated group, whereas radiation-induced increased level of cholesterol was reduced by plant extract treatment in experimental animals (in plant extract with radiation-treated group), a normal level was achieved by day 30 post-treatment. Hence, O. elatior is beneficial to control radiation-induced blood cholesterol level.

Conclusion: Radiation-induced side effects get lowered by herbal treatment and herbal products do not have their own side effects on body on their physical and chemical processes; thus, OEE is useful to manage blood cholesterol level as an edible part, it is easy to use as treatment and in my results OEE also support to maintain cholesterol level in serum of mice.
Challenges and Opportunities of Nuclear Medicine in Health Care
Authors: Gupta Arun K.
Published: October 2019

AERB Sponsored National Seminar

Challenges and Opportunities of Nuclear Medicine in Health Care

(Saturday 02 February 201

Organized by-Chameli Devi Institute of Pharmacy, Indore
FORMULATION AND EVALUATION OF PRONIOSOMAL GEL-BASED TRANSDERMAL DELIVERY OF ATORVASTATIN CALCIUM BY BOX–BEHNKEN DESIGN
Authors: SOUJANYA C  , RAVI PRAKASH P
Published: October 2019

Objective: The aim of this study was to investigate the combined influence of three independent variables in the preparation of atorvastatin proniosomes by coacervation-phase separation method.

Methods: On the basis of the preliminary trials, a 3-factor, 3-level Box–Behnken design was employed to study the effect of cholesterol, soya lecithin, and Span 60 independent variable on dependent variables (particle size and % entrapment efficiency). Transmission electron microscopy analysis of optimized formulation has demonstrated the presence of individual proniosomes in spherical shape.

Results: Atorvastatin optimized proniosomal formulation F2 shown better particle size and % entrapment efficiency, and also, the drug release was 99.72% within 24 h in slow and controlled manner when compared with control. Kinetic analysis of drug release profiles showed that the drug release was followed by zero-order manner with Korsmeyer–Peppas model, which implies super case II release kinetics. The particle size and zeta potential of the optimized atorvastatin proniosomal gel were found to be 65.72 and −10.5, respectively. The optimized batch of proniosomes was used for the preparation of atorvastatin-based proniosomal hydrogel by incorporating hydrated proniosomes to carbopol matrix to enhance the stability and viscosity of the system.

Conclusion: The enhanced skin permeation, for a prolonged period of time, may lead to improved efficacy and better patient compliance. This study suggests that proniosomal gel-containing atorvastatin could perform therapeutically better effects than the conventional formulations.
PECULIAR PROPERTIES OF THE PLANT TAXONOMY AT THE HERBARIUMMUSEUM DEPARTMENT PHARMACEUTICAL AND NATURAL SCIENCES FIRST MOSCOW STATE MEDICAL UNIVERSITY NAMED AFTER SECHENOV
Authors: SAMYLINA IA  , ERMAKOVA VA  , STRELIAEVA AV  , KARTASHOVA NV
Published: October 2019

Objective: Department of Pharmaceutical and Natural Sciences of Sechenov First Moscow State Medical University offers students herbarium which should be attributed to special herbaria, namely the collection contains medicinal plants that are well known as official medicine and are widely used in folk medicine. The herbarium provides samples of medicinal plants for the formation of knowledge, practical skills of students of the pharmaceutical faculty. More than 7000 copies of herbarium sheets are offered for the work of students.

Methods: Herbarium samples were identified and selected according to the engage thematic plan: Medicinal plants containing essential oils, cardiac glycosides, saponins, polysaccharides, phenolic glycosides, coumarins, lignans, flavonoids, tannins, anthracene derivatives, vitamins, fatty oils, and different groups of biologically active substances. In addition, the department made a small collection of the rare herbarium, which presents medicinal plants widely used in homeopathy, which is used for conducting elective discipline. The wide research of different branches of the medicinal plan was made with the help of pharmacognosy department. The study was carried out with an objective to estimate the need for each herbarium by topic

Results: The herbarium fund was formed by the staff of the pharmacognosy department for many years on the basis of the approved pharmacognosy program. The collection is used for research by students – to perform diploma, qualifying works, and teachers to prepare teaching aids, and pharmacopeia articles develop and conduct research. The number of herbarium specimens is stored in the main fund – more than 5000. 240 species of medicinal plants belonging to 104 families are represented.
EVALUATION OF ANTIUROLITHIC HERBAL FORMULA FOR UROLITHIASIS: A RANDOMIZED OPEN-LABEL CLINICAL STUDY
Authors: ULFATUN NISA  , PERISTIWAN R WIDHI ASTANA
Published: October 2019

Objective: The objective of the study was to evaluate the safety and efficacy of antiurolithic herbal formula (AHF) compared with commercial polyherbal lithotriptic (CPL) agent in urolithiasis subjects.

Materials and Method: The study was conducted with the design of purposive randomized open-label, end-blinded observation. The sample size and randomization were done by computer with generated statistical program. The total of subjects who met the inclusion and exclusion criteria was 200 patients. Every subject was given AHF or CPL according to their group and the intervention was carried out for 8 weeks. The study used the difference of stone’s size and number as parameter to observe the efficacy between two groups. While in terms of safety, this study used biochemical parameters of liver and kidney function.

Results: A total of 191 adult patients with urolithiasis were enrolled. There were 97 and 94 subjects in AHF and CPL group, respectively. The study showed a significant size reduction of single’s and multiple’s stone in AHF group (p<0.05). The size reduction difference in AHF group is greater than in CPL group. The number of multiple stone’s subjects who treated AHF was significantly decreased. Whereas in CPL group, there was no significant size difference between pre and prost treatment. The biochemical parameters showed normal liver and renal function in both groups.

Conclusion: This study result indicates that AHF is safe and effective in the treatment of urolithiasis.
DESIGN AND SYNTHESIS OF NOVEL 4-(4-FLUORO-3-METHYLPHENYL)-6-(SUBSTITUTED ARYL)-1,6-DIHYDROPYRIMIDIN-2-OL DERIVATIVES AS POTENT ANTI-INFLAMMATORY AND ANALGESIC AGENTS
Authors: MURALIDHARAN V  , RAJA S  , ASHA DEEPTI
Published: October 2019

Objective: Pyrimidine heterocycles possessing hydroxy group has a unique place in medicinal chemistry and also plays a key role in biological processes. In the biological functions at cellular level pyrimidine plays imperative roles which lead the researchers to design a variety of its derivatives. The aim of the present study was to synthesize the novel set of 4-(4-fluoro-3-methylphenyl)-6-(substituted aryl)-1,6-dihydropyrimidin-2-ol derivatives. These compounds were screened for their analgesic and anti-inflammatory activities.

Methods: A novel series of 4-(4-fluoro-3-methylphenyl)-6-(substituted aryl)-1,6-dihydro pyrimidin-2-ol derivatives were furnished in two steps starting from 4-fluoro-3-methyl acetophenone through chalcone formation. Human red blood cell membrane stabilization method and carrageenan-induced rat paw edema test were performed for screening in vitro and in vivo anti-inflammatory activity, respectively. Tail-flick technique was performed for screening analgesic activity.

Results: All the synthesized 4-(4-fluoro-3-methylphenyl)-6-(substituted aryl)-1,6-dihydro pyrimidin-2-ol derivatives were characterized by Fourier-transform infrared spectroscopy,1H nuclear magnetic resonance, mass spectroscopy, and bases of elemental analysis. The result of biological screening revealed that many of the new derivatives were endowed with improved anti-inflammatory and analgesic activities.

Conclusion: Nature of the substituent played a major role in anti-inflammatory and analgesic activities. The pyrimidine derivative with chlorophenyl substitution exhibited potent anti-inflammatory and analgesic activities. From the results, it was concluded that 6-(4-chlorophenyl)-4-(4-fluoro-3- methyl phenyl)-1,6-dihydropyrimidin-2-ol was the most active compound.
AN ETHNOBOTANICAL STUDY OF WILD MEDICINAL PLANTS USED BY MIGRATORY SHEPHERDS – A TRIBAL COMMUNITY OF WESTERN HIMALAYAS
Authors: RADHA  , PURI S  , KUMAR S
Published: October 2019

Objectives: Migratory shepherds of Kinnaur, Shimla, and Sirmaur districts in Himachal Pradesh of the western Himalayas have rich traditional knowledge of medicinal plants and its uses, in this respect; an ethnobotanical survey was carried out from 2017 to 2018.

Methods: The required information on ethnomedicines used by tribal migratory shepherds was collected through personal field visits, interview method and using a pretested questionnaire.

Results: It was observed that in all 78 species were used by shepherds en route from high hills to low hills. In high hills 35 species, in mid hills 20 species, and low hills 23 species were found to be used as ethnomedicine source.

Conclusion: This study shows that shepherds in tribal areas are highly dependent on ethnobotanical remedies, which evolved over generations of experience and practices, for health care. The common diseases were treated by ethnomedicinal plants such as cough, cold, body pain, Skin infection, wounds, diarrhea, respiratory problems, and sunburn. The collected detailed information on the list of plants and their therapeutic practices among tribal migratory shepherds may be helpful to improve the future pharmaceutical applications.
HYDROALCOHOLIC EXTRACT OF MATRICARIA CHAMOMILLA LINN. AMELIORATES LIPIDS, LIPOPROTEINS, AND PARAOXONASE IN ISOPROTERENOL-INDUCED MYOCARDIAL INFARCTION IN WISTAR RATS
Authors: VADIVELAN RAMACHANDRAN  , GAUTAM ADHIKARI
Published: October 2019

Objective: The objective of this study was to evaluate the effect of the hydroalcoholic extract of Matricaria Chamomilla Linn. (CHAE) on lipids, lipoproteins, and antioxidants activity in isoproterenol (ISO)-induced myocardial infarcted rats.

Methods: ISO (85 mg/kg, s.c.)-induced myocardial infarction for 2 consecutive days at an interval of 24 h. Rats were pretreated with CHAE (100 and 200 mg/kg, oral) for a period of 20 days and ISO was injected on 21 and 22 days at 24 h intervals and after 24 h, blood was collected through retro-orbital plexus for the estimation of lipids, lipoproteins, and antioxidants assay.

Results: In the present study, ISO caused a significant increase in the concentration of total cholesterol, triglycerides, low-density lipoprotein cholesterol (LDL-C), very LDL-C, and lipid peroxidation whereas a significant decrease in the concentration of high-density lipoprotein-C. ISO administration also significantly decreased the activities of paraoxonase (PON) enzyme. Oral pre-treatment of CHAE at doses of 100 and 200 mg/kg body weight (bw) for 20 days challenged with a concurrent injection of ISO (85 mg/kg bw) on 21 and 22 days significantly attenuated these alterations and restored the levels of lipids and lipoproteins. In addition, CHAE significantly elevated the serum antioxidants enzyme PON and catalase (CAT).

Conclusion: The report revealed that pre-treatment with CHAE ameliorated lipid and lipoprotein and increased the antioxidant PON and CAT activity and decreased LPO level in ISO-treated male albino Wistar rats.
STABILITY-INDICATING HIGH-PERFORMANCE THIN-LAYER CHROMATOGRAPHY METHOD FOR SIMULTANEOUS ESTIMATION OF FORMOTEROL FUMARATE DIHYDRATE AND FLUTICASONE PROPIONATE IN BULK DRUG AND PHARMACEUTICAL DOSAGE FORM
Authors: RAJASHI B PHARATE  , SUNEELA S DHANESHWAR
Published: October 2019

Objective: The objective of the present work was to develop validated stability-indicating high-performance thin-layer chromatographic method for simultaneous estimation of formoterol fumarate dihydrate (FFD) and fluticasone propionate (FP) in bulk drug and pharmaceutical dosage form.
Methods: Pre-coated silica gel aluminum plates 60 F-254 were used as stationary phase. The mixture of toluene:ethyl acetate:formic acid (98%) (6:4:0.1; v/v/v) was used as a mobile phase. The densitometric quantification was carried out at 233 nm. The method was validated according to the ICH guidelines. The specificity and stability indicating the capability of the method were proven though degradation studies. Both drugs were subjected to acid (0.1N HCl) and base (0.1N NaOH) hydrolysis, oxidation (3% v/v H2O2), photolytic, and neutral degradation conditions.
Results: The selected mobile phase resolved peaks of FFD and FP with Rf values 0.27±0.10 and 0.64±0.10, respectively. Determination coefficients of calibration curves were found to be 0.998 and 0.999 in the range of 1–3.5 μg/spot and 10–60 μg/spot for FFD and FP with an accuracy of 99.09% for FFD and 99.20% for FP. The degradation products of FFD and FP were resolved from the pure drug with significant differences in their retention factor values.
Conclusion: The developed method is simple, accurate and can be successfully applied for quantification of FFD and FP in bulk drug and pharmaceutical dosage form, contributing to improve the quality control and assure the therapeutic efficacy.
A STUDY ON PHYTOCHEMICALS, ANTIMICROBIAL, AND SYNERGISTIC ANTIMICROBIAL ACTIVITIES OF HIBISCUS SABDARIFFA
Authors: SIVAN KUMAR  , ANNA SHEBA L
Published: October 2019

Objective: The aim of the present study was to screen phytochemical constituents and evaluate antimicrobial and synergistic antimicrobial properties of leaves and stem of Hibiscus sabdariffa.
Methods: The extraction was done by cold maceration method using 80% aqueous methanol. The antimicrobial efficacy and synergistic antimicrobial activity were carried out by disc diffusion assay against the bacteria Staphylococcus aureus and Pseudomonas aeruginosa.
Results: Phytochemical analysis revealed the presence of carbohydrate, protein, alkaloids, phytosterols, flavonoids, and diterpenes in both the leaves and stem extracts while saponins, phenol, and tannins were found to be present only in the leaf extract. Both the extracts inhibited the tested bacteria with minimum inhibitory concentration value of 10 mg/ml. Aqueous methanolic extract of leaf showed higher antibacterial activity against S. aureus and P. aeruginosa and also exhibited synergistic activity with the antibiotic chloramphenicol against S. aureus.
Conclusion: The present study concludes that H. sabdariffa is a potential source of bioactive components and also provides information on synergistic activity of leaf extract. The results can contribute to the development of potent antibacterial agents.
EFFICACY AND TOLERABILITY OF FLUPIRTINE VERSUS TRAMADOL IN THE TREATMENT OF MODERATE CHRONIC LOW BACK PAIN
Authors: VINEELA KARTHIK NAGURI  , RAVI BABU KOMARAM  , TAMILISETTI VIDYA SAGAR
Published: October 2019

Objective: The objective of the study was to assess and compare the efficacy and tolerability of flupirtine versus tramadol in patients with chronic moderate low back pain (LBP).

Materials and Methods: A prospective study was conducted in the outpatient department of orthopaedics at tertiary care hospital, Rajamahendravarm. After meeting the inclusion criteria, a total of 60 patients were randomly allocated to tablet flupirtine 100 mg in Group A and tablet tramadol 50 mg in Group B. The efficacy of the study drugs was assessed at baseline and the end of treatment by numerical rating scale11, visual analog scale-100 mm, physician’s, and patient’s global assessment. Statistical analysis was done using paired and unpaired t-test and data were presented as mean±standard deviation. Adverse drug reactions were monitored during the treatment.

Results: The study results showed that 90% of the patients in Group A and 78% of the patients in Group B had shown a good response to their respective drugs. 30% of flupirtine group patients reported adverse drug reactions which were mild.

Conclusion: Both the drugs are effective in the treatment of moderate chronic LBP, but the advantage of flupirtine was, the incidence of adverse drug reactions was less when compared to tramadol group.
DEVELOPMENT OF METOCLOPRAMIDE HYDROCHLORIDE IN SITU GEL: NASAL DELIVERY AND PHARMACOKINETICS IN NEW ZEALAND RABBITS
Authors: UPENDRA C GALGATTE  , PRAVIN D CHAUDHARI
Published: October 2019

Objective: Systemic bioavailability of metoclopramide hydrochloride (MCH) is 32–80% by oral route. The study was targeted to develop in situ gel of MCH for nasal delivery and to study its pharmacokinetics in healthy rabbits. Pre-systemic metabolism can be overcome.

Methods: Poloxamer 407 (P407) aqueous solutions were prepared by cold method. In 32 factorial design, independent variables were Carbopol 934P and polyethylene glycol 6000 (PEG 6000), and dependent responses were gelation temperature, mucoadhesive strength, and drug release. A Pharmacokinetic study was carried out in New Zealand rabbits. The optimized in situ gel (1 mg/ml) was compared with marketed Reglan® (2 mg/2 ml) injection. Area under the curve (AUC), Cmax, and Tmax were estimated.

Results: F2 was an optimized formulation. The study showed that P407 solutions formed a gel at nasal temperature 34°C having mucoadhesive strength 806.12±3.45 dyne/cm2. MCH release was found to be 93.74±1.31% within 6 h. Histopathological examination of formulation F2 exhibited safety to the nasal mucosa. The pH of formulations was 5.1±0.1 to 5.6±0.1 in the range of pH of nasal cavity. Plasma samples were analyzed by liquid chromatography/mass spectroscopy (LC/MS). The area under curve AUC0-4 for in situ gel by nasal route was 2716±4.617 ng/h/ml and for marketed solution by intravenous route was 2874±1.0816 ng/h/ml. These were comparable. Nasal bioavailability was found 94.50% from in situ gel. Duration of action was longer, and steady-state concentration was found for in situ gel.

Conclusion: In situ gel was capable to release MCH in systemic circulation. In vivo study in rabbits has proved the improved bioavailability of MCH administered nasally. The optimized gel preparation was found to be promising for improved bioavailability.
DESIGN, FORMULATION, AND EVALUATION OF SOLID DISPERSION TABLETS OF POORLY WATER-SOLUBLE ANTIDIABETIC DRUG USING NATURAL POLYMER
Authors: SUDIPTA DAS  , PRIYANKA MANDAL
Published: October 2019

Objective: The objective of the present study was to formulate the solid dispersion (SD) of poorly water-soluble drug glimepiride and the development of the tablets of prepared SD of glimepiride using natural and synthetic polymers.

Methods: The SD of glimepiride was to prepare using fusion method. The tablets were prepared by wet granulation method using synthetic polymer such as HPMC and natural polymer gellan gum.

Results: The granules were evaluated by determining the angle of repose (23.70±0.761 to 29.21±0.127º), bulk density, tapped density, Hausner ratio, and Carr’s index. It shows satisfactory results. The tablets were subjected to the measurement of hardness (3.9±0.08 to 4.6±0.04kg/cm2), friability (0.22±0.004 to 0.40±0.005%), and in vitro release studied. Release study of pure drug was performed. In the release study, SD of glimepiride tablets with gellan gum gives considerably good result compared to HPMC.

Conclusion: From the results, it was shown that dissolution rate of pure glimepiride was very slow. When the glimepiride was prepared in SD form, then the dissolution rate was very fast. The tablets of the SD of glimepiride were prepared and release study was shown depending on various quantities of HPMC and gellan gum used. Therefore, the long term stability study is required for future development of this formulation.
UTILITY OF PLACENTAL LEUCINE AMINOPEPTIDASE/OXYTOCINASE IN THE PREDICTION OF PRETERM DELIVERY IN PREGNANT WOMEN WITH THREATENED PRETERM LABOR
Authors: MIAMI ABD–AL HASSAN  , ISRAA TALIB ABD AL KADIR  , NOOR HUMAM MOHAMMED
Published: October 2019

Objective: The study objective was to assess the utility of placental leucine aminopeptidase (P-LAP) marker for the prediction of delivery in patients presented with threatened preterm labor (TPL).

Setting: This study was conducted at the Obstetrics and Gynaecology Department of Al-Yarmouk Teaching Hospital in the period from March 2017 to June 2018.

Type of Study: This is a prospective case control study.

Methods: This study included 90 pregnant women with gestational age from (28-36+6) weeks; 45 of them who presented with preterm uterine contractions were considered as the study group which was further subdivided into three subgroups according to gestational age 28–31+6 weeks, 32– 33+6 weeks, and 34–36+6 weeks. The other 45 pregnant women who presented to the hospital for regular antenatal care visit at comparable gestational age to the study group were considered as the control group. Hence, this study aimed to assess the serum level of P-LAP in both groups and compare it between those delivered preterm from term to assess its applicability as a predictor of preterm labor.

Results: Serum level of P-LAP in pregnant women presented with TPL was found to be significantly lower in those delivered preterm (p<0.001), compared to those continued to term and control group especially in gestational ages ≥32 weeks, while the study found P-LAP level to be statistically insignificant in gestational age <32 weeks (p=0.052). The cutoff point for P-LAP serum level was = 21 (IU/ml) that below it, the pregnant women with TPL most probably deliver before 37 weeks of gestation with Sensitivity (85.7%) Specificity (90.3%), Positive predictive value (80.0%) Negative predictive (93.3%).

Conclusion: The serum level of P-LAP was lower in women delivered preterm than those delivered at term, so it can be used as one of the markers for the prediction of preterm delivery, especially at gestational age >32 weeks.
EVALUATION OF IN VITRO CYTOTOXIC AND ANTICANCER ACTIVITY OF HEPATOPROTECTIVE POLYHERBAL FORMULATION IN CELL LINE MODEL
Authors: JAYACHANDRA KUNCHA  , THIRUGNANASAMBANTHAM P  , KUMARAN S  , NARAYANAN N  , SHARMILA DEVI V
Published: October 2019

Introduction: The use of natural products as anticancer agents has a long history that began with folklore medicine and through the years has been incorporated into traditional and allopathic medicine. Several drugs currently used are derived from medicinal plants.

Objective: The main objective of this study is to investigate the cytotoxic potential of hepatoprotective polyherbal formulation in normal and cancer cell lines.

Methods: A 3-(4,5-dimethythiazol-2-yl)-2,5-diphenyltetrazolium bromide assay was utilized to screen the cytotoxic activity.

Results: The results revealed that the formulation does not induce much mortality in normal liver and kidney cell lines, and LC50 value of liver cell lines was found 1716.355 μg/ml and kidney cell lines 2464.910 μg/ml. The in vitro anticancer activity was performed on liver, colon, and prostate cancer cell lines, and IC50 values are found 2.077, 3.850, and 11.989 μg/ml, respectively, which show excellent anticancer activity.

Conclusion: Based on the results obtained, the hepatoprotective polyherbal formulation is safe for normal cells and cytotoxic for cancer cells. Further, identification and quantification of phytoconstituents responsible for the activity are in progress.
COMBINATION OF LEPTIN ANALOG AND SALBUTAMOL: TREATMENT APPROACH FOR OBESITY-INDUCED ASTHMA
Authors: ARUN K SONI  , SHRIKALP S DESHPANDE
Published: October 2019

Objective: The objective of the study was to investigate the effect of leptin analog and salbutamol in obese asthmatic mice.

Methods: Obese asthmatic condition was induced by administration of hypercaloric diet for 8 weeks followed by ovalbumin-aluminum hydroxide. The animals were treated with leptin analog (0.4 mg/kg, i.p. for 14 days) and salbutamol (2 mg/kg, PO for 14 days). Biochemical parameters such as serum leptin, ghrelin, and tumor necrosis factor-α and physical parameters such as tidal volume and airflow rate were estimated to confirm the state of asthma and obesity, respectively.

Results: Elevated serum leptin and ghrelin were associated with leptin resistance in obese asthmatic mice. It was found that a significant increase in serum leptin level with animal treated with leptin analog and salbutamol when compared to animals treated with leptin analog alone. The result of respiratory parameters and serum parameters also improved with the combination of leptin analog and salbutamol. From our study, we found that salbutamol potentiates the effect of leptin analog in obese asthmatic condition.

Conclusion: Leptin analog and salbutamol are an alternative treatment approach to treat the obese asthmatic condition.
GREEN TEA CATECHIN LOADED NANODELIVERY SYSTEMS FOR THE TREATMENT OF PANDEMIC DISEASES
Authors: SATHEESH BABU NATARAJAN  , SURIYAKALA PERUMAL CHANDRAN  , ANJANEYULU VINUKONDA  , SENTHIL RAJAN D
Published: October 2019

Tea (Camellia sinensis, Family: Theaceae) is one of the extremely consumed beverages around the world, behind to water. The brew tea is the merely food product contains abundant quantity of the catechins. Green tea is the least processed and thus contains rich antioxidant, polyphenols, especially catechin called epigallocatechin-3-gallate (EGCG), which is whispered to be responsible for a wide range of the health benefits. The key to the amazing health benefits that are derived from green tea is that the leaves are steamed which preserves the EGCG compound from being oxidized. However, the other varieties of teas are under go fermentation process, which breaks down the potential EGCG and destroy from its healing properties. In reality, green tea has very extensive history dating back thousands and thousands of years ago. However, the pharmacological efficacy and stability of green tea catchiness are primarily depended on the formulation and way to drink to alleviate the deadly diseases with scientific evidence. Nanotechnology is a vibrantly emerging field especially in the pharmaceutical industry to explore a lot of application. The promising nano-delivery system used to enhance the therapeutic efficacy with a minimal dose, minimize the dose-related toxicity, target delivery, site-specific delivery, and controlled/sustain the delivery application. In recent decades, the application of nanotechnology has been utilized for phytopharmaceutical industry including green tea catechins to maximize the health benefits. In this review, we tried our level best retrieve the value of information on nanodelivery application of green tea catchiness for various devastating diseases.
IN VITRO ANTIOXIDANT AND ANTICANCER ACTIVITY OF ULVA LACTUCA L.USING MOLT-3 CELL LINE
Authors: CHIDAMBARARAJAN P  , KEERTHANA V  , PRIYADHARSHINI K,  , SAKTHIVEL B
Published: October 2019

Objective: The aim of the present investigation was to determine the in vitro antioxidant and anticancer activity of the ethanol extract of Ulva lactuca L.

Methods: The present study was to investigate the antioxidant and anticancer activity of U. lactuca L. The extract of U. lactuca L. was extracted by ethanol and subject to analysis. An in vitro antioxidant activity of the ethanol extract of U. lactuca L. was performed by 1, 1-diphenyl-2-picrylhydrazyl free radical scavenging assay. Simultaneously anticancer activity was also performed using blood cancer (MOLT-3) cell line, and the species showed a strong selective cell proliferation inhibition of the cancer cell line.

Results: The scavenging activity was measured and determined to be 78.5%. This might be due to high polyphenolic compounds and flavonoid contents of the extract, which showed maximum growth inhibition of 74.4%.

Conclusion: Thus, the study concludes that the constituents of seaweeds can act as potent in treating various diseases and can be used as an alternative for therapeutic treatment.
STUDIES ON TOXICOLOGICAL AND NEUROBEHAVIORAL PROFILE OF METHANOL EXTRACT OF MUSSAENDA ROXBURGHII HOOK. F. LEAVES IN MICE
Authors: SANJIT NAMASUDRA  , PANKAJ PHUKAN  , MEENAKSHI BAWARI
Published: October 2019

Objective: The aim of this study was to evaluate the toxicity of Mussaenda roxburghii with special reference to the nervous system.

Methods: For the study, 15 mice were obtained from Pasteur Institute, Shillong. The mice were then divided into three groups containing five mice in each group. The groups were, namely Group I, Group II, and Group III; Group I mice received distilled water and acted as a control group, Group II mice received plant extract at a dose of 600 mg/kg body weight (BWT.), and Group III mice received plant extract at a dose of 800 mg/kg BWT. The doses were administered orally through oral gavage tube for 28 days and the BWT of the mice was measured at 7th, 14th, 21th, and 28th days. The behavior of mice was evaluated for anxiety, locomotion, immobility, learning, and memory with the elevated plus maze test (EPMT), open field test (OFT), forced swim test (FST), and Morris water maze test (MWMT), respectively.

Results: The result of the experiment showed a decrease in the BWT of mice exposed to plant extracts significantly as compared to the control. In the OFT, there is a significant decrease in total distance travel in OFT and also total distance travel in the central zone in mice treated with the plant extracts as compared to the control mice. In the EPMT, the plant extract treated mice showed a decreased in the time spent in open arms. The FST results in increased immobility in mice exposed to plant extracts as compared to control. In the present study, MWMT results in an increased escape latency and path length and in decreased annulus crossovers in plant extract treated group as compared to control.

Conclusion: The results of the present study suggest that the plant extract alters the behavior of the treated mice and possesses neurotoxic activity.