IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
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AUGUST 2020
1

IN SILICO MOLECULAR DOCKING STUDIES ON SOME NOVEL N-SUBSTITUTED SULFONAMIDE ANTHRANILATE HYDROXAMIC ACID DERIVATIVES FOR ITS CYTOTOXIC POTENTIAL AGAINST CANCER MARKERS

Abinash Pandit*1, S.N. Sriharsha1, N. Habeela Jainab1, Praveen P2, Sheshagiri R Dixit2
1Hillside College of Pharmacy and Research Centre, Raghuvanahalli, Kanakapura Main Road, Bangalore-560062.
2JSS College of Pharmacy, JSS Academy of Higher Education and Research, Mysuru-570015, Karnataka, India.

N-Substituted sulfonamide anthranilate hydroxamic acid derivatives have a better binding affinity towards the Matrix Metalloprotease (MMP) enzyme as per the literature. Based on that we have selected the Matrix Metalloprotease-1 (MMP-1) domain of MMP enzyme and performed the molecular docking studies using the SYBYL X 2.1 software. We have designed fifteen new chemical new entities for the docking studies and among that two chemical entities were found to have better binding affinities towards the MMP-1 target. By studying the total docking scores of all the new chemical entities we have concluded that the groups like benzyl group at Nth position, methoxy group at 4th position of phenyl sulfonamide nucleus, dimethylamine group at 3rd position of hydroxyl benzamide nucleus, etc. are responsible for better activities and binding affinities towards MMP-1 target. So, based on that we can proceed for the further synthesis of those molecules which has higher affinities towards the MMP domains. Some of the positions like 4th, 6th position in Hydroxy Benzamide Nucleus and 2nd, 3rd, 5th, 6th positions in Phenyl Sulfamido Nucleus are unsubstituted and still, we are in process of study in the future projects. 


 


2

IN SILICO MOLECULAR DOCKING STUDIES ON THE CHEMICAL CONSTITUENTS OF CLERODENDRUM PHLOMIDIS LEAF FOR ITS CYTOTOXIC POTENTIAL AGAINST LUNG CANCER MARKERS

Anu Pandit*1, N. Habeela Jainab1, S. N. Sriharsha1, Praveen P2, Sheshagiri R Dixit2
1Hillside College of Pharmacy and Research Centre, Raghuvanahalli, Kanakapura Main Road, Bangalore-560062.
2JSS College of Pharmacy, JSS Academy of Higher Education and Research, Mysuru-570015, Karnataka, India.

Lung cancer remains the leading cause of cancer morbidity and mortality worldwide and is the second cause of the death. In 2018, there were 234,030 newly diagnosed lung cancer patients, accounting for 13.5% of all types of malignant tumors. The vascular endothelial growth factor (VEGF) is the main mediator of angiogenesis and it contributes to cancer growth and metastasis directly targeting the tumor cells. Clerodendrum phlomidis is a shrub common in India and Sri-lanka with valuable medicinal properties. GC-MC analysis of the methanol leaf extract of C. phlomidis revealed the presence of 17 compounds. In the current study, we aimed to find out the binding effectiveness of the various chemical constituents present in the methanol extract of C. phlomidis leaf against lung cancer targets VEGFR-1 and VEGFR-2 and to identify the potent chemical moiety by in silico molecular docking studies. In silico docking studies were carried out using SYBYL package. The results indicated that the chemical constituents of C. phlomidis binds with the target VEGFR-1 and VEGFR-2 effectively with the total score value ranging from 3.0623 to 13.6396 and 0.2089 to 15.4975 respectively. Among the docked molecules compounds oleic acid eicosyl ester and DL- Alpha Tocopherol were found to have good total score value against VEGFR-1, oleic acid eicosyl ester and isopropyl linoleate were found to have good total score value against VEGFR-2. In future, designing of the chemical constituents having the pharmacophore similar to oleic acid, eicosyl ester, DL- Alpha Tocopherol and isopropyl linoleate or their derivatives with varying substituents in different position will be a good drug for the lung cancer target VEGFR-1 and VEGFR-2. 


 


3

REPEATED DOSE 90-DAY ORAL TOXICITY EVALUATION OF KUMAARA VEERIYA KAANTHA CHENDURAM, A SIDDHA HERBOMINERAL FORMULATION IN WISTER ALBINO RATS

Siva Lakshmi.S*1, H.Vetha Merlin Kumari1, S.Mohan2, R.Meenakumari3
1Department of Maruthuvam, National Institute of Siddha, Chennai.
2Department of Maruthuvam, Former director, National Institute of Siddha, Chennai.
3National Institute of Siddha, Chennai.

Aim: In siddha system of medicine, one of the typical kantham formulation is ‘Kumaara veeriya kaantha chenduram’ (KVKC) which is indicated for anaemia. The toxicological study of the drug was not reported. The objective of this study is to evaluate its safety by performing repeated dose 90-day oral toxicity studies as per OECD test guidelines 408 for the further clinical application in anaemia cases. Methods: In this study KVKC was administered in wister albino rats orally at low dose 100 mg/kg/ b.wt, Mid dose 200 mg/kg/b.wt, High dose 400 mg/ kg/ b.wt once a day for 90 days with honey. Animals were observed for toxic signs for 90 days. On 91st day cage side observations, hematological, biochemical and histopathological analysis were executed to recognize the toxic effects. Results: Results of the hematological, biochemical and histopathological analysis conducted on 91th day revealed that there were no significant changes in all the drug treated animals when compared with those of respective controls. According to these results, Kumaara veeriya kaantha chenduram could be concluded as no-observed-adverse-effect level (NOAEL). Conclusion: This study provides scientific validation for the drug’s safety and also proved its effectiveness in long-term administration without harming the human being. And the drug KVKC is safe in the dose of 260 mg for human adult mentioned in the siddha literature. 


 


4

MULTI DRUG RESISTANCE PATTERNS AMONG GRAM NEGATIVE BACTERIA IN HOSPITALIZED PATIENTS AND THE ECONOMIC IMPACT IN THEIR TREATMENT

B.V.S Lakshmi, M. Hima bindu, M.Sudhakar, M.Samhitha, S.Manasi*
Malla Reddy College of Pharmacy, Dhulapally, Secunderabad, Telangana-500100 (Affiliated to Osmania University).

BACKGROUND: Infections caused by multidrug resistant gram negative bacteria are often corresponded with increased comorbidities, prolonged hospitalization and mortality. These bacteria not only pose a serious threat to global public health but also create a burden to health care systems. The present study was aimed to identify the incidence of Multi drug resistance patterns among gram negative bacteria in hospitalized patients and the economic impact in their treatment. We have also studied the sensitivity and resistance patterns of the isolated gram negative organisms. METHODS: Prospective study was conducted on 165 patients. Relevant data pertaining to demographics characteristics, comorbid conditions, length of stay and costs of antibiotics was taken from the patients. Blood and other samples like swab, sputum, urine, CSF etc were also sent for the culture sensitivity testing. Antimicrobial susceptibility testing was carried out using the Kirby bauer disc diffusion method. RESULTS : The most common multi drug resistant Gram negative bacteria were E.coli (33.94% )and Klebsiella pneumoniae(12.12%) The multidrug resistance patterns show that E.coli is most resistant to Tetracycline and Amoxyclav , Klebsiella is highly resistant to Ampicillin, Ertapenem & Gentamicin. The economic burden was more in Multidrug resistant cases when compared to sensitive cases. CONCLUSION: There is an increase in multidrug resistance patterns especially in E.coli & Klebsiella pneumonia with a significant increase in costs in MDR cases, due to change in their therapy to a more sensitive antibiotic. 


 


5

ASSESSMENT OF THE IMPACT OF PATIENT COUNSELING ON THE KNOWLEDGE, ATTITUDE AND PRACTICE IN PATIENTS WITH DIABETES MELLITUS IN A TERTIARY CARE HOSPITAL

Catherin Babu*, Jeffin Joseph, Cheryln Ann Chacko, Gikku Mariyam Varghese, Mr.Philip Jacob, Dr.Roshiny Thankom James, Dr: Elessy Abraham
Department of Pharmacy Practice, Nazareth College of Pharmacy, Othera, Thiruvalla.

INTRODUCTION: Diabetes Mellitus (DM) is a chronic condition associated with abnormally high levels of sugar (glucose) in the blood. The management of diabetes mellitus (DM) largely depends on patients’ ability to self-care in their daily lives, and therefore, patient education is always considered an essential element of DM management. Patient counselling involves providing drug information, dietary and lifestyle modifications. Thus patient counselling plays a major role in increasing patient’s medication adherence and improving the patient’s quality of life. The current study is to study the effect of counselling on Knowledge, attitude and Practice among type 2 Diabetes mellitus. MATERIALS AND METHODS: A prospective observational study was carried out over a period of six months in General Medicine Department Of Muthoot Healthcare, Pvt. Ltd, Kozhencherry. The type 2 diabetic patients who were on oral hypoglycemic were enrolled in the study. A suitable data collection form was prepared and used to collect the required data. The demographic data, disease data and the utilization of various oral antidiabetic agents were analyzedand the knowledge of the patients was assessed by using a Knowledge,Attitude and Practice questionnaire. For this study 398 subjects were enrolled based on the inclusion and exclusion criteria. RESULTS: Among 398 subject, 89.5% shows elevated FBS before counselling and this is decreased to 53.5% after counseling, mean value of Pre-test (Before counselling) and Post-test(After counselling) was 35 and 16.4 respectively. In our study it was found that counseling was effective in maintaining glycemic control. 


 


6

A COMMUNITY BASED SURVEY ON ROLE OF CLINICAL PHARMACIST IN CREATING AWARENESS AMONG WOMEN ABOUT BREAST SELF-EXAMINATION KNOWLEDGE AND PRACTICES IN BANGALORE- INDIA.

G. Jyoteshwari1*, Dr. Sushma Muchukota2, Dr. E. Bhavya2
1Gautham College of Pharmacy Affiliated to RGUHS, Bangalore, Karnataka, India.
2School of Pharmaceutical Sciences, VISTAS, Pallavaram, Chennai, Tamilnadu, India.

Background: Breast self-examination (BSE) is simple, painless, very important, low-cost and non-invasive technique for early method for detection of Breast cancer in the initial stages. It is ought to be done for all women at all age groups. Aim and Objectives: The aim of this study was to assess the awareness, knowledge and practices of Breast Self Examination (BSE) as a method of prevention and early diagnosis of breast cancer among women with involvement of clinical pharmacist and providing proper counselling and educating them regularly about BSE in order to prevent further complications. Methods: A cross-sectional study was conducted among 189 women, among few areas in Bangalore for a period of 6 months, using self-administrated questionnaire and women aged >19 years old, who are having minimal knowledge about BSE in 2019. Results: Majority of the participants, were between 20 -25 years 86(44.3%) also our study reveals that 13(6.7%) had family history of breast cancer. 120 (61.8%) of the participants had heard BSE and 35(18.5%) had good knowledge about BSE. Mass media and internet were the most common source of information about breast cancer. Few of the participants 60 (30.9%) had performed BSE. Family history of breast cancer, knowledge, and attitude of BSE were found to be extensively associated with BSE practice. Conclusion: Health education programs are very much essential to encourage and improve women’s knowledge and practice of BSE, provide proper counselling so as to prevent further complications. As the knowledge 65(33.5%) and Practices about Breast Self Examination are very poor 99 (51%) It is very important to expand health educational programs to raise awareness about BSE and breast cancer so as to practice self-breast examination. Educational interventions are compulsorily required to encourage young women to perform BSE regularly at home, so that breast abnormalities can be detected early on and mortalities can be minimized. 


 


7

EVALUATION OF ISOLATED PHYTOSTEROL FROM LEAVES OF HOLOPTELEA INTEGRIFOLIA (ROXB.) PLANCH FOR IT’S ANTIDEPRESSANT ACTIVITY IN EXPERIMENTAL ANIMALS

Ravindra C. Sutar*
Department of Pharmacology, Sanjivani College of Pharmaceutical Education and Research, Kopargaon. At-Sahajanandnagar, Post-Shinganapur (Pin code- 423603), Tal- Kopargaon, Dist- Ahmednagar, Maharashtra, India.

Background: Majority of scientific documentation suggested prominent role of Phytosterols towards Antidepressant activity. The main objective of the work was to evaluate Antidepressant activity of Holoptelea integrifolia isolated Phytosterol (HIIP) from petroleum ether extract (PEHI) of leaves of Holoptelea integrifolia (Roxb) Planch. Methods: The Antidepressant activity of different doses of HIIP (10 and 30 mg/kg-p.o.) was evaluated using Forced Swim Test (FST) in mice. Results: HIIP-30 mg/kg was more potent than HIIP-10 mg/kg for showing Antidepressant activity. Conclusions: The results indicate that HIIP shows Antidepressant activity which was dose dependent.