Editor(s)

Dr. Wagih Mommtaz Ghannam
Professor,
Department of General Surgery, Faculty of Medicine, Mansoura University, Egypt.

ISBN 978-93-91473-57-0 (Print)
ISBN 978-93-91473-73-0 (eBook)
DOI: 10.9734/bpi/tipr/v9

This book covers key areas of pharmaceutical research. The contributions by the authors include prednisolone, HPLC and method validation, medication adherence, Morisky medication adherence scale, type II diabetes mellitus, therapeutic outcome, isolated rabbit intestine, relaxant activity, ethanolic extract, adrenaline, adverse drug reaction, pharmacovigilance, arthritis, C-reactive protein, pharmacological screening, gastro-retentive drug delivery system, floating tablets, keto amino acids, glomerular filtration rate, conservative management, end stage renal disease, mother's womb, complexation, antiepileptic’s, epilepsy, histopathological examination, kidney disease, tumor incidence, carcinoma, breast cancer, spectroscopic analysis, phytocompounds, glycogen phosphorylase protein, docking, diabetes. This book contains various materials suitable for students, researchers and academicians in the field of pharmaceutical research.

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Chapters

An Advanced Study on Development and Validation of RP-HPLC Method for Simultaneous Estimation of Mesalamine and Prednisolone in Bulk and Formulation

N. K. Drisya, S. S. Prasanth, V. Akhila, K. Sruthi

Technological Innovation in Pharmaceutical Research Vol. 9, 19 July 2021, Page 1-10
https://doi.org/10.9734/bpi/tipr/v9/2881F

In accordance with the analytical parameter mentioned in the ICH guidelines, a simple, precise, accurate, sensitive, and economical reversed phase high performance liquid chromatographic method was developed and validated for the simultaneous determination of Mesalamine (MSL) and Prednisolone (PRD) in combined dosage forms The medicines were separated by chromatography on a C-18 Phenomenex column (250 mm 4.6 mm i.d.) with a mobile phase of acetonitrile: phosphate buffer (pH adjusted to 6 with Orthophosphoric acid) (20:80 v/v). The detection was done at a wavelength of 330 nm. Mesalamine and Prednisolone had retention durations of 4.373 minutes and 1.589 minutes, respectively. Linearity was established for Meselamine in the range of 5-25 $$\mu$$g/ml and Prednisolone in the range of 2-10 $$\mu$$g/ml. Mesalamine and Prednisolone were shown to have 99.57 percent and 100.63 percent recovery rates, respectively. Correlation coefficient of Mesalamine was found to be 0.9973 and for Prednisolone it is 0.9984. The method showed adequate precision with smaller RSD (less than 1%).

A Cross-sectional Study on Medication Adherence in Patients with Type 2 Diabetes Mellitus

T. Prathyusha Rani, B. Prashanthi, Ayesha Amreen Fathima, Ayesha Firdose, Sara Naser, Mohammed Najma Unnisa, Kauser Begum

Technological Innovation in Pharmaceutical Research Vol. 9, 19 July 2021, Page 11-22
https://doi.org/10.9734/bpi/tipr/v9/2456F

Background and Objectives: Diabetes is a chronic disorder and requires long-term therapy. Lack of adherence to anti-diabetic medication causes suboptimal glycemic control and can lead to treatment failures, development of complications, and increased mortality. The objective of the study was to determine the adherence of medications among type 2 diabetes mellitus patients. To evaluate adherence to therapy and study factors associated with nonadherence and adherence in patients with type II diabetics mellitus.

Materials and methods: A cross-sectional, observational study was conducted for a period of 6 months in three hospitals .A total of 200 type II diabetic patients, who were on anti- diabetic drug therapy for at least 6 months, were enrolled. Blood glucose was measured and details of drug therapy were noted. Medication adherence was assessed using Morisky Medication Adherence Scale and adherence scores were calculated.

Results: Only 15% had high medication adherence, while 24% had moderate and 61% had low medication adherence. Only 30% were having optimally controlled glycemic levels, whereas 70% were having uncontrolled glycemic levels. Medication adherence scores were lower (reflecting lower adherence) in type II patients with uncontrolled glycemic levels than those having optimally controlled glycemic levels, but this difference was not statistically significant.

Interpretation and Conclusion: Overall, the medication adherence was low in type II diabetic patients. The study shows that to improve medication adherence, better counseling and health education of patients are required. Although most patients were adherent to therapy, adherent patients are more likely to achieve glycemic control than no nadherent patients. Greater efforts are needed to facilitate diabetes self management behaviours to improve patient outcomes. There is a need for regular monitoring of patient adherence to medication and initiate steps to improve the adherence to anti dabetic medication. Therefore, counselling and health education of the patients related to medication adherence and strateagies to increase drug availability need to be improved.

The in vitro Pharmacological Effects of Fagonia cretica Linn Ethanolic Extract on Isolated Rabbit Intestine

Aimun A. E. Ahmed, Mawahib E. H. Elfeil, Samrin K. N. Ahmed, Tasnim O. Elsammani

Technological Innovation in Pharmaceutical Research Vol. 9, 19 July 2021, Page 23-36
https://doi.org/10.9734/bpi/tipr/v9/3117F

The goal of this work was to use isolated rabbit intestine to evaluate the pharmacological effect(s) of the Fagonia cretica linn (Zygophyllaceae) ethanolic extract and to determine the mechanism(s) underlying its activity. The cumulative dose-response curves of Fagonia cretica extract and standard adrenaline were constructed using different doses ranging from (10-3 - 102 µg/ml), and (10-9 - 10-5 M) alone, and  in the presence of a single dose of a blocker, then the values of EC50, Emax and pA2 were determined as mean ± S.E.M, and and statistically compared. The non-selective adrenergic blockers phentolamine and propranolol were utilised in concentrations of (10-8 and 10-5 M) to identify the exact mechanism mediating the relaxing effect of Fagonia cretica linn's ethanolic extract. Fagonia cretica had a dose-dependent relaxant action on rabbit intestine that was comparable to that of normal adrenaline,with Emax= [56.4 ± 7.5], [7.2 ± 4.3] and EC50= [0.12 ± 0.27], [9.85 ± 1.6] x 10-6 respectively. This effect was mediated by both$$\alpha$$ and $$\beta$$ adrenoceptors, with no direct muscle relaxant involved in mediating the relaxing effect of the plant extract.

It was suggested that more detailed research be conducted to further analyse and confirm these findings utilising various approaches.

An Assessment of Educational Intervention to Improve Knowledge, Attitude and Practice of Pharmacovigilance among Nursing Staff in Tertiary Care Hospital

Sadhana Hingorani, Chaitali Mehta, Paresh Gajera, S. K. Srivastava

Technological Innovation in Pharmaceutical Research Vol. 9, 19 July 2021, Page 37-43
https://doi.org/10.9734/bpi/tipr/v9/10886D

Objectives: The present study was planned 1) To assess the knowledge, attitude and practice among nursing staff and to evaluate the effect of educational intervention. 2) a. To clarify problems regarding ADR reporting such as apprehension, legal issues, and lack of confidence etc. b. To improve reporting of ADR by training nursing staff regarding ADR reporting and filling the ADR reporting form.

Material and Methods: Nursing staff were given a questionnaire about knowledge, attitude, and practice (KAP) before and after an educational intervention in a tertiary care hospital. The information gathered was statistically analysed.

Result: KAP among nursing personnel has improved as a result of the training provided in several sessions. In comparison to the pre-training session, 96% of them correctly identified who can report ADR (69%).When asked about pharmacovigilance as a means of ensuring the safe use of medicines, 71% said yes after training, compared to 54% before. In PvPI questions, 94 percent of nursing personnel correctly identified the scale to be used for causality assessment, compared to 79 percent prior to training. The majority of them thought only unknown and dangerous ADRs should be reported, but after training, they said all ADRs should be reported. A significant improvement has been noticed in questions related to attitude and practice.

Conclusion: KAP among nursing personnel has improved significantly as a result of the educational intervention.

Determination of Pharmacological Screening for Anti-arthritic Potential of Moringa oleifera in Rats Challenged with Formalin

Nishat Fatima

Technological Innovation in Pharmaceutical Research Vol. 9, 19 July 2021, Page 44-56
https://doi.org/10.9734/bpi/tipr/v9/10831D

Objective: Moringa oleifera Lam (Moringaceae), a plant native to Indian sub-continent with high nutritional and medicinal value. Since time immemorial various parts of Moringa have been utilized as food supplement. The recent available data highlights the potential use of M. oleifera leaves for various types of inflammatory diseases. The present work targeted to study arthritis along with the protective effect of Moringa oleifera (MO) leaf extracts in laboratory rats challenged with formaldehyde.

Methods: Arthritis was induced in albino Wistar rats by administration of 0.1 ml formaldehyde (2% v/v, sc) into subplantar region of the right hind paw. Diclofenac sodium (10 mg/kg, i.p.) was used as the standard drug. The ethanolic leaf extracts of MO at doses of 250 and 500 mg/kg and aqueous leaf extract at 500 mg/kg body weight p.o were administered for 10 days. At the end of the study period, changes in paw edema volume, paw thickness, arthritis score, and C-reactive protein (CRP) levels were recorded along with histopathology of knee joints in all groups were studied.

Results:  The results of the study showed a marked decrease in paw edema volume, paw thickness and arthritis score on treatment with diclofenac sodium, ethanolic and aqueous extracts of MO.  There was significant reduction observed in the marker of inflammation in treated animals compared to control. The histopathological data suggested restoration of extract treated tissues to normalcy in comparison to the toxicant. Treatment with aqueous extract in the dose of 500 mg/kg body weight was found to be more potent.

Conclusion: The results demonstrated a more significant anti-arthritic activity of aqueous leaf extracts of MO at a dose of 500 mg/kg body weight compared to ethanolic.

Study on Formulation Development and Characterization of Floating Tablets Using Mentha piperita Extract

Nethaji Ramalingam, Aiswarya Madathil, Neethu Krishna, S. Sudha, K. R. Vimal, Babu Ganesan, N. Dakshan Kumar

Technological Innovation in Pharmaceutical Research Vol. 9, 19 July 2021, Page 57-71
https://doi.org/10.9734/bpi/tipr/v9/11078D

Objectives: Floating tablets is a novel gastro-retentive drug delivery system which buoyant in stomach and ensure controlled effect. Mentha Piperita is a natural herbal regimen used as carminative, anti-oxidant properties and inhibits gastro-duodenal ulcers disease with increasing mucosal resistance against noxious chemical. Based on the concepts, an objective of present study to develop floating tablets of Mentha Piperita herbal extract used as a medicament for an effective treatment of gastric ulcer.

Methods: Floating tablets containing HPMC K100M and Hibiscus Rosa-sinensis mucilage in different formulations were prepared by direct compression technique and evaluated the relevant parameters.

Results: Depending upon the different ratios, prepared powder blend were subjected to the micromeritic properties which shown good flow characteristics. Prepared tablets were investigated for post-compression parameters and there is no significant variation was observed. Percentage drug content found significant results (90.99±0.15 to 98.53±0.32%) and indicates that, distribution of medicament over an area of floating tablets. From swelling index, F1 formulation has shown highest swelling (78.12%) upto 8h. In-vitro buoyancy studies were found that F1 possess highest floating efficiency (>13 hrs.), lowest floating lag time (0.33±0.1sec) and possesses good buoyancy properties. An in-vitro drug release study shown that, F1 exhibits better controlled release (70.61±0.11%) upto sufficient hours and in-vitro kinetic models were also proven zero order kinetics and medicament release follows Non-Fickian diffusion mechanism.

Conclusions: Developed gastro retentive floating tablets using Mentha piperita extract are more effective for stomach specific drug delivery especially in ulcer disease which suitable for potential therapeutic uses and improves the patient compliance.

Determination of Efficacy and Safety of $$\alpha$$-keto Analogs of Essential Amino Acids Supplementation in Patients of Chronic Kidney Disease: A Clinical Evaluation

Technological Innovation in Pharmaceutical Research Vol. 9, 19 July 2021, Page 72-80
https://doi.org/10.9734/bpi/tipr/v9/10923D

Background: The objective was to determine the efficacy and safety of $$\alpha$$-keto analogs of essential amino acids (KAA) as a supplement in chronic kidney disease (CKD).

Methods: In a tertiary care hospital in North India, a prospective comparison research was undertaken in patients with CKD.Two interventional groups were assigned to the patients. Group I (control) patients were administered conservative management and placebo, while in patients of Group II (KAA), conservative management along with KAA (600 mg, thrice daily) was administered for 12 weeks. Hemogram, renal function tests, lipid profiles, along adverse effects were recorded at 0, 4, 8, and 12 weeks of treatment.

Results:

After 12 weeks of treatment, both groups showed gradual improvement in clinical aspects, although the KAA group showed more pronounced improvement than the control group. Both groups demonstrated a steady improvement in biochemical indicators compared to their pre-treatment levels, with the KAA supplemented group showing a greater improvement. Blood glucose, blood urea, serum creatinine, and 24 hour total urine protein all decreased. Hemoglobin, total urine volume in 24 hours, and glomerular filtration rate all increased. When compared to the control group, the KAA group demonstrated a substantial (p<0.05) improvement in lipid profiles.In terms of side effects, there was no significant difference between the two groups (p>0.05). Conclusion: In patients with CKD, KAA supplementation combined with conservative management is effective and safe in preventing disease progression.

Expanded Form - Concept of Child Care in Ayurveda

Dilip Kumar Goswami

Technological Innovation in Pharmaceutical Research Vol. 9, 19 July 2021, Page 81-84
https://doi.org/10.9734/bpi/tipr/v9/10853D

Childhood is the determinant of the adulthood. A fetus, after developing in the mother's womb, takes birth as a newborn baby and gradually becomes a man. Childhood is such a period of life when both the anatomical and physiological developments remain incomplete. The resistance of the children are also poor. Even they cannot differentiate the useful and harmful objects. They want to play with the poisonous snake also. To speak in brief a child is vulnerable to danger in respect of disease, injury etc. due to low resistance, inability to differentiate the beneficial and harmful agents etc.

The nation expects healthy children to form a healthy society. Hence utmost attention is paid towards the children with special reference to protection from diseases, injuries etc. since long past. Interestingly the ancient Ayurvedic classics also contain vivid discussion on the points of healthy conception, pregnancy, delivery, child care etc. like the present time.

The Concept of Direct Perception in Ayurveda

Dilip Kr. Goswami

Technological Innovation in Pharmaceutical Research Vol. 9, 19 July 2021, Page 85-88
https://doi.org/10.9734/bpi/tipr/v9/10689D

Direct perception can be considered as the one and only dependable way to acquire knowledge from the surrounding. Though, in common sense, with the term "direct perception" "seeing an object" is understood but actually it also includes the process of acquiring knowledge through hearing , smelling, touching , taking taste through the sense organs other than the eyes, viz. ears, nose, skin and tongue. An individual acquires knowledge of an object in existence through the five sense organs.

But the practical experience establish that, an object , even in existence, may not be able to prove it's existence through direct perception due to a number of factors. A substance  can not be seen if it is too small or too large, a sound can not be perceived if it is of low pitch, smell can not be got if it is coming from a distance, a substance can not be touched if it is being pressed with another substance, taste can not be taken if the sample can not be got.

Interestingly Charaka, the founder of Indian Medicine has explained the obstacles of direct perception under the heading "PRATYAKSHYANUPALABDHI" which proves the depth of knowledge and observation of the ancient scholars.

Assessment of Quality of Life and It’s Socio-Demographic Correlates in Post Menopausal Women

Purnima Raj, Namita Deshmukh, Avinash Borkar

Technological Innovation in Pharmaceutical Research Vol. 9, 19 July 2021, Page 89-96
https://doi.org/10.9734/bpi/tipr/v9/3045F

Introduction: Menopause can include psychological, physical, and vasomotor symptoms, as well as sexual dysfunction. However, current health care models fail to realise that these symptoms have a significant impact on a woman's personal and social functioning, and hence her quality of life. As a result, the goal of this study is to determine the quality of life of postmenopausal women as well as the socio-demographic characteristics that influence quality of life.

Materials and Methods: A cross-sectional study was conducted in an urban slum area, with 105 females aged 45 to 65 years old being questioned using the MENQOL questionnaire. The study participants were interviewed for sociodemographic variables like age, duration of menopause, education, occupation, employment status, family income, marital status, number of children.

Results: The average age of the participants in this study was54.13 ± 4.05 (45-62) years. Twenty percent of the 105 postmenopausal women in the research were illiterate, while 26.7 percent had completed secondary school education. The total MEN-QOL scores varied from 62 to 148, with a mean of  101.3 ± 23.44.

Conclusion: Menopause affects a woman's physical health as well as her psychological well-being, as evidenced by the current study, which found that MEN-QOL scores were higher after menopause, indicating a lower quality of life.The bad quality of life was exacerbated by age, poorer education, lower socioeconomic level, unemployment, and a lack of spouse support.

Study on Prescribing Pattern of Fixed Dose Combinations of Antibiotics in a Post-operative Surgical Ward of Tertiary Care Teaching Hospital, India

R. Velvizhy, J. Johan Pandian

Technological Innovation in Pharmaceutical Research Vol. 9, 19 July 2021, Page 97-103
https://doi.org/10.9734/bpi/tipr/v9/10903D

Background: Fixed dose drug combinations (FDCs), are combinations of two or more active medicines. It should be utilised when the combination has a documented advantage over single medicine in efficacy, safety and compliance. Only 19 such combinations are listed by the World Health Organization (WHO). However, the Indian market is flooded with hundreds of unapproved FDCs, leading to irrational use.

Aim: This study was focused on finding out the fixed dose combination of antimicrobial agents used in the post-operative general surgery ward of a tertiary care teaching hospital.

Methods: After getting approval from institutional human ethics committee the prescriptions of patients admitted during April 2013 to March 2014 were analyzed. Demographic data, FDC prescribed by surgeons, Dose, Frequency, Duration, Route, Formulation, Brand or generic drugs, Adverse events due to use of FDC were collected and SPSS version 17 was used for statistical analysis. Fixed dose combinations were used in 90 Patients. The most commonly used FDC were ampicillin with Cloxacillin (43) followed by amoxicillin with clavulanic acid (22), cefoperazone with sulbactam (19) and piperacillin with tazobactam (6). A common drug used in combination along with FDC was metronidazole and aminoglycoside. The irrational combination seen in this study was ampicillin with Cloxacillin (8.88%) of the total FDC which is not approved by DCGI or FDA.

Results: In this study out of 145 drugs used, 41drugs were administered three times a day, 90 drugs were given two times a day and 14 drugs were given once a day dosing. 53 patients received FDCs for prophylaxis and 37 patients for treatment purpose. All FDCs were prescribed in brand names. No adverse drug reaction was observed in this study.

Conclusions: Consultants should undergo continuing medical education (CME) on newer drug combinations and their adverse drug reactions which will be evidence-based rather than to rely on representatives.

Design and Development of Taste Masked Formulations of Model Drug by Using Eudragit L-100: A Recent Study

Bhagyashri M. Raut, Bharati V. Bakade, Sayali S. Bompelwar

Technological Innovation in Pharmaceutical Research Vol. 9, 19 July 2021, Page 104-113
https://doi.org/10.9734/bpi/tipr/v9/11366D

Tenofovir disoproxil fumarate is a nucleotide reverse transcriptase inhibitor medication with a very bitter taste that plays an essential role in patient compliance in the oral dosing form. In this study, an attempt was made to mask the bitter taste of Tenofovir Disproxil Fumarate utilising a complexation process and an oral dispersible tablet formulation including super disintegrant croscarmellose sodium in various concentrations. Polymer Eudragit L -100 was used in the formulation of the complex with the Tenofovir Disproxil Fumarate. The complexes were formulated as 1:1, 1:2 and 1:3 ratios. The drug and polymer ratio were used to optimise the loading procedure. Taste masking was determined using the panel method, and the complexes were characterised using FTIR. Oral dispersible tablets were manufactured and assessed for pre-formulation and post-formulation parameters using the optimised drug-polymer complexes (1:3 ratio). The formulations were tested for thickness, hardness, diameter, weight variation, friability, disintegration time, invitro dissolution time, and stability. The test is passed by all parameters. This discovery can be used to develop a non-bitter Tenofovir Disoproxil Fumarate dosage form with high bioavailability and stability.

A Hospital Based Cross Sectional Study for Assessment of Quality of Life in Patients on Antiepileptic Drugs

Junaid A. Ahangar, Samina Farhat, Rabbanie T. Wani

Technological Innovation in Pharmaceutical Research Vol. 9, 19 July 2021, Page 114-122
https://doi.org/10.9734/bpi/tipr/v9/2848F

Background: Quality of life (QOL) is a broad, multidimensional concept that usually includes subjective evaluations of both positive and negative aspects of life. Very few studies have been carried out on QOLIE 31 in India and research in this area will identify factors affecting QOL. study was therefore conducted to determine the level of health related QOL of patients of epilepsy in a tertiary care teaching hospital. To evaluate patterns of the use of anti-epileptic drugs (AEDs) and their impact on the Quality of Life (QOL) in patients with epilepsy.

Methods: The study was a hospital based cross sectional study conducted by the Department of Pharmacology in association with the Department of Medicine, Government Medical College, Srinagar. A total number of 134 patients, aged >18 years were studied for a period of one and a half years, January 2015-July 2016. QOLIE?31 questionnaire was used for collecting data on health-related QOL.

Results: The mean overall QOLIE-31 score was 53 corresponding to a t-score of

1. Amongst the QOLIE-31 subscales, the highest mean score was the cognitive subscale (73.6) followed by medication effects (55.5) and social functions (52).

Conclusions: It is evident from our study that there are many factors that influence QOL of people with epilepsy. Among them, type of drug therapy plays an important role. Adding clinical counselling and other interventions to address the physical, mental, psychological, social, and emotional aspects of health wellbeing is likely to achieve better health outcomes for epilepsy patients.

A Histopathological Study of Proton Pump Inhibitors: Are They Safe on Kidneys?

Ramchandra Prabhakar Limaye, Shabbir Rafik Pendhari, Kedar Shashikant Joshi

Technological Innovation in Pharmaceutical Research Vol. 9, 19 July 2021, Page 123-131
https://doi.org/10.9734/bpi/tipr/v9/11342D

Background: In India, PPI is used between 45 and 85 percent of the cases. Patients with chronic renal disease were prescribed PPI in 82.96 percent of cases. However, recent case reports imply that PPI can cause AIN. Because many patients take numerous medications, it's impossible to assess the exact rate of this uncommon side event, making it much more difficult to establish a causal link between AIN and PPI. Early identification of AIN and discontinuation of the culprit drug may prevent AIN from progressing to end-stage chronic renal disease. As a result, we planned a study to determine whether or not there is a link between PPI and AIN.

Methods: The study was aimed at finding out histopathological impact of concomitant use of PPI and NSAID or AMA on experimental animal. The objectives were to find out the effect of concomitant administration of PPI with NSAIDS / antimicrobials on kidneys by histopathological studies and to compare it with normal histopathological picture to note the changes that have occurred due to drug administration. Rats weighing 150-250 gm were employed in the experiment. Omeprazole, pantoprazole, and rabeprazole were given for 28 days in three groups: group A was given nothing, group B was given diclofenac, and group C was given ofloxacin. After the 28th day, the animals with disordered RFTs were put together. Each group had two animals sacrificed. Their histopathology examinations were also completed.

Results: Each group had at least three rats with abnormal RFTs. And, with or without AIN, the majority of histopathological studies demonstrate structural and vascular alterations.

Conclusions: PPI alone are known to cause AIN, but the risk of AIN rises when other nephrotoxic drugs are added.

Study on Resveratrol Chemoprotective Effect and COX 2 Down Regulation in Tumor Suppression in DMBA Induced Breast Cancer in Female Sprague Dawley Rats

Aneena Suresh, Rajat Rana, Keerthana C.

Technological Innovation in Pharmaceutical Research Vol. 9, 19 July 2021, Page 132-139
https://doi.org/10.9734/bpi/tipr/v9/3080F

Background: The study's goal was to evaluate Resveratrol's chemoprotective role in 7,12 Dimethylbenzanthracene (DMBA) induced breast cancer in Female Sprague Dawley rats, as well as its possible role in downregulating COX 2, an enzyme known to be expressed in breast cancer tissues. Methods: A total of 40 female Sprague Dawley rats (n = 10 per group) were used in this study. 6 week old rats, group 1 on pulverised rodent diet, group 2 on DMBA and diet, group 3 on DMBA and diet with Resveratrol 100mcg, and group 4 on DMBA and diet with Resveratrol 200mcg.The trial was stopped after 120 days, and tumours were examined for multiplicity, incidence, and histology. Western blot analysis was used to look at Cox 2 expression. Values were statistically tested using one way variance and Tukey’s comparison test.

Results: In the resveratrol-treated groups, body weight and tumour volume were similar, and there was a very long latency time for tumour initiation, as well as a reduction in tumour multiplicity and incidence. Tumor incidence was 42.27±10.17 for Group 2, 21.91±5.87 for Group 3, 13.73±3.98 for group 4. Tumor multiplicity was reported as 0.8909±0.30 for group 2, 0.1036±0.04 for group 3, 0.04545±0.02 for group 4. Histopathological analysis revealed ductal carcinoma in group 2, minor tissue necrosis in group 3 and fibroadenoma in group 4.

Conclusions: Resveratrol inhibits COX 2 expression in breast carcinoma and has a chemopreventive effect against DMBA-induced breast cancer.

Study on Isolation, Characterization, and Docking Studies of Isolated Compounds as Antidiabetic Molecules from Cressa cretica

Sangeeta Rani, Kavita Gahlot, Arvind Kumar

Technological Innovation in Pharmaceutical Research Vol. 9, 19 July 2021, Page 140-151
https://doi.org/10.9734/bpi/tipr/v9/2891F

Objective: The purpose of this study was to investigate the diabetic effect of phytocompounds isolated from Cressa cretica Linn. using spectroscopic analysis and molecular docking studies.

Methods: Coarse powder of the whole plant of C. cretica was extracted with methanol, extracted part was subjected to silica column isolation, and two compounds: 2-Isopropyl-4-(1-methyl-dodeca-2,4-dienyloxy)-benzene-1,3,5-triol (Compound CN-01) and 11-Methyl-dodeca-2,4,6,8,10-pentenoic acid 2,3-dihydroxy-5-methyl-phenyl ester (Compound CN-02) were isolated in pure form. The three-dimensional structure of target protein was downloaded from PDB (www.rcsb.org) Protein Data Bank, Ligand file CN-01 and CN-02 were converted to MDL Molfile (V2000) format using Chem Sketch 2017.2.1. These files could not be used directly in AutoDock 4.0 tools; thus, they were first converted to PDB files using an open babel tool.

Results: Compounds were revealed through spectroscopic analysis and screened using AutoDock 4.0 tools. Docking study recommended that CN-01 and CN-02 an existing phytochemical from the plant of C. cretica had the highest fitness docking score and hence could be a potent antidiabetic drug.

Conclusion: In this investigation, we docked the receptor (glycogen phosphorylase protein) holds a promising lead target formation against diabetes based on molecular docking analysis (minimum hydrogen bond length and maximum docked score). Thus, these compounds can be effectively used as drugs for treating diabetes which is predicted on the basis of docking scores.