Editor(s)
Dr. M.V.N.L. Chaitanya
Associate professor,
Chitkara college of pharmacy Chitkara university Punjab, India.

 

ISBN 978-93-5547-082-9 (Print)
ISBN 978-93-5547-090-4 (eBook)
DOI: 10.9734/bpi/caprd/v7

 

This book covers key areas of Pharmaceutical Research and Development. The contributions by the authors include  genetic instability, risk assessment, epigenetic alteration, single nucleotide polymorphism, environmental stress, diet, oxidative stress, aging, cardiovascular disease, systemic health care, multi-omics, fish immunity, antimicrobial activity, bioactive compounds, feed conversion, pancytopenia, megaloblastic anaemia, scrub typhus, epigenetic drugs, virtual screening, AutoDock, hydrogen bond, histogram, cluster, histone H3B E6K mutant, DNA methyltransferase, allopathic drug, COVID 19, telemedicine, disintegration time, mouth dissolving film, virgin coconut oil, oxidative enzymes, gluthatione, transepithelial electrical resistance, cell desquamation, heavy metals, detoxification, herbal formula, hyperaccumulator species, human health, medicinal plants, antiviral properties, reverse phase high performance liquid chromatography. This book contains various materials suitable for students, researchers and academicians in the field of Pharmaceutical Research and Development.

 

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Chapters


Cardiovascular Disease (CVD) and Genomics Imbalance to Risk Oxidative Stress Following Environmental Stress: Molecular Vitality for Prediction and Prevention

Aleq M. Jaffery, Yoon Ju Lee, Diane E. Heck, Hong Duck Kim

Current Aspects in Pharmaceutical Research and Development Vol. 7, 21 January 2022, Page 1-6
https://doi.org/10.9734/bpi/caprd/v7/2299C

Cardiovascular disease (CVD) is one of high burdens accompanied with health cost and intensive care by personalized prevention platforms including various drug options. It develops differently following risk factors (i.e., smoking, high fat diet, alcohol, stressor, and sedentary behavior) which may cause blood flow and heart dysfunction such as microvascular dysfunction (eg. Artery diseases), myocardial infarction (MI), arrhythmias, angina, and atherosclerosis. There are still bias CVD pathogenesis and endpoint variation between plaque formation and risk factors derived from intrinsic (or genetic risk) or extrinsic (or environmental risk). In previous studies Lipoprotein is predominantly affected to blood flow and plaque formation in previous studies. In addition, there is compelling evidence to emphasize several risk factors in patient history such as a high blood pressure, vascular damage to heart value, and metabolic disorder could be associated with diets which may contribute to developing heart failure and stroke in clinic and animal models like apoE transgenic animals. In this report, we review molecular tools (i.e., multidimensional Omics or systemic biology equipped with various detection module like genomics, proteomics, metabolomics, and pharmacogenomics, etc) for support early prediction and prevention patient from environmental risks and conduct systematic health care align with surveillance and monitoring including molecular sensitivity and validation combined with traditional imaging system in therapeutic and prevention options to reduce drug insensitivity upon individual genetic diversity which may observed in several metabolic symptoms in the aging population

Using Genomics, we visualized patient’s genomics variation or polymorphism by accessing DNA sequences for a comparison to those unaffected.  Those output is worth determining what genes are mutated and who are more at risk due to their genetic makeup.  Furthermore, proteomics will enhance the study of targeting proteins, including their locations, structures, and functions to better regulate the cardiopathy or cardiac malfunction.  Metabolomics is the Omics tool for studying drug efficacy and metabolism that are involved in the transmission of cardiopathies.  Moreover, Metabolite’s identification can enhance one’s knowledge of metabolic pathways to high fat diets, and how certain environmental factors and genetic factors surrounding blood flow and altered molecular networks in plaque formation can affect cardiac dysfunction and its regulatory pathways.  Finally, pharmacogenomics will help determine effective drugs on a more personalized based approach to ensure that anyone with any form of metabolic disorder or hypertension has a predisposition chronic diseases pattern.  This will specifically enlighten the value of systemic detection using molecular tools by integrating to target, Lipoproteins, the correct focus in early cardiomyopathy process and validation in various therapeutic endpoints to ensure quality outcomes.

The Use of Medicinal Herbs in Aquaculture Industry: A Review

Irwan Effendi, Dessy Yoswaty, Henni Syawal, Brian Austin, Alastair Robert Lyndon, Ronal Kurniawan, Sri Wahyuni, Ahmed Al-Harbi

Current Aspects in Pharmaceutical Research and Development Vol. 7, 21 January 2022, Page 7-20
https://doi.org/10.9734/bpi/caprd/v7/2190C

Fish from the aquaculture industry will continue to be one of the mainstays in meeting human animal protein needs. Various global challenges face the aquaculture industry. Starting from the issue of environmental degradation, water pollution, conversion of agricultural land and aquaculture, to diseases attacks and the use of antibiotics to control fish pests and diseases. The presence of antibiotics and insecticides in food is no longer acceptable. Therefore, it is necessary to find an environmentally friendly solution for this disease and disturbance of water and environmental pollution. The use of natural ingredients in the form of medicinal plants to increase fish immunity and treat infectious diseases is a promising option. Water and environmental pollution are increasingly inevitable and the use of plants for the bioremediation process is the right choice. This paper presents a review of research on the use of several plant species that may be used for the purposes of improvement of fish immunity, enhancement of antimicrobial activity, replacement of the role of antibiotics, improvement of fish growth, improvement of feed conversion, and water quality improvement of polluted waters.

Background: Bicytopenia and Pancytopenia are relatively common presentations in adults as compared to paediatric patients. Clinical features present in different manifestations in children with Pancytopenia/Bicytopenia, which can range from bone marrow suppression temporarily to marrow infiltration by life-threatening malignancies. The bone marrow findings may vary depending on the causative factors, from normocellular with non-specific changes to hypercellular being overshadowed by malignant cells.

Aim: To study the clinical and haematological profile in the paediatric age group with Cytopenias. The study aims to analyze the severity of hematological findings as per causative factors in patients with Pancytopenia and Bicytopenia.

Methods: Prospective Observational Study conducted in the Department of Paediatrics in Dr. RPGMC Tanda Himachal Pradesh (INDIA). The study included all patients except those falling in the exclusion criteria. It was performed after oral and written informed consent.A total of 50 children admitted with bicytopenia and pancytopenia were enrolled from March 2013 to March pancytopenia. Bicytopenia was seen in 14 (20%) and pancytopenia in 8 (16%) cases with infection. Scrub typhus was the commonest Infection seen in 18(32%).Leukaemia was notedin 11(22%) cases.

Conclusions: The commonest age group affected was 11-15 years with female domination with a Male: Female ratio of 0.78:1. The commonest symptom was fever 37(74%) then generalized weakness in 29 (58%) cases.Pallor was the most common sign in 43(86%) followed by Hepatomegaly 32(64%), Lymphadenopathy 30(60%), and Splenomeagly in 29 (58%) patients. Infection was the commonest etiology followed by leukemia and megaloblastic anaemia. Scrub typhus was the commonest infection encountered in the present study.

Objective: Over the last 30 years, cancer epigenetics research has grown extensively. Epigenetic events are involved throughout the entire human lifecycle, from embryogenesis to adulthood. It is note-worthy to recognize that epigenetic misregulation could substantiate the development of cancer and we need to continue to look for anti-neoplastic epi-drugs. Taking into consideration this phenomenon, our first aim is to search for an effective epi-drugs by virtual screening from ZINC database and to explore the validity of the virtual screening. The second aim is to explore a binding conformation of the top affinity ligands against macromolecules, by docking experiment.

Methods: The virtual screening was conducted by our Virtual Screening by Docking (VSDK) algorithm and procedure. Small molecules were randomly downloaded by ZINC database. For docking experiment, AutoDock 4.2.6 and AutoDock Tool were used.

Results: It took eight to ten hours for the successful virtual screening of the 2778 small compounds retrieved at random from ZINC database. Among histone H2B E76K mutant (HHEM) inhibitors and DNA methyltransferase (DNMT) inhibitors, the first ranked inhibitors were 1H-1,2,4- triazole-3,5-diamine and 2-ethyl-1,3,4-oxadiazole respectively.

Conclusion: As for the molecular structures obtained from virtual screening, most of the top ten HHEM and DNMT inhibitors contained 5-member rings. More than two times in affinity difference between the top and bottom ten compounds would indicate a successful virtual screening experiment. The histogram chart of AutoDock4 runs appeared in the lowest affinity region with two or three hydrogen bonds indicating a reliable conformation docking.

Medicinal Effects of Mollugo cerviana - A Brief Review

A. A. Aglin

Current Aspects in Pharmaceutical Research and Development Vol. 7, 21 January 2022, Page 45-51
https://doi.org/10.9734/bpi/caprd/v7/4346F

Over the past few years, human kind have been diagnosed with a wide range of infections and disorders. However, there are fewer effective allopathic drugs on the market. The increased knowledge in disease pathogenesis and bioactive components in last few years helps in the development of drugs.  Based on knowledge from Ayurveda and Siddha practises, the immune system is supported in this scenario by using plant extracts. Mollugo cerviana is a phytochemical-rich herb that is available in India (commonly known as thread stem carpet weed). This plant is used to treat fever, stomach aches, jaundice, gout, and rheumatism. It is also used to encourage vaginal discharge following childbirth. The plant has antimicrobial, anti-inflammatory, antioxidant, and spermicidal properties. Because of the presence of phytochemicals such as carbohydrates, saponins, tannins, terpenoids, flavonoids, steroids, phenols, proteins, and alkaloids, the plant has hepatoprotective efficiency and photoprotective capacity in excess. In short, the plant extract is responsible for the majority of the medicinal applications. This review is a compilation of useful studies on Mollugo cerviana and its bioactivities.

Current Perspectives of Telemedicine in COVID-19

Imrana Masood

Current Aspects in Pharmaceutical Research and Development Vol. 7, 21 January 2022, Page 52-56
https://doi.org/10.9734/bpi/caprd/v7/15157D

The current Pandemic of COVID-19 has led to renewed focus on Telehealth resources in order to contain the spread of the disease as well as to reach out to wider areas of population. This article discusses the current scenario of Telehealth services in India and ways to make it more accessible affordable and acceptable to all.

Formulation and Evaluation of Captopril Mouth Dissolving Film: A Recent Study

V. T. Iswariya, P. Deepika, Sowjanya Battu

Current Aspects in Pharmaceutical Research and Development Vol. 7, 21 January 2022, Page 57-64
https://doi.org/10.9734/bpi/caprd/v7/15251D

Now a day's fast dissolving films are preferred over conventional tablets and capsules for masking the taste of bitter drugs to increase the patient compliance. Fast dissolving films consist of a very thin oral strip which dissolves in less than one minute when placed on the tongue. The goal of this research is to develop captopril mouth dissolving films and evaluate the impact of various formulation factors on the physical and mechanical properties of the films, as well as drug release behaviour. In different grades, hydroxypropyl methyl cellulose (HPMC E15 and K4M) was employed as the film forming polymer.  The various manufacturing techniques for the preparation of films have also been detailed in the review. Formulation disintegration times were determined to be in the range of (52 2.5 to 125.6 2.02 s). Formula F2 had the fastest disintegration time in vitro (52 2.5 s) and was determined to be acceptable for film production with ideal physicochemical qualities, faster disintegration, and optimal in vitro release. It may be concluded that the solvent casting approach can be used to make captopril mouth dissolving films with a higher dissolution rate and greater patient compliance.

Determination of Atrazine/Streptozotocin-Induced Oxidative Stress and Mitigating Effect of Virgin Coconut Oil in Male Wistar Rats

Olatunbosun Titilope Helen, Uka Emmanuel, Asuquo Etim Asuquo, Jessica David Utibe, Otanwa Oladunni Omolabake, Akwo-Nelson Violet

Current Aspects in Pharmaceutical Research and Development Vol. 7, 21 January 2022, Page 65-82
https://doi.org/10.9734/bpi/caprd/v7/5116F

The purpose of this study is to assess the ameliorative effect of Virgin Coconut Oil (VCO) following atrazine-induced metabolic derangement in rats. The research used adult male albino wistar rats weighing 180-200g body weight. They were divided into two major experimental groups at random (The test and recovery groups). Thirty-five (35) rats were randomly divided into five sub-groups of seven rats each (n=7) in the test group and were handled as follows: Subgroup (SG) 1 served as the normal control and received 10ml/kg body weight of distilled water, SG 2 received 10 ml/kg of VCO, SG 3 received 123mg/kg of Atrazine (ATZ), SG 4 was the diabetic control that was left untreated, and SG 5 was the diabetic group that received 10 ml/kg of VCO. The test group received treatment for two weeks, after which the animals were sacrificed and blood was collected for analysis. During these two weeks, thirty-five rats from the recovery group were divided into five sub-groups of seven rats each (n=7) and treated as follows: SG 1 served as the control group, receiving 10 ml/kg body weight of distilled water, SG 2 received 10 ml/kg of VCO, and SG 3, 4, and 5 received 123 mg/kg of ATZ. After 2 weeks, the animals were re-treated for recovery as follows: SG 1 was given 10ml/kg body weight of distilled water, SG 2 was given 10ml/kg of VCO, SG 3 was given 123mg/kg of ATZ, SG 4 was given 10ml/kg of VCO, and SG 5 was given 10ml/kg of distilled water.  After two weeks, the animals were sacrificed and their blood was collected for analysis. When compared to the normal control, Gluthatione (GSH), Superoxide Dismutase (SOD), and Catalase (CAT) levels were significantly lower (p0.05) in the atrazine and diabetic groups. Following recovery, GSH levels in the VCO recovery group were significantly higher (p<0.05) than in the ATZ group. Finally, ATZ toxicity caused oxidative stress, but its withdrawal significantly reduced stress, with a more pronounced effect after VCO administration.

Controlled Desquamation of Urinary Bladder Epithelium by Cationic Polymer Poly-L-Lysine

Andreja Erman, Mojca Kerec Kos

Current Aspects in Pharmaceutical Research and Development Vol. 7, 21 January 2022, Page 83-95
https://doi.org/10.9734/bpi/caprd/v7/1794A

The aim of our study was to evaluate the experimental conditions under which the cationic polymer poly-L-lysine induces effective and safe desquamation of the urinary bladder epithelium, also called the urothelium. Induced desquamation of the urothelium is a frequently used approach in studies of urothelium regeneration and also to establish animal disease models. Chitosan has previously been shown to induce large-scale desquamation of urothelial cells. We have investigated the desquamation ability of another positively charged polymer poly-L-lysine. Its effect on the functional and structural integrity of the urothelium was studied in ex vivo and in vivo experiments. The results revealed that the effect of poly-L-lysine on the structure and function of the urothelium was mainly influenced by the concentration of the polymer, while the treatment time and the molecular weight of poly-L-lysine had little effect. Fifteen minutes exposure of the urothelium to 0.01% poly-L-lysine was found to be efficient and safe in ex vivo and in vivo experiments and resulted in intense cell desquamation, which was limited to the superficial cell layer only. Functional and structural regeneration of the urothelium occurred ex vivo within 2 to 3 hours after the induced injury by poly-L-lysine. Therefore, poly-L-lysine is a promising inducer of urothelial cells desquamation that has the potential to be used in the clinic for the treatment of urologic disorders.

Detoxification Capacity and Protective Effects of Medicinal Plants against Heavy Metals in Polluted Human Systems: A Recent Study

Mardi M. Algandaby, Khadiga M. Al-Hadead, Salama M. El-Darier

Current Aspects in Pharmaceutical Research and Development Vol. 7, 21 January 2022, Page 96-105
https://doi.org/10.9734/bpi/caprd/v7/15281D

The primary goal of this study was to recommend specific herbal formulas as supplements in polluted human societies in order to reduce the harmful effects of prevailing heavy metals. The concentrations of various heavy metals in Abu Qir, Amreyya, and Abis districts were determined, as well as the various methods by which these metals were introduced into the body system. There are many ways by which heavy metals can be broadcasted into the body such as ingesting of foods, beverages, skin exposure and inhaled air. Based on the types of heavy metals and their concentrations, a herbal assemblage (ACOSTU) was created.  The results of the herbal assembly application for six months showed a significant improvement in the medical examined cases recorded in the study areas. The study concluded that the implementation of health-care-specific programmes for people living in polluted areas is critical as part of a long-term development strategy to save endangered rural communities.

Medicinal Plant-derived Compounds as Potential Phytotherapy for COVID-19 Disease: A Review

Salama M. El-Darier, Suzan A. Rashed, Ayat Fayez, Sarah S. Hassanein, Muhammed R. Sharaby, Noran M. Tawfik, Heba Mansour, Mohamed Adel

Current Aspects in Pharmaceutical Research and Development Vol. 7, 21 January 2022, Page 106-125
https://doi.org/10.9734/bpi/caprd/v7/15279D

Currently, the human being faces a contagious virus called SARS-CoV-2 with a high transmission ability, infection, and a relatively high mortality rate, especially for the elderly. General symptoms of the disease involve fever, sore throat, pneumonia, cough, headache, diarrhea, muscle pain, shortness of breath, renal failure, and even death. All research interest is directed to finding a drug or vaccine to save millions of people’s lives; some have succeeded and applied now in some countries. Medicinal plants represent a green treasure that renders plentiful primary and secondary metabolites characterized by potent biological activities. Interestingly, the secondary metabolites, alkaloids, flavonoids, tannins, and terpenoids, own a broad antiviral history. The plant antiviral capabilities may be due to inhibition of viral attachment to/penetration of the host cell; inhibition of the virus replication; suppressing RNA replication; down regulation of viral proteins translation; interfering with virus non-structural/structural protein; down regulation of virus-induced pro-inflammatory/inflammatory signaling pathways in the host cell, and antioxidant activity thus abating the virus-induced oxidative stress effect. Presently, as we are trapped with a surly virus, there are attempts to exploit the power of nature. Therefore, the main objective of this review is to refer to some medicinal plants or their derivatives that limit the virus’s virulence or alleviate the symptoms associated with this virus.

Assessment of Phenazone and Lidocaine Hydrochloride in Bulk and Pharmaceutical Dosage Form by Using RP-HPLC Method

Charushila J. Bhangale, Shivanand Hiremath

Current Aspects in Pharmaceutical Research and Development Vol. 7, 21 January 2022, Page 126-136
https://doi.org/10.9734/bpi/caprd/v7/1737A

An attempt has been made to develop an accurate, specific and reproducible method for the determination of Phenazone (PNZ) and Lidocaine (LID) in combined dosage forms in presence of degradation product for the content analysis during stability studies from pharmaceutical dosage form. Pharmaceutical grade of Phenazone and Lidocaine HCL kindly supplied as a gift sample by Glenmark Pharmaceutical Ltd., Nashik, India. Recovery studies by standard addition method were performed in view of justifying accuracy of the proposed methods. Previously analysed samples containing LID and PNZ was spiked with standard LID and PNZ, and the mixtures were analysed in triplicate (n=3) by proposed methods. The results of robustness testing showed that little change of method conditions, such as pH of the mobile phase, composition of the mobile phase, temperature, flow rate, and wavelength, does not affect the method significantly, and so it is robust within the acceptable limits. Percent of recovery was within the range of for LID 99.0% to 101.0% and for PNZ was found to be 99.65-101.23%. The % R.S.D. less than two values indicated robustness of the method. The proposed HPLC methodprovide simple, accurate and reproducible quantitative analysis for determination of PNZ and LID and in tablet. As the method could effectively separate the drugs from their degradation products; therefore, it can be employed as a stability indicating study.