25 results on '"Md Sayeed Akhtar"'
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2. Ganoderma lucidum: Insight into antimicrobial and antioxidant properties with development of secondary metabolites
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Md Faruque Ahmad, Abdulrahman A. Alsayegh, Fakhruddin Ali Ahmad, Md Sayeed Akhtar, Sirajudeen S. Alavudeen, Farkad Bantun, Shadma Wahab, Awais Ahmed, M. Ali, Ehab Y. Elbendary, António Raposo, Nahla Kambal, and Mohamed H. Abdelrahman
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Antimicrobial ,Antioxidant ,Secondary metabolites ,Triterpenoids and polysaccharides ,Science (General) ,Q1-390 ,Social sciences (General) ,H1-99 - Abstract
Ganoderma lucidum is a versatile mushroom. Polysaccharides and triterpenoids are the major bioactive compounds and have been used as traditional medicinal mushrooms since ancient times. They are currently used as nutraceuticals and functional foods. G. lucidum extracts and their bioactive compounds have been used as an alternative to antioxidants and antimicrobial agents. Secondary metabolites with many medicinal properties make it a possible substitute that could be applied as immunomodulatory, anticancer, antimicrobial, anti-oxidant, anti-inflammatory, and anti-diabetic. The miraculous properties of secondary metabolites fascinate researchers for their development and production. Recent studies have paid close attention to the different physical, genetic, biochemical, and nutritional parameters that potentiate the production of secondary metabolites. This review is an effort to collect biologically active constituents from G. lucidum that reveal potential actions against diseases with the latest improvement in a novel technique to get maximum production of secondary metabolites. Studies are going ahead to determine the efficacy of numerous compounds and assess the valuable properties achieved by G. lucidum in favor of antimicrobial and antioxidant outcomes.
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- 2024
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3. Evaluation of public's knowledge, attitude and experiences towards the generic medications in building healthcare policy.
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Md Sayeed Akhtar and Khalid Orayj
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Medicine ,Science - Abstract
The increasing cost of prescription drugs has high concern and associated with medication nonadherence and adverse health outcomes. The use of generic prescription drugs by the patients depends on if recommended by competent healthcare providers. Generic medicines, which are cheaper and bioequivalent to brand-name drugs, offer an opportunity to reduce healthcare expenditures of Saudi Arabia's healthcare system as per the Vision 2030 plan. Therefore, the current study was conducted to assess the population awareness, attitude and perception towards the generic medications particularly those locally manufactured in Saudi Arabia. We managed a cross-sectional, questionnaire-based study and included indices like demographic sections, knowledge of generic medications, perception of generic medication use, and previous experience. Data was collected over 12 weeks from February 2022 to April 2022 using an online survey tool. A study of 462 participants found that the majority were male (54.97%), young (55.4%), with a graduate or post-graduate degree (73.5%) and employed (43.29%). The majority reported good health, with 75.5% reporting good health. The study found significant differences in knowledge about generic drugs, their country of origin, and their benefits and utility. Most participants had positive attitudes towards generic medications, with 45% believing they are as effective as those from other countries. The study also revealed a significant difference in participants' experience and usage of medications particularly satisfaction to health outcome. Enhancing healthcare professionals' perceptions of generics can positively influence patient/consumer opinions and trust in generic medicines. Patients' high trust in prescribing physicians also influences these opinions, as their opinions can influence patient/consumer opinions.
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- 2024
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4. Knowledge, attitude and preparedness of healthcare students toward basic life support at King Khalid University, Abha, Kingdom of Saudi Arabia
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Sirajudeen Shaik Alavudeen, Viqar Basharat, Ahmed Khaled Bahamdan, Vigneshwaran Easwaran, Ghadah Khaled Bahamdan, Md Sayeed Akhtar, Sultan Alshahrani, Ali Alqahtani, and Krishnaraju Venkatesan
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basic life support cardiopulmonary resuscitation ,knowledge ,attitude ,preparedness health care students ,Diseases of the circulatory (Cardiovascular) system ,RC666-701 - Abstract
Background Worldwide, millions of people die of sudden cardiac arrest every year. A well-timed cardiopulmonary resuscitation (CPR) increases the possibility of survival by two- to fourfolds. This study aimed to assess the knowledge, attitude, and preparedness of health care students toward basic life support (BLS) at King Khalid University. Methods A cross-sectional study was conducted among the health care students of King Khalid University from August to October 2020. Data were collected using a pretested, semi-structured questionnaire and the data were analyzed using Statistical Package for the Social Sciences. Resulrs The total number of participants was 346. Overall, the participant’s knowledge regarding the BLS was inadequate. Majority of the participants were not aware of the acronyms used in BLS. The level of education has a significant impact on the knowledge, whereas gender has no significant impact on the knowledge. The answers to the attitude and the preparedness items were also not satisfying. Lack of knowledge is one of the common reasons for not performing BLS. Periodical training program and refresher courses were the most recommended methods to increase the knowledge toward the BLS. Conclusion It is evident from the current study that there is a lack of knowledge and preparedness toward BLS among most health care students. It is recommended to incorporate more BLS training and refresher courses in the health care college curricula.
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- 2022
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5. Edaravone and benidipine protect myocardial damage by regulating mitochondrial stress, apoptosis signalling and cardiac biomarkers against doxorubicin-induced cardiotoxicity
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Md Quamrul Hassan, Md Sayeed Akhtar, Obaid Afzal, Ibraheem Hussain, Mohd Akhtar, Syed Ehtaishamul Haque, and Abul Kalam Najmi
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edaravone ,benidipine ,doxorubicin ,mitochondrial stress ,apoptosis ,cardiac biomarker ,Diseases of the circulatory (Cardiovascular) system ,RC666-701 - Abstract
Background: Doxorubicin (DOX) is a potential chemotherapeutic agent but its use is restricted due to cardiotoxicity. Edaravone is a potent-free radical scavenging agent used in cerebral ischaemia. Benidipine is a triple calcium channel blocker. Objective: We investigated the potential cardioprotective effects of edaravone and benidipine alone and their combination against DOX-induced cardiotoxicity. Cardiotoxicity was induced by administering six equal injections of DOX (2.5 mg/kg) on alternative days for 2 weeks. Result: DOX-treated group showed significant increase level of lipid peroxide and decrease in antioxidant status along with mitochondrial enzymatic activity. Cardiotoxity effect of DOX illustrated by significantly increased the cardiac biomarkers such as Cardiac troponin-I, Brain natriuretic peptide, Creatine kinase-MB in serum. Significant increased activation of TNF-α, Caspase-3 activity and myocardial infarct size in DOX-treated group. Histopathological evaluation also confirmed the DOX-induced cardiotoxicity. Pretreated with edaravone and benidipine was significantly attenuated level of thiobarbituric acid reactive substance, endogenous enzymes, mitochondrial enzyme activities and cardiac biomarkers. Furthermore, pretreated group showed decreased activation of TNF-α, Caspase-3 activity along with reduction in the myocardial infarct size. Histopathological evaluation also strengthened the above results. Conclusion: Taken together these results suggest that the pretreated with edaravone and benidipine have potential protective effect against DOX-induced cardiotoxicity.
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- 2020
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6. Resveratrol-Loaded Chia Seed Oil-Based Nanogel as an Anti-Inflammatory in Adjuvant-Induced Arthritis
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Obaid Afzal, Abdulamalik S. A. Altamimi, Mubarak A. Alamri, Ali Altharawi, Manal A. Alossaimi, Md Sayeed Akhtar, Fauzia Tabassum, Waleed H. Almalki, and Tanuja Singh
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resveratrol ,chia seed oil ,nanoemulsion ,phase diagram ,skin permeation ,pro-inflammatory cytokines ,Science ,Chemistry ,QD1-999 ,Inorganic chemistry ,QD146-197 ,General. Including alchemy ,QD1-65 - Abstract
Natural anti-inflammatory nutraceuticals may be useful in preventing rheumatoid arthritis from worsening. Resveratrol (RV) and chia seed oil, having antioxidant potential, can assist in avoiding oxidative stress-related disorders. This investigation developed and evaluated resveratrol-loaded chia seed oil-based nanoemulsion (NE) gel formulations through in vitro and in vivo studies. The physical stability and in vitro drug permeability of the chosen formulations (NE1 to NE10) were studied. The optimized RV-loaded nanoemulsion (NE2) had droplets with an average size of 37.48 nm that were homogeneous in shape and had a zeta potential of −18 mV. RV-NE2, with a permeability of 98.21 ± 4.32 µg/cm2/h, was gelled with 1% carbopol-940P. A 28-day anti-arthritic assessment (body weight, paw edema, and levels of pro-inflammatory mediators including TNF-α, IL-6, IL-1β, and COX-2) following topical administration of RV-NE2 gel showed significant reversal of arthritic symptoms in arthritic Wistar rats induced by Freund’s complete adjuvant injection. Therefore, RV-NE2 gel demonstrated the potential to achieve local therapeutic benefits in inflammatory arthritic conditions due to its increased topical bioavailability and balancing of pro-inflammatory mediators.
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- 2023
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7. Evaluation of Antibiotic Prescribing Practices and Antimicrobial Sensitivity Patterns in Urinary Tract Related Infectious Diseases in Pediatric Patients
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Sirajudeen S. Alavudeen, Anas Ali Asiri, Shatha Abdulrahman Fageeh, Ahmed Abdoh Aljarie, Mir Javid Iqbal, Noohu Abdulla Khan, Fauzia Tabassum, Mohamed Rahamathulla, Umme Hani, and Md Sayeed Akhtar
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urinary tract infections ,pediatric ,Escherichia coli ,sensitivity pattern ,antibacterial resistance ,Pediatrics ,RJ1-570 - Abstract
Complications of urinary tract infections (UTIs) like kidney failure and septicaemia develop once infections spread from the upper urinary tract to other parts of the body by haematogenous dissemination and they pose great health and economic burden to the countries. This retrospective study was conducted among 132 patients with bacterial UTIs in the inpatient department of tertiary care hospital in Abha, Saudi Arabia. During the study period, Escherichia coli (E. coli) and Klebsiella pneumonia (K. pneumonia) along with other 15 different bacteria were isolated. A significant difference (P < 0.05) was observed between the male and female children population in different age groups. We observed fever (84.09%) as a major symptom (P < 0.05), and seizure (9%) was reported as a major concomitant condition among UTI cases. Around 31.82% of E. coli was found to be the most common uropathogens in pediatric cases followed by 25% in K. pneumoniae. E. coli was observed to be more susceptible (92.86%) to amikacin, ceftriaxone, levofloxacin, ertapenem, gentamycin, meropenem, piperacillin-tazobactam, tigecycline, and ceftazidime. However, meropenem, tigecycline, and amikacin were observed to be effective in 100% of cases of K. pneumoniae. Meanwhile, cephalosporins were the most commonly prescribed drug category among different classes of drugs. Almost 99% of pediatric cases, based on their age, were admitted to the ward, and drugs were administered intravenously. We concluded that microbiology laboratory evidence on the causative organisms and choice of treatment together allows tailoring appropriate treatment regimens in conjunction with clinical experiences.
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- 2021
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8. Pitavastatin ameliorates myocardial damage by preventing inflammation and collagen deposition via reduced free radical generation in isoproterenol-induced cardiomyopathy
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Ramsha Iqbal, Md Sayeed Akhtar, Md Quamrul Hassan, Zeeba Jairajpuri, Mohd. Akhtar, and Abul Kalam Najmi
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isoproterenol ,pitavastatin ,hmgcoa ,oxidative stress ,bnp ,Diseases of the circulatory (Cardiovascular) system ,RC666-701 - Abstract
Pitavastatin inhibits 3 hydroxy 3 methyl glutaryl coenzyme A (HMGCoA) reductase enzyme, preventing cholesterol synthesis along with elevating high density apolipoprotein A1 (Apo-A1). The present study was designed to evaluate cardioprotective potential of pitavastatin at 1 mg/kg/day and 3 mg/kg/day dose for 14 days in low dose isoproterenol (ISO) (5 mg/kg/day for 7 consecutive days) induced myocardial damage. ISO administration induced significant reduction in endogenous antioxidant enzymes like reduced glutathione (GSH), superoxide dismutase (SOD), catalase (CAT) and raised thiobarbituric acid reactive substances (TBARS) indicating activated lipid peroxidation. Along with this, a significant increase in level of cardiac injury biomarkers vie, creatine kinase (CK-MB), lactate dehydrogenase (LDH), aspartate amino transferase (AST), tumor necrosis factor (TNF-α) and transforming growth factor (TGF-β) as well as brain natriuretic peptide (BNP). Histological examination also revealed marked myocardial tissue damage in ISO treated rats. However, pretreatment with pitavastatin (3 mg/kg/day) significantly maintained nearly normal levels of cardiac biomarkers and oxidant antioxidant status as well as lipid peroxidation in ISO induced MI rats. Cardiac histological assessment and infarct size assessment also showed marked reduction in myocardial architecture alteration including infarct size as well as collagen deposition by pitavastatin that strongly supported biochemical findings. These observations strongly corroborate that pitavastatin prevents myocardial damages via up regulation of endogenous oxidants along with its hypocholesterolemic activity.
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- 2019
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9. Sacubitril and valsartan protect from experimental myocardial infarction by ameliorating oxidative damage in Wistar rats
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Mohd Imran, Md Quamrul Hassan, Md Sayeed Akhtar, Obaid Rahman, M. Akhtar, and Abul Kalam Najmi
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aneprilysin inhibitor ,oxidative damage ,sacubitril ,valsartan ,isoproterenol ,myocardial infarction ,Diseases of the circulatory (Cardiovascular) system ,RC666-701 - Abstract
Background: Sacubitril (SAC), a neprilysin inhibitor prevent degradation of neprilysin and activate cGMP signaling pathways leading to rise in blood volume concurrent to blood pressure by means of vasoactive peptides, adrenomedullin, and bradykinin. Objective: The aim of this study was to evaluate the anti-ischemic effects of SAC through inhibiting neprilysin in isoproterenol (ISO) induced myocardial infarction (MI) in Wistar albino rats. ISO (85 mg/kg) was injected subcutaneously at the end of 14 days pre-treatment with SAC and valsartan (VAL). Result: Biochemical investigation revealed that SAC along with VAL significantly prevented the antioxidant enzymes (SOD, Catalase, GR, GPx, GST, and GSH) degradation and malondialdehyde (MDA) induced by ISO intoxication in Wistar rats. Along with this, cardiac biomarkers (LDH, CK-MB, ALT, AST, and ALP) were also significantly ameliorated by SACand VAL in ISO-treated rats. Concurrently, decreased infarction area (IA)and marked reduction in myofibril damage by SACand VAL further supported its protective benefits in MI. Conclusion: Taken together, the results suggest that inhibition of enzyme neprilysin alleviated the ISO induces myocardial damage mediated by its strong antioxidant potential.
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- 2019
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10. Potential Efficacy of β-Amyrin Targeting Mycobacterial Universal Stress Protein by In Vitro and In Silico Approach
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Md Amjad Beg, Shivangi, Obaid Afzal, Md Sayeed Akhtar, Abdulmalik S. A. Altamimi, Afzal Hussain, Md Ali Imam, Mohammad Naiyaz Ahmad, Sidharth Chopra, and Fareeda Athar
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A. aspera ,β-amyrin ,C. gigantea ,C. procera ,GC-MS ,Minimum inhibitory concentration (MIC) ,Organic chemistry ,QD241-441 - Abstract
The emergence of drug resistance and the limited number of approved antitubercular drugs prompted identification and development of new antitubercular compounds to cure Tuberculosis (TB). In this work, an attempt was made to identify potential natural compounds that target mycobacterial proteins. Three plant extracts (A. aspera, C. gigantea and C. procera) were investigated. The ethyl acetate fraction of the aerial part of A. aspera and the flower ash of C. gigantea were found to be effective against M. tuberculosis H37Rv. Furthermore, the GC-MS analysis of the plant fractions confirmed the presence of active compounds in the extracts. The Mycobacterium target proteins, i.e., available PDB dataset proteins and proteins classified in virulence, detoxification, and adaptation, were investigated. A total of ten target proteins were shortlisted for further study, identified as follows: BpoC, RipA, MazF4, RipD, TB15.3, VapC15, VapC20, VapC21, TB31.7, and MazF9. Molecular docking studies showed that β-amyrin interacted with most of these proteins and its highest binding affinity was observed with Mycobacterium Rv1636 (TB15.3) protein. The stability of the protein-ligand complex was assessed by molecular dynamic simulation, which confirmed that β-amyrin most firmly interacted with Rv1636 protein. Rv1636 is a universal stress protein, which regulates Mycobacterium growth in different stress conditions and, thus, targeting Rv1636 makes M. tuberculosis vulnerable to host-derived stress conditions.
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- 2022
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11. Impact of polycystic ovary syndrome on quality of life of women in correlation to age, basal metabolic index, education and marriage.
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Fauzia Tabassum, Chandra Jyoti, Hemali Heidi Sinha, Kavita Dhar, and Md Sayeed Akhtar
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Medicine ,Science - Abstract
Polycystic ovary syndrome (PCOS) is the major endocrine related disorder in young age women. Physical appearance, menstrual irregularity as well as infertility are considered as a sole cause of mental distress affecting health-related quality of life (HRQOL). This prospective case-control study was conducted among 100 PCOS and 200 healthy control cases attending tertiary care set up of AIIMS, Patna during year 2017 and 2018. Pre-validated questionnaires like Short Form Health survey-36 were used for evaluating impact of PCOS in women. Multivariate analysis was applied for statistical analysis. In PCOS cases, socioeconomic status was comparable in comparison to healthy control. But, PCOS cases showed significantly decreased HRQOL. The higher age of menarche, irregular/delayed menstrual history, absence of child, were significantly altered in PCOS cases than control. Number of child, frequency of pregnancy, and miscarriage were also observed higher in PCOS cases. Furthermore, in various category of age, BMI, educational status and marital status, significant differences were observed in the different domain of SF-36 between PCOS and healthy control. Altogether, increased BMI, menstrual irregularities, educational status and marital status play a major role in altering HRQOL in PCOS cases and psychological care must be given during patient care.
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- 2021
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12. Evaluation of Prescribing Pattern, Therapeutic Adherence and Occurrence of Adverse Drug Reactions in Patients with Type 2 Diabetes Mellitus
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Manju Sharma, Md. Sayeed Akhtar, Sanusi Sani, Prem Kapur, Gunjan Sharma, Fauzia Tabassum, and Mohd Faiyaz Khan
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Pharmacology (medical) ,General Pharmacology, Toxicology and Pharmaceutics - Abstract
Background: Persistent hyperglycemia in diabetes mellitus (DM) is considered the leading cause of morbidity and mortality associated with both microvascular and macrovascular complications, having a greater economic impact. This study aimed to assess the impact of socioeconomic status, prescribing patterns, and patient compliance in type 2 diabetes mellitus patients. Method: This study was carried out at the Department of Medicine and Diabetic Clinic of Hakeem Abdul Hameed (HAH) Centenary Hospital at Hamdard University, New Delhi, India. We conducted a prospective observational study on prescribing patterns and monitoring adverse drug reactions (ADRs) in patients with type 2 DM (T2DM) under standard care. We enrolled 150 confirmed cases, and data was obtained from pre-validated questionnaires and then coded and analyzed to observe the association between variables. Results: The glycosylated haemoglobin level in 56% of the cases was between 6.4 to 8.0, and cardiovascular complications were observed as the major comorbidities. 45.33 % of the cases were on mono drug therapy, and metformin (23. 52 %) was the drug of choice, followed by glimepiride (23.52 %). Among the dual drug therapies, sitagliptin with metformin and triple-drug therapy, glimepiride concurrent with metformin and voglibose was the most preferred drug in the treatment of T2DM. Sitagliptin was observed to be a major patient burden (46.213 USD). In only 7.33 % of the cases, we observed definite ADR in T2DM patients. Underprivileged awareness, mainly due to low literacy, was a major concern in the development of new cases of T2DM. Conclusion: We observed better patient compliance; however, a disease awareness program must be implemented. The use of oral hypoglycaemic drugs is still dominant in clinical practice and cardiovascular disorders as comorbidities emerge as a greater challenge in terms of patient outcome and cost burden.
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- 2022
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13. Alzheimer's Disease
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Md. Sayeed Akhtar, Moteb Khobrani, Faheem Hyder Pottoo, and Jawad ur Rahman
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- 2023
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14. Levosimendan: mechanistic insight and its diverse future aspects in cardiac care
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Md Sayeed Akhtar, Md Quamrul Hassan, Aisha Siddiqui, Sirajudeen S. Alavudeen, Obaid Afzal, Abdulmalik S.A Altamimi, Syed Obaidur Rahman, Mallika Khurana, Mohamed Jawed Ahsan, Arun Kumar Sharma, and Fauzia Tabassum
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General Medicine ,Cardiology and Cardiovascular Medicine - Abstract
Inotropic agents are generally recommended to use in patients with acute decompensated heart failure (HF) with reduced ejection fraction (HFrEF) concurrent to end-organ dysfunction. However, due to certain pharmacological limitations like developing life threatening arrhythmia and tolerance, cannot be employed as much as needed. Meanwhile, Calcium ion (Ca
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- 2022
15. Dysbiosis versus diabesity: Pathological signaling and promising therapeutic strategies
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Arun K. Sharma, Akash Sharma, Samridhi Lal, Ashish Kumar, Nirmala K. Yadav, Fauzia Tabassum, Md. Sayeed Akhtar, Mohammad Tarique Imam, Ziyad Saeed Almalki, and Monalisa Mukherjee
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Pharmacology ,Drug Discovery - Published
- 2023
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16. Potential Efficacy of
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Md Amjad, Beg, Shivangi, Obaid, Afzal, Md Sayeed, Akhtar, Abdulmalik S A, Altamimi, Afzal, Hussain, Md Ali, Imam, Mohammad Naiyaz, Ahmad, Sidharth, Chopra, and Fareeda, Athar
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Molecular Docking Simulation ,Antitubercular Agents ,Microbial Sensitivity Tests ,Mycobacterium tuberculosis ,Oleanolic Acid ,Heat-Shock Proteins - Abstract
The emergence of drug resistance and the limited number of approved antitubercular drugs prompted identification and development of new antitubercular compounds to cure
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- 2022
17. Comparative efficacy of levosimendan, ramipril, and sacubitril/valsartan in isoproterenol induced experimental heart failure: a hemodynamic and molecular approach
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Fauzia Tabassum, Md Sayeed Akhtar, Quamrul Hassan, Obaid Afzal, Abdulmalik Altamimi, Mohd. Zaheen Hassan, Arun Kumar Sharma, and Asif Ansari Shaik Mohammad
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General Medicine - Abstract
Objetive: Cardiac ischemia related myocardial damage has been considered as a major reason of heart failure. We aimed to investigate the role of levosimendan (LEVO) in comparison to ramipril and sacubitril/valsartan (Sac/Val) in preventing the damage associated to isoproterenol (ISO) induced myocardial infarction. Method: Myocardial infarction was induced by injecting subcutaneous isoproterenol (5 mg/kg once for 7 consecutive days) to establish experimental heart failure model. Simultaneously, LEVO (1 mg/kg/day), ramipril (3mg/kg/day) and Sac/Val (68 mg/kg/day) suspension were administered orally for four weeks. Results: We observed a significant correlation between ISO induced ischemia with cardiac remodeling and alterations in myocardial architecture. LEVO, ramipril, and Sac/Val significantly prevented lipid peroxidation, damage of antioxidant enzymes like superoxide dismutase, catalase, glutathione and thioredoxin reductase. We also observed their ameliorative effects in cardiac hypertrophy of myocardium evidenced by reduced heart weight to body weight ratio and transforming growth factor β related collagen deposition. LEVO, ramipril, and Sac/Val also maintained cardiac biomarkers like lactate dehydrogenase, creatine kinase-MB, brain natriuretic peptide and cardiac Troponin-I indicating reduced myocardial damage that further demonstrated by histopathological examination. Decreased sarcoplasmic endoplasmic reticulum Ca2+ATPase2a and sodium-calcium exchanger-1 protein depletion after LEVO, ramipril, and Sac/Val adminisreration indicated improved Ca2+ homeostasis during myocardial contractility. Conclusion: Our findings suggest that LEVO have comparable effects to ramipril, and Sac/Val in preventing myocardial damage via balancing oxidant-antioxidant system, decreased collagen deposition, reduced myocardial stress as well as improved Ca2+ homeostasis during myocardial contractility.
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- 2022
18. Preliminary investigation on impact of intergenerational treatment of resveratrol endorses the development of ‘super-pups’
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Arun K. Sharma, Monalisa Mukherjee, Ashish Kumar, Gunjan Sharma, Fauzia Tabassum, Md. Sayeed Akhtar, Mohammad Tarique Imam, and Ziyad Saeed Almalki
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General Medicine ,General Pharmacology, Toxicology and Pharmaceutics ,General Biochemistry, Genetics and Molecular Biology - Abstract
Redox biology balances free radical generation and scavenging systems, whereas an imbalanced cellular redox can hasten the onset of various diseases and be regarded as a Pandora's box of ailments. The current study aims to assess the pathophysiological impact of intergenerational resveratrol treatment on diabetes-related cognitive and cardio-renal disorders.Diabetic rats of the first, second, and third generations were subjected to an intergenerational treatment of resveratrol (20 mg/kg/p.o./day) for 5 months. During this period, the second generation of animals (pups of the first generation) was produced. After the adulthood of second-generation rats, they used to produce third-generation rats. The rats of each generation were evaluated for physiological parameters (BMI, litter size, and life expectancy) and the pathological impact of streptozotocin (55 mg/kg/i.p.), cognitive dysfunctions, and cardio-renal injury.The intergenerational treatment of resveratrol significantly reduced litter size and improved anthropometric parameters, life expectancy, and blood glucose levels in diabetic animals. Resveratrol treatment ameliorates oxidative stress as measured by increased serum nitrite/nitrate concentrations, SOD activity, reduced glutathione concentrations, total serum antioxidant capacity, and diminished serum TBARS level in diabetic animals. Furthermore, diabetic rats receiving intergenerational resveratrol treatment showed improved cognitive behaviour and cardio-renal functionality when compared to the disease control group.The intergenerational treatment of resveratrol improved the physiological traits and vital abilities of the heart, kidney, and brain, which endorse its antioxidant potential. Surprisingly, resveratrol treatment increases the second and third generations' resistance to neurobehavioral changes, diabetes, and -associated cardio-renal dysfunction, implying that these generations are "super-pups."
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- 2023
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19. Synthesis of stable benzimidazole derivatives bearing pyrazole as anticancer and EGFR receptor inhibitors
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M. Shahar Yar, Md. Quamrul Hassan, Zulphikar Ali, Rikeshwer Prasad Dewangan, Md. Rafi, Sangh Partap, Md. Sayeed Akhtar, Md. Jawaid Akhtar, Santosh Pasha, Anees A. Siddiqui, and Ahsan Ahmed Khan
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0301 basic medicine ,Benzimidazole ,Stereochemistry ,Antineoplastic Agents ,Apoptosis ,Pyrazole ,01 natural sciences ,Biochemistry ,Structure-Activity Relationship ,03 medical and health sciences ,chemistry.chemical_compound ,Cell Line, Tumor ,Drug Discovery ,Animals ,Humans ,Phosphorylation ,Protein Kinase Inhibitors ,Molecular Biology ,IC50 ,Cell Proliferation ,Dose-Response Relationship, Drug ,010405 organic chemistry ,Chemistry ,Organic Chemistry ,In vitro ,Rats ,0104 chemical sciences ,ErbB Receptors ,Molecular Docking Simulation ,HaCaT ,030104 developmental biology ,Liver ,Cell culture ,Cancer cell ,Pyrazoles ,Benzimidazoles ,Female ,Drug Screening Assays, Antitumor - Abstract
A new series of benzimidazole linked pyrazole derivatives were synthesized by cyclocondensation reaction through one-pot multicomponent reaction in absolute ethanol. All the synthesized compounds were tested for their in vitro anticancer activities on five human cancer cell lines including MCF-7, HaCaT, MDA-MB231, A549 and HepG2. EGFR receptor inhibitory activities were carried out for all the compounds. Majority of the compounds showed potent antiproliferative activity against the tested cancer cell lines. Compound 5a showed the most effective activity against the lungs cancer cell lines (IC50 = 2.2 µM) and EGFR binding (IC50 = 0.97 µM) affinity as compared to other members of the series. Compound 5a inhibited growth of A549 cancer cells by inducing a strong G2/M phase arrest. In addition, same compound inhibited growth of A549 cancer cells by inducing apoptosis. In molecular docking studies compound 5a was bound to the active pocket of the EGFR (PDB 1M17) with five key hydrogen bonds and two π-π interaction with binding energies ΔG = −34.581 Kcal/mol.
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- 2018
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20. 2-[(4-Chlorobenzyl) amino]-4-methyl-1,3-thiazole-5-carboxylic acid exhibits antidiabetic potential and raises insulin sensitivity via amelioration of oxidative enzymes and inflammatory cytokines in streptozotocin˗induced diabetic rats
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Md. Sayeed Akhtar, Sadia Shah, Mohd Adil, Manju Sharma, Md. Rahmat Ali, Sandhya Bawa, Yam Nath Paudel, and Ravisha Wadhwa
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Blood Glucose ,0301 basic medicine ,medicine.medical_specialty ,medicine.medical_treatment ,medicine.disease_cause ,01 natural sciences ,Diabetes Mellitus, Experimental ,Superoxide dismutase ,Lipid peroxidation ,03 medical and health sciences ,chemistry.chemical_compound ,Insulin resistance ,Internal medicine ,Diabetes mellitus ,medicine ,Hyperinsulinemia ,Animals ,Hypoglycemic Agents ,Rats, Wistar ,Pancreas ,Glycated Hemoglobin ,Pharmacology ,biology ,010405 organic chemistry ,business.industry ,Insulin ,General Medicine ,Glucose Tolerance Test ,Lipid Metabolism ,Streptozotocin ,medicine.disease ,Rats ,0104 chemical sciences ,Oxidative Stress ,Thiazoles ,030104 developmental biology ,Endocrinology ,Animals, Newborn ,Diabetes Mellitus, Type 2 ,chemistry ,biology.protein ,Cytokines ,Insulin Resistance ,business ,Oxidative stress ,medicine.drug - Abstract
Thiazole derivatives are potential candidates for drug development. They can be efficiently synthesized and are extremely active against several diseases, including diabetes. In our present study, we investigated the anti-diabetic, anti-oxidant and anti-inflammatory properties of 2-[(4-Chlorobenzyl) amino]-4-methyl-1,3-thiazole-5-carboxylic acid (BAC) a new thiazole derivative, in a streptozotocin (STZ) induced neonatal model of non-insulin dependent diabetes mellitus (NIDDM) rats. Diabetes was induced by injecting STZ (100 mg/kg) intraperitoneally to two days old pups. BAC administration for 3 weeks significantly decreased blood glucose and raised insulin level and improves insulin sensitivity ( K ITT ) level. Additionally, BAC also suppressed several inflammatory cytokines generation as evidenced by decreased levels of serum tumor necrosis factor-α and interleukin-6. In addition, BAC also protects against hyperlipidemia and liver injury. Furthermore, BAC significantly restored pancreatic lipid peroxidation, catalase, superoxide dismutase, and reduced glutathione content. Histological studies of pancreatic tissues showed normal architecture after BAC administration to diabetic rats. Altogether, our results suggest that BAC successfully reduces the blood glucose level and possesses anti-oxidant as well as anti-inflammatory activity. This leads to decreased histological damage in diabetic pancreatic tissues suggesting the possibility of future diabetes treatments.
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- 2017
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21. EGFR tyrosine kinase inhibition decreases cardiac remodeling and SERCA2a/NCX1 depletion in streptozotocin induced cardiomyopathy in C57/BL6 mice
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Abul Kalam Najmi, Yam Nath Paudel, Md. Sayeed Akhtar, Mohd Akhtar, Md. Quamrul Hassan, and Sadia Shah
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0301 basic medicine ,medicine.medical_specialty ,Diabetic Cardiomyopathies ,030204 cardiovascular system & hematology ,General Biochemistry, Genetics and Molecular Biology ,Sodium-Calcium Exchanger ,Diabetes Mellitus, Experimental ,Sarcoplasmic Reticulum Calcium-Transporting ATPases ,Superoxide dismutase ,Lipid peroxidation ,03 medical and health sciences ,chemistry.chemical_compound ,Mice ,0302 clinical medicine ,Gefitinib ,Lactate dehydrogenase ,Diabetic cardiomyopathy ,Internal medicine ,medicine ,Animals ,Epidermal growth factor receptor ,General Pharmacology, Toxicology and Pharmaceutics ,Protein Kinase Inhibitors ,Cells, Cultured ,chemistry.chemical_classification ,Reactive oxygen species ,biology ,Myocardium ,General Medicine ,medicine.disease ,Streptozotocin ,ErbB Receptors ,Mice, Inbred C57BL ,030104 developmental biology ,Endocrinology ,chemistry ,biology.protein ,Quinazolines ,medicine.drug - Abstract
Aim Epidermal growth factor receptor (EGFR) related reactive oxygen species (ROS) generation results in myocardial damage. We aimed to investigate the role of gefitinib (EGFR-tyrosine kinase inhibitor) in diabetic cardiomyopathy (DbCM). Method DbCM was induced by injecting streptozotocin (55 mg/kg for 5 consecutive days) to C57/BL6 mice intraperitoneally. Diabetic C57/BL6 mice (fasting blood glucose level ≥ 250 mg/dl) were allocated into four study groups and treated with two doses of gefitinib (30 mg/kg and 350 mg/kg per day) as well as ramipril (3 mg/kg/day) for four weeks. Key findings We observed a significant correlation between persistent hyperglycaemia with cardiac remodeling and alterations in myocardial architecture. Gefitinib significantly prevented lipid peroxidation (MDA), damage of antioxidant enzymes like superoxide dismutase (SOD), Catalase, glutathione (GSH) and thioredoxin reductase (TrxR). Gefitinib also prevented hypertrophy of myocardium evidenced by reduced heart weight to body weight ratio and TGF‑β related collagen deposition. Gefitinib maintained cardiac biomarkers like lactate dehydrogenase (LDH), Creatine Kinase‑MB, brain natriuretic peptide (BNP) and cardiac Troponin‑I (cTroponinI) indicating reduced myocardial damage. Decreased sarcoplasmic endoplasmic reticulum Ca2 + ATPase2a (SERCA2a) and sodium‑calcium exchanger-1 (NCX1) protein depletion after gefitinib administration indicated improved Ca2+ homeostasis during myocardial contractility. Histopathology and transmission electron microscopy clearly showed almost normal myofibrils and mitochondrial arrangements in gefitinib treated mice. Significance Our findings suggest that gefitinib protects myocardial damage in DbCM via balancing oxidant-antioxidant system, decreased collagen deposition as well as improved CKMB, BNP, cTroponinI and SERCA2a/NCX-1. Thereby, it indicated that gefitinib may be a potential therapeutic drug for treating DbCM.
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- 2018
22. PREVALENCE OF INDUCIBLE CLINDAMYCIN RESISTANCE IN CLINICAL ISOLATES OF METHICILLIN-RESISTANT STAPHYLOCOCCUS AUREUS MEDIATED THROUGH GENE ERMC EXPRESSION
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Tandon, Nimisha, primary, Kulkarni, Madhuri, additional, Gs, Sowmya, additional, Tabassum, Fauzia, additional, and Md, Sayeed Akhtar, additional
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- 2018
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23. Edaravone, a potent free radical scavenger and a calcium channel blocker attenuate isoproterenol induced myocardial infarction by suppressing oxidative stress, apoptotic signaling and ultrastructural damage
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Abul Kalam Najmi, Mohd Akhtar, Syed Ehtaishamul Haque, Md. Sayeed Akhtar, Md. Quamrul Hassan, and Javed Ali
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0301 basic medicine ,Male ,Dihydropyridines ,Combination therapy ,medicine.drug_class ,Myocardial Infarction ,Apoptosis ,Calcium channel blocker ,030204 cardiovascular system & hematology ,Pharmacology ,medicine.disease_cause ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Malondialdehyde ,Edaravone ,Medicine ,Animals ,Pharmacology (medical) ,Myocardial infarction ,Rats, Wistar ,Original Research ,business.industry ,Caspase 3 ,Myocardium ,Isoproterenol ,Free Radical Scavengers ,Free radical scavenger ,medicine.disease ,Calcium Channel Blockers ,Rats ,Oxidative Stress ,030104 developmental biology ,C-Reactive Protein ,chemistry ,Biochemistry ,Benidipine ,Female ,Cardiology and Cardiovascular Medicine ,business ,Oxidative stress ,Antipyrine - Abstract
Objectives: In the present study, we investigated whether combination therapy of low-dose benidipine with the potent free radical scavenger edaravone has a cardioprotective effect against isoproterenol (ISO)-induced myocardial infarction (MI) in Wistar rats. Methods: Rats were pretreated with concurrent doses of benidipine and edaravone (1 μg/kg/day + 1 mg/kg/day and 3 μg/kg/day + 3 mg/kg/day) by intravenous (i.v.) and intraperitoneal (i.p.) routes respectively for 28 days, followed by MI induction using ISO (85 mg/kg) by subcutaneous route for two days at 24 h intervals. After the treatment period, blood was withdrawn and the heart was preserved for biochemical estimations. Results: The activities of the cardiac biomarkers (lactate dehydrogenase and creatine kinase-MB), and the level of malondialdehyde (MDA) significantly increased, while antioxidant markers (reduced glutathione, catalase, superoxidase dismutase, glutathione peroxidase, glutathione reductase) were significantly decreased in the ISO intoxicated group compared with the control group. Moreover, the level of C-reactive protein (CRP) and Caspase-3 activity significantly increased in ISO-intoxicated group. An ultrastructure study was also carried out. Pretreatment with a combination of benidipine and edaravone significantly attenuated the activities of the cardiac biomarkers and the level of MDA, and significantly increased the antioxidant markers compared with the ISO-intoxicated group. Furthermore, pretreatment with the combination of benidipine and edaravone significantly decreased the level of CRP and Caspase-3 activity as compared to the ISO-treated group. The ultrastructure study of myocardium revealed that pretreated groups preserved the mitochondrial shape, the membrane and its internal structures. Conclusion: Taken together these results suggest that the combination of benidipine and edaravone showed significant protective effect in ISO-induced MI.
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- 2016
24. Development of Bedaquiline-Loaded SNEDDS Using Quality by Design (QbD) Approach to Improve Biopharmaceutical Attributes for the Management of Multidrug-Resistant Tuberculosis (MDR-TB)
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Rao Nargis Jahan, Zafar Khan, Md. Sayeed Akhtar, Mohd Danish Ansari, Pavitra Solanki, Farhan J. Ahmad, Mohd Aqil, and Yasmin Sultana
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bedaquiline ,oral bioavailability ,solubility ,quality by design (QbD) ,pseudo-ternary ,self-nanoemulsifying drug delivery systems (SNEDDS) ,Therapeutics. Pharmacology ,RM1-950 - Abstract
Background: The ever-growing emergence of antibiotic resistance associated with tuberculosis (TB) has become a global challenge. In 2012, the USFDA gave expedited approval to bedaquiline (BDQ) as a new treatment for drug-resistant TB in adults when no other viable options are available. BDQ is a diarylquinoline derivative and exhibits targeted action on mycobacterium tuberculosis, but due to poor solubility, the desired therapeutic action is not achieved. Objective: To develop a QbD-based self-nanoemulsifying drug delivery system of bedaquiline using various oils, surfactants, and co-surfactants. Methods: The quality target product profile (QTPP) and critical quality attributes (CQAs) were identified with a patient-centric approach, which facilitated the selection of critical material attributes (CMAs) during pre-formulation studies and initial risk assessment. Caprylic acid as a lipid, propylene glycol as a surfactant, and Transcutol-P as a co-surfactant were selected as CMAs for the formulation of bedaquiline fumarate SNEDDS. Pseudo-ternary phase diagrams were constructed to determine the optimal ratio of oil and Smix. To optimize the formulation, a Box–Benkhen design (BBD) was used. The optimized formulation (BDQ-F-SNEDSS) was further evaluated for parameters such as droplet size, polydispersity index (PDI), percentage transmittance, dilution studies, stability studies, and cell toxicity through the A549 cell. Results: Optimized BDQ-F-SNEDDS showed well-formed droplets of 98.88 ± 2.1 nm with a zeta potential of 21.16 mV. In vitro studies showed enhanced drug release with a high degree of stability at 25 ± 2 °C, 60 ± 5% and 40 ± 2 °C, 75 ± 5%. Furthermore, BDQ-F-SNEDDS showed promising cell viability in A549 cells, indicating BDQ-F-SNEDDS as a safer formulation for oral delivery. Conclusion: Finally, it was concluded that the utilization of a QbD approach in the development of BDQ-F-loaded SNEDDS offers a promising strategy to improve the biopharmaceutical properties of the drug, resulting in potential cost and time savings.
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- 2023
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25. Investigating miRNA subfamilies: Can they assist in the early diagnosis of acute myocardial infarction?
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Sharma AK, Bisht P, Gupta B, Sayeed Akhtar MD, Shaik Alavudeen S, Afzal O, and Sa Altamimi A
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- Humans, Biomarkers, Prognosis, Early Diagnosis, MicroRNAs genetics, Myocardial Infarction diagnosis, Myocardial Infarction genetics
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This report focuses on small non-coding RNA molecules (miRNAs), which have emerged as potential biomarkers with variable diagnostic values and false-positives in different conditions that limit their clinical preference. Current investigations focus on small non-coding RNA molecules (miRNAs), which have emerged as potential biomarkers with variable diagnostic values and false-positives in different conditions that limit their clinical preference. We thoroughly scrutinize the leading pathology of myocardial infarction and contemporary alterations in miRNAs for their specificity, stability and significant prognostic value at the early stage of acute myocardial infarction (AMI). Based on secondary data analysis, we explore common biomarkers and further investigate included miRNA biomarkers for their specificity, stability and area under the curve (AUC) values. We conclude that a group of novel biomarkers, including miRNA-1, miRNA-208a/b and miRNA-499, could help predict the emergence of AMI at an early stage., (Copyright © 2023 Elsevier Ltd. All rights reserved.)
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- 2023
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