Browsing by Author "Zehravi, Mehrukh"

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A rapid and large volume synthesis of mono-, di-, tri-, and tetra-substituted imidazole derivatives via ultrasonic radiation-driven technique
(Scopus, 2024-01-12) Shaikh, Mohd Sayeed; Kale, Mayura A.; Zehravi, Mehrukh; Unnisa, Aziz; Haque, M. Akiful; Kumar, Kusuma Praveen; Khan, Sharuk L.; Siddiqui, Syed Sarfaraz Ali Falak A.; Khandaker, Mayeen Uddin
Sonochemistry under controlled conditions has proven effective in medicinal chemistry and drug development. It can substantially shorten reaction timelines from days or hours to minutes. A convenient one-pot synthesis of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives catalyzed by PTSA and benzenesulfonic acid in ethanol as solvent, under ultrasonic irradiation and without ultrasound irradiation at 50° C has been achieved successfully. These 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives synthesis were also accomplished using different solvents viz., Methanol, Ethanol, DCM, DMF, Acetonitrile and THF and PTSA as the catalyst. This method yielded the highest % synthesis of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives with PTSA as the catalyst in solvent ethanol. These reactions were also optimized for % of PTSA catalyst required to obtain the maximum yield of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives with and without ultrasound irradiation at 50° C. Synthesis of 2,4,5-trisubstituted Imidazole derivatives reaction follows first-order rate kinetics while that of 1,2,4,5-tetrasubstituted Imidazole derivatives reaction follows the second-order rate kinetics. Furthermore, sonochemistry has higher yields, lower cost, easier workups, and higher purity than conventional thermal organic synthesis, which has lower yields, tedious workups, longer reaction periods, lower purity, and numerous byproducts.
A Rapid and Large Volume Synthesis of Mono-, Di-, Tri-, and Tetra-Substituted Imidazole Derivatives via Ultrasonic Radiation-Driven Technique
(Taylor & Francis Group, 2024-01-12) Shaikh, Mohd Sayeed; Kale, Mayura A.; Zehravi, Mehrukh; Unnisa, Aziz; Haque, M. Akiful; Kumar, Kusuma Praveen; Khan, Sharuk L.; Ali, Syed Sarfaraz; Siddiqui, Falak A.; Emran, Talha Bin; Elrahim, Elrashed Abd; Khandaker, Mayeen Uddin
Sonochemistry under controlled conditions has proven effective in medicinal chemistry and drug development. It can substantially shorten reaction timelines from days or hours to minutes. A convenient one-pot synthesis of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives catalyzed by PTSA and benzenesulfonic acid in ethanol as solvent, under ultrasonic irradiation and without ultrasound irradiation at 50° C has been achieved successfully. These 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives synthesis were also accomplished using different solvents viz., Methanol, Ethanol, DCM, DMF, Acetonitrile and THF and PTSA as the catalyst. This method yielded the highest % synthesis of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives with PTSA as the catalyst in solvent ethanol. These reactions were also optimized for % of PTSA catalyst required to obtain the maximum yield of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives with and without ultrasound irradiation at 50° C. Synthesis of 2,4,5-trisubstituted Imidazole derivatives reaction follows first-order rate kinetics while that of 1,2,4,5-tetrasubstituted Imidazole derivatives reaction follows the second-order rate kinetics. Furthermore, sonochemistry has higher yields, lower cost, easier workups, and higher purity than conventional thermal organic synthesis, which has lower yields, tedious workups, longer reaction periods, lower purity, and numerous byproducts.
Alkaloid-based modulators of the PI3K/Akt/mTOR pathway for cancer therapy: Understandings from pharmacological point of view
(Scopus, 2024) Mokhfi, Fatima Zohra; Amin, Md Al; Zehravi, Mehrukh; Sweilam, Sherouk Hussein; Arjun, Uppuluri Varuna Naga Venkata; Gupta, Jeetendra Kumar; Vallamkonda, Bhaskar; Balakrishnan, Anitha; Challa, Manjula; Singh, Jyoti; Prasad, P. Dharani; Ali, Syed Salman; Ahmad, Irfan; Doukani, Koula; Emran, Talha Bin
This review aims to summarize the role of alkaloids as potential modulators of the PI3K/Akt/mTOR (PAMT) pathway in cancer therapy. The PAMT pathway plays a critical role in cell growth, survival, and metabolism, and its dysregulation contributes to cancer hallmarks. In healthy cells, this pathway is tightly controlled. However, this pathway is frequently dysregulated in cancers and becomes abnormally active. This can happen due to mutations in genes within the pathway itself or due to other factors. This chronic overactivity promotes cancer hallmarks such as uncontrolled cell division, resistance to cell death, and increased blood vessel formation to nourish the tumor. As a result, the PAMT pathway is a crucial therapeutic target for cancer. Researchers are developing drugs that specifically target different components of this pathway, aiming to turn it off and slow cancer progression. Alkaloids, a class of naturally occurring nitrogen-containing molecules found in plants, have emerged as potential therapeutic agents. These alkaloids can target different points within the PAMT pathway, inhibiting its activity and potentially resulting in cancer cell death or suppression of tumor growth. Research is ongoing to explore the role of various alkaloids in cancer treatment. Berberine reduces mTOR activity and increases apoptosis by targeting the PAMT pathway, inhibiting cancer cell proliferation. Lycorine inhibits Akt phosphorylation and mTOR activation, increasing pro-apoptotic protein production and decreasing cell viability. In glioblastoma models, harmine suppresses mTORC1. This review focuses on alkaloids such as evodiamine, hirsuteine, chaetocochin J, indole-3-carbinol, noscapine, berberine, piperlongumine, and so on, which have shown promise in targeting the PAMT pathway. Clinical studies evaluating alkaloids as part of cancer treatment are underway, and their potential impact on patient outcomes is being investigated. In summary, alkaloids represent a promising avenue for targeting the dysregulated PAMT pathway in cancer, and further research is warranted.
Alkaloid-based Modulators of the PI3K/AKT/MTOR Pathway for Cancer Therapy: Understandings from Pharmacological Point of View
(Elsevier, 2024-10-01) Mokhfi, Fatima Zohra; Amin, Md Al; Zehravi, Mehrukh; Sweilam, Sherouk Hussein; Arjun, Uppuluri Varuna Naga Venkata; Gupta, Jeetendra Kumar; Vallamkonda, Bhaskar; Balakrishnan, Anitha; Challa, Manjula; Singh, Jyoti; Prasad, Dharani; Ali, Syed Salman; Ahmad, Irfan; Doukani, Koula; Emran, Talha Bin
This review aims to summarize the role of alkaloids as potential modulators of the PI3K/Akt/mTOR (PAMT) pathway in cancer therapy. The PAMT pathway plays a critical role in cell growth, survival, and metabolism, and its dysregulation contributes to cancer hallmarks. In healthy cells, this pathway is tightly controlled. However, this pathway is frequently dysregulated in cancers and becomes abnormally active. This can happen due to mutations in genes within the pathway itself or due to other factors. This chronic overactivity promotes cancer hallmarks such as uncontrolled cell division, resistance to cell death, and increased blood vessel formation to nourish the tumor. As a result, the PAMT pathway is a crucial therapeutic target for cancer. Researchers are developing drugs that specifically target different components of this pathway, aiming to turn it off and slow cancer progression. Alkaloids, a class of naturally occurring nitrogen-containing molecules found in plants, have emerged as potential therapeutic agents. These alkaloids can target different points within the PAMT pathway, inhibiting its activity and potentially resulting in cancer cell death or suppression of tumor growth. Research is ongoing to explore the role of various alkaloids in cancer treatment. Berberine reduces mTOR activity and increases apoptosis by targeting the PAMT pathway, inhibiting cancer cell proliferation. Lycorine inhibits Akt phosphorylation and mTOR activation, increasing pro-apoptotic protein production and decreasing cell viability. In glioblastoma models, harmine suppresses mTORC1. This review focuses on alkaloids such as evodiamine, hirsuteine, chaetocochin J, indole-3-carbinol, noscapine, berberine, piperlongumine, and so on, which have shown promise in targeting the PAMT pathway. Clinical studies evaluating alkaloids as part of cancer treatment are underway, and their potential impact on patient outcomes is being investigated. In summary, alkaloids represent a promising avenue for targeting the dysregulated PAMT pathway in cancer, and further research is warranted.
An Overview of Antimicrobial Stewardship Optimization
(Daffodil International University, 2022-05-20) Rahman, Md. Mominur; Tumpa, Mst. Afroza Alam; Zehravi, Mehrukh; Sarker, Md. Taslim; Yamin, Md.; Islam, Md. Rezaul; Harun-Or-Rashid, Md.; Ahmed, Muniruddin; Ramproshad, Sarker; Mondal, Banani; Dey, Abhijit; Damiri, Fouad; Berrada, Mohammed; Rahman, Md. Habibur; Cavalu, Simona
Antimicrobial s are a type of agent widely used to prevent various microbial infections in humans and animals. Antimicrobial resistance is a major cause of clinical antimicrobial therapy failure, and it has become a major public health concern around the world. Increasing the development of multiple antimicrobial s has become available for humans and animals with no appropriate guidance. As a result, inappropriate use of antimicrobial s has significantly produced antimicrobial resistance. However, an increasing number of infections such as sepsis are untreatable due to this antimicrobial resistance. In either case, life-saving drugs are rendered ineffective in most cases. The actual causes of antimicrobial resistance are complex and versatile. A lack of adequate health services, um-optimized use of antimicrobial s in humans and animals, poor water and sanitation systems, wide gaps in access and research and development in healthcare technologies, and environmental pollution have vital impacts on antimicrobial resistance. This current review will highlight the natural history and basics of the development of antimicrobial s, the relationship between antimicrobial use in humans and antimicrobial use in animals, the simplistic pathways, and mechanisms of antimicrobial resistance, and how to control the spread of this resistance.
An Overview of Diabetic Foot Ulcers and Associated Problems with Special Emphasis on Treatments with Antimicrobials
(Daffodil International University, 2022-07-14) Baig, Mirza Shahed; Banu, Ahmadi; Zehravi, Mehrukh; Rana, Ritesh; Burle, Sushil S.; Khan, Sharuk L.; Islam, Fahadul; Siddiqui, Falak A.; Massoud, Ehab El Sayed; Rahman, Md. Habibur; Cavalu, Simona
One of the most significant challenges of diabetes health care is diabetic foot ulcers (DFU). DFUs are more challenging to cure, and this is particularly true for people who already have a compromised immune system. Pathogenic bacteria and fungi are becoming more resistant to antibiotics, so they may be unable to fight microbial infections at the wound site with the antibiotics we have now. This article discusses the dressings, topical antibacterial treatment, medications and debridement techniques used for DFU and provides a deep discussion of DFU and its associated problems. English-language publications on DFU were gathered from many different databases, such as Scopus, Web of Science, Science Direct, Springer Nature, and Google Scholar. For the treatment of DFU, a multidisciplinary approach involving the use of diagnostic equipment, skills, and experience is required. Preventing amputations starts with patient education and the implementation of new categorization systems. The microbiota involved in DFU can be better understood using novel diagnostic techniques, such as the 16S-ribosomal DNA sequence in bacteria. This could be achieved by using new biological and molecular treatments that have been shown to help prevent infections, to control local inflammation, and to improve the healing process.
An Overview of Polymer Surface Coated Synthetic Quantum Dots As Therapeutics and Sensors Applications
(Elsevier, 2023-11-15) Babu, Ancha Kishore; Raja, M. K. Mohan Maruga; Zehravi, Mehrukh; Mohammad, Badrud Duza; Anees, Mohammed Imran; Prasad, Cheepurupalli; Yahya, Barrawaz Aateka; Sultana, Rokeya; Sharma, Rohit; Singh, Jay; Khan, Khalid Ali; Siddiqui, Falak A.; Khan, Sharuk L.; Emran, Talha Bin
Quantum dots (QDs) are a class of remarkable materials that have garnered significant attention since their initial discovery. It is noteworthy to mention that it took approximately a decade for these materials to be successfully implemented in practical applications. While QDs have demonstrated notable optical properties, it is important to note that these attributes alone have not rendered them a feasible substitute for traditional organic dyes. Furthermore, it is worth noting that the substance under investigation exhibited inherent toxicity and instability in its initial state, primarily due to the presence of a heavy metal core. In the initial stages of research, it was observed that the integration of nanocomposites had a positive impact on the properties of QDs. The discovery of these nanocomposites was motivated by the remarkable properties exhibited by biocomposites found in nature. Recent discoveries have shed light on the potential utilization of QDs as a viable strategy for drug delivery, offering a promising avenue to enhance the efficacy of current pharmaceuticals and pave the way for the creation of innovative therapeutic approaches. The primary objective of this review was to elucidate the distinctive characteristics that render QDs highly suitable for utilization as nanocarriers. In this study, we will delve into the multifaceted applications of QDs as sensing nanoprobes and their utilization in diverse drug delivery systems. The focus of our investigation was directed toward the utilization of QD/polymer composites in sensing applications, with particular emphasis on their potential as chemical sensors, biosensors, and physical sensors.
Exploring the Role of Natural Bioactive Molecules in Genitourinary Cancers
(Springer, 2023-10-16) Islam, Fahadul; Nath, Nikhil; Zehravi, Mehrukh; Khan, Jishan; Jashim, Sumiya Ben‑Ta; Charde, Manoj Shrawan; Chakole, Rita Dadarao; Kumar, Praveen; Babu, A. Kishore; Nainu, Firzan; Khan, Sharuk L.; Rab, Safia Obaidur; Emran, Talha Bin; Wilairatana, Polrat
The primary approaches to treat cancerous diseases include drug treatment, surgical procedures, biotherapy, and radiation therapy. Chemotherapy has been the primary treatment for cancer for a long time, but its main drawback is that it kills cancerous cells along with healthy ones, leading to deadly adverse health effects. However, genitourinary cancer has become a concern in recent years as it is more common in middle-aged people. So, researchers are trying to find possible therapeutic options from natural small molecules due to the many drawbacks associated with chemotherapy and other radiation-based therapies. Plenty of research was conducted regarding genitourinary cancer to determine the promising role of natural small molecules. So, this review focused on natural small molecules along with their potential therapeutic targets in the case of genitourinary cancers such as prostate cancer, renal cancer, bladder cancer, testicular cancer, and so on. Also, this review states some ongoing or completed clinical evidence in this regard.
Flavonoids as Potential Therapeutics Against Neurodegenerative Disorders
(Springer Nature, 2024-08-15) Faysal, Md.; Dehbia, Zerrouki; Zehravi, Mehrukh; Sweilam, Sherouk Hussein; Haque, M. Akiful; Kumar, Kusuma Praveen; Chakole, Rita D.; Shelke, Satish P.; Sirikonda, Swapna; Nafady, Mohamed H.; Khan, Sharuk L.; Nainu, Firzan; Ahmad, Irfan; Emran, Talha Bin
Neurodegeneration, the decline of nerve cells in the brain, is a common feature of neurodegenerative disorders (NDDs). Oxidative stress, a key factor in NDDs such as Alzheimer’s disease, Parkinson’s disease, amyotrophic lateral sclerosis, and Huntington’s disease can lead to neuronal cell death, mitochondria impairment, excitotoxicity, and Ca2+ stress. Environmental factors compromising stress response lead to cell damage, necessitating novel therapeutics for preventing or treating brain disorders in older individuals and an aging population. Synthetic medications offer symptomatic benefits but can have adverse effects. This research explores the potential of flavonoids derived from plants in treating NDDs. Flavonoids compounds, have been studied for their potential to enter the brain and treat NDDs. These compounds have diverse biological effects and are currently being explored for their potential in the treatment of central nervous system disorders. Flavonoids have various beneficial effects, including antiviral, anti-allergic, antiplatelet, anti-inflammatory, anti-tumor, anti-apoptotic, and antioxidant properties. Their potential to alleviate symptoms of NDDs is significant.
Flavonoids as Potential Therapeutics Against Neurodegenerative Disorders: Unlocking the Prospects
(2024-06-01) Faysal, Md.; Dehbia, Zerrouki; Zehravi, Mehrukh; Sweilam, Sherouk Hussein; Akiful Haque, M.; Kumar, Kusuma Praveen; D. Chakole, Rita; P. Shelke, Satish; Sirikonda, Swapna; H. Nafady, Mohamed; L. Khan, Sharuk; Nainu, Firzan; Ahmad, Irfan; Bin Emran, Talha
Neurodegeneration, the decline of nerve cells in the brain, is a common feature of neurodegenerative disorders (NDDs). Oxidative stress, a key factor in NDDs such as Alzheimer’s disease, Parkinson’s disease, amyotrophic lateral sclerosis, and Huntington’s disease can lead to neuronal cell death, mitochondria impairment, excitotoxicity, and Ca2+ stress. Environmental factors compromising stress response lead to cell damage, necessitating novel therapeutics for preventing or treating brain disorders in older individuals and an aging population. Synthetic medications offer symptomatic benefits but can have adverse effects. This research explores the potential of flavonoids derived from plants in treating NDDs. Flavonoids compounds, have been studied for their potential to enter the brain and treat NDDs. These compounds have diverse biological effects and are currently being explored for their potential in the treatment of central nervous system disorders. Flavonoids have various beneficial effects, including antiviral, anti-allergic, antiplatelet, anti-inflammatory, anti-tumor, anti-apoptotic, and antioxidant properties. Their potential to alleviate symptoms of NDDs is significant.
Genus Amorphophallus: A Comprehensive Overview on Phytochemistry, Ethnomedicinal Uses, and Pharmacological Activities
(MDPI Publications, 2023-11-23) Islam, Fahadul; Labib, Rafiuddin Khan; Zehravi, Mehrukh; Lami, Mashia Subha; Das, Rajib; Singh, Laliteshwar Pratap; Mandhadi, Jithendar Reddy; Balan, P.; Khan, Jishan; Khan, Sharuk L.; Nainu, Firzan; Nafady, Mohamed H.; Rab, Safia Obaidur; Emran, Talha Bin; Wilairatana, Polrat
The genus Amorphophallus belongs to the family Araceae. Plants belonging to this genus are available worldwide and have been used in traditional medicines since ancient times, mainly in Ayurveda and Unani medical practices. Amorphophallus species are an abundant source of polyphenolic compounds; these are accountable for their pharmacological properties, such as their analgesic, neuroprotective, hepatoprotective, anti-inflammatory, anticonvulsant, antibacterial, antioxidant, anticancer, antiobesity, and immunomodulatory effects, as well as their ability to prevent gastrointestinal disturbance and reduce blood glucose. Moreover, Amorphophallus species contain numerous other classes of chemical compounds, such as alkaloids, steroids, fats and fixed oils, tannins, proteins, and carbohydrates, each of which contributes to the pharmacological effects for the treatment of acute rheumatism, tumors, lung swelling, asthma, vomiting, abdominal pain, and so on. Additionally, Amorphophallus species have been employed in numerous herbal formulations and pharmaceutical applications. There has been no extensive review conducted on the Amorphophallus genus as of yet, despite the fact that several experimental studies are being published regularly discussing these plants' pharmacological properties. So, this review discusses in detail the pharmacological properties of Amorphophallus species. We also discuss phytochemical constituents in the Amorphophallus species and their ethnomedicinal uses and toxicological profiles.
Indole Alkaloids From Marine Resources: Understandings From Therapeutic Point of View To Treat Cancers
(Chemico-Biological Interactions, 2023-08-28) Islam, Fahadul; Dehbia, Zerrouki; Zehravi, Mehrukh; Das, Rajib; Sivakumar, M.; Krishnan, Karthickeyan; Billah, Abdul Ajeed Mohathasim; Bose, Bharadhan; Ghosh, Avoy; Paul, Shyamjit; Nainu, Firzan; Ahmad, Irfan; Emran, Talha Bin
Cancer is the leading cause of mortality all over the world. Scientific investigation has demonstrated that disruptions in the process of autophagy are frequently interrelated with the emergence of cancer. Hence, scientists are seeking permanent solutions to counter the deadly disease. Indole alkaloids have been extensively studied and are acknowledged to exhibit several bioactivities. The current state of disease necessitates novel pharmacophores development. In recent decades, indole alkaloids have become increasingly significant in cancer treatment and are also used as adjuvants. A substantial amount of pharmacologically active molecules come from indole alkaloids, which are widely distributed in nature. Indole alkaloids derived from marine organisms show immense potential for therapeutic applications and seem highly effective in cancer treatment. A couple of experiments have been conducted preclinically to investigate the possibility of indole alkaloids in cancer treatment. Marine-derived indole alkaloids possess the ability to exhibit anticancer properties through diverse antiproliferative mechanisms. Certain indole alkaloids, including vincristine and vinblastine, were verified in clinical trials or are presently undergoing clinical assessments for preventing and treating cancer. Indole alkaloids from marine resources hold a significant functionality in identifying new antitumor agents. The current literature highlights recent advancements in indole alkaloids that appear to be anticancer agents and the underlying mechanisms. © 2023 Elsevier B.V.
Natural Polymers As Potential P-Glycoprotein Inhibitors: Pre-ADMET Profile and Computational Analysis as a Proof of Concept To Fight Multidrug Resistance in Cancer
(Elsevier, 2023-08-24) Gandla, Kumaraswamy; Islam, Fahadul; Zehravi, Mehrukh; Karunakaran, Anandakumar; Sharma, Indu; Haque, Akiful; Kumar, Sanjay; Pratyush, Kumar; Dhawale, Sachin A.; Nainu, Firzan; Khan, Sharuk L.; Islam, Md. Rezaul; Al-Mugren, Kholoud Saad; Siddiqui, Falak A.; Emran, Talha Bin; Khandaker, Mayeen Uddin
P-glycoprotein (P-gp) is known as the "multidrug resistance protein" because it contributes to tumor resistance to several different classes of anticancer drugs. The effectiveness of such polymers in treating cancer and delivering drugs has been shown in a wide range of in vitro and in vivo experiments. The primary objective of the present study was to investigate the inhibitory effects of several naturally occurring polymers on P-gp efflux, as it is known that P-gp inhibition can impede the elimination of medications. The objective of our study is to identify polymers that possess the potential to inhibit P-gp, a protein involved in drug resistance, with the aim of enhancing the effectiveness of anticancer drug formulations. The ADMET profile of all the selected polymers (Agarose, Alginate, Carrageenan, Cyclodextrin, Dextran, Hyaluronic acid, and Polysialic acid) has been studied, and binding affinities were investigated through a computational approach using the recently released crystal structure of P-gp with PDB ID: 7O9W. The advanced computational study was also done with the help of molecular dynamics simulation. The aim of the present study is to overcome MDR resulting from the activity of P-gp by using such polymers that can inhibit P-gp when used in formulations. The docking scores of native ligand, Agarose, Alginate, Carrageenan, Chitosan, Cyclodextrin, Dextran, Hyaluronic acid, and Polysialic acid were found to be −10.7, −8.5, −6.6, −8.7, −8.6, −24.5, −6.7, −8.3, and −7.9, respectively. It was observed that, Cyclodextrin possess multiple properties in drug delivery science and here also demonstrated excellent binding affinity. We propose that drug efflux-related MDR may be prevented by the use of Agarose, Carregeenan, Chitosan, Cyclodextrin, Hyaluronic acid, and/or Polysialic acid in the administration of anticancer drugs.
Neuropharmacological Potential of Honokiol and Its Derivatives From Chinese Herb Magnolia Species: Understandings From Therapeutic Viewpoint
(PubMed Central Press, 2023-11-24) Faysal, Md.; Khan, Jishan; Zehravi, Mehrukh; Nath, Nikhil; Singh, Laliteshwar Pratap; Kakkar, Saloni; Perusomula, Rajashekar; Khan, Pathan Amanulla; Nainu, Firzan; Asiri, Mohammed; Khan, Sharuk L.; Das, Rajib; Emran, Talha Bin; Wilairatana, Polrat
Honokiol is a neolignan biphenol found in aerial parts of the Magnolia plant species. The Magnolia plant species traditionally belong to China and have been used for centuries to treat many pathological conditions. Honokiol mitigates the severity of several pathological conditions and has the potential to work as an anti-inflammatory, anti-angiogenic, anticancer, antioxidant, and neurotherapeutic agent. It has a long history of being employed in the healthcare practices of Southeast Asia, but in recent years, a greater scope of research has been conducted on it. Plenty of experimental evidence suggests it could be beneficial as a neuroprotective bioactive molecule. Honokiol has several pharmacological effects, leading to its exploration as a potential therapy for neurological diseases (NDs), including Alzheimer's disease (AD), Parkinson's disease (PD), cerebral ischemia, anxiety, depression, spinal cord injury, and so on. So, based on the previous experimentation reports, our goal is to discuss the neuroprotective properties of honokiol. Besides, honokiol derivatives have been highlighted recently as possible therapeutic options for NDs. So, this review focuses on honokiol's neurotherapeutic actions and toxicological profile to determine their safety and potential use in neurotherapeutics.
Pharmacogenomics of Immunosuppressants
(Elsevier, 2023-01-15) Islam, Fahadul; Islam, Md. Rezaul; Nafady, Mohamed H.; Faysal, Md.; Khan, Sharuk L.; Zehravi, Mehrukh; Emran, Talha Bin; Rahman, Md. Habibur
In recent years, pharmacogenetics has become a powerful technique for selecting the appropriate immunosuppressant medicine and dose. Pharmacogenetics can have three different effects on immunosuppressive medication. The study of the genes that code for the drug pharmacokinetic proteins and drug breakdown enzymes is known as pharmacogenetics. The study of genetic variants that code for proteins that act as pharmacodynamic immunosuppressant trigger pathways is known as pharmacogenetics. Immunosuppressants, such as calcineurin inhibitors (e.g., cyclosporine A and tacrolimus) and antimetabolic medicines, must be used wisely for patients to survive long-term after solid organ transplantation (e.g., mycophenolic acid). Therapeutic drug monitoring and personalized therapy require the limited therapeutic index of many drugs and vital interindividual and individual variability in pharmacokinetics (PK) and pharmacodynamics (PD). Genetic polymorphisms along with immunosuppressant PD have received more attention in recent years. Monitoring these pharmacogenetic indicators gives us an excellent tool for developing personalized immunosuppressant dose regimens. The findings of the studies on the prospective genes mentioned above and the improvement of omics methodologies may one day permit us to choose the suitable immunosuppressant for the particular client at the appropriate dose.
Polyphenols as Therapeutics in Respiratory Diseases: Moving from Preclinical Evidence to Potential Clinical Applications
(2024-06-03) Bin Emran, Talha; Eva, Taslima Akter; Zehravi, Mehrukh; Islam, Fahadul; Khan, Jishan; Kareemulla, Shaik; Venkata Arjun, Uppuluri Varuna Naga; Balakrishnan, Anitha; Taru, Poonam Popatrao; Nainu, Firzan; Salim, Emil; Rab, Safia Obaidur; H Nafady, Mohamed; Wilairatana, Polrat; Park, Moon Nyeo; Kim, Bonglee
Respiratory diseases are the most common and severe health complication and a leading cause of death worldwide. Despite breakthroughs in diagnosis and treatment, few safe and effective therapeutics have been reported. Phytochemicals are gaining popularity due to their beneficial effects and low toxicity. Polyphenols are secondary metabolites with high molecular weights found at high levels in natural food sources such as fruits, vegetables, grains, and citrus seeds. Over recent decades, polyphenols and their beneficial effects on human health have been the subject of intense research, with notable successes in preventing major chronic non-communicable diseases. Many respiratory syndromes can be treated effectively with polyphenolic supplements, including acute lung damage, pulmonary fibrosis, asthma, pulmonary hypertension, and lung cancer. This review summarizes the role of polyphenols in respiratory conditions with sufficient experimental data, highlights polyphenols with beneficial effects for each, and identifies those with therapeutic potential and their underlying mechanisms. Moreover, clinical studies and future research opportunities in this area are discussed.
Polyphenols in Wound Healing: Unlocking Prospects with Clinical Applications
(Springer Nature, 2024-10-15) Utpal, Biswajit Kumar; Sutradhar, Baishakhi; Zehravi, Mehrukh; Sweilam, Sherouk Hussein; Panigrahy, Uttam Prasad; Urs, Deepadarshan; Fatima, Ayesha Farhath; Nallasivan, Kumar; Chhabra, Gurmeet Singh; Sayeed, Mohammed; Alshehri, Mohammed Ali; Rab, Safia Obaidur; Khan, Sharuk L.; Emran, Talha Bin
Wound healing is a multifaceted, complex process that factors like aging, metabolic diseases, and infections may influence. The potentiality of polyphenols, natural compounds, has shown anti-inflammatory and antimicrobial properties in promoting wound healing and their potential applications in wound management. The studies reviewed indicate that polyphenols have multiple mechanisms that promote wound healing. This involves enhancing antioxidant defenses, reducing oxidative stress, modulating inflammatory responses, improving healing times, reducing infection rates, and enhancing tissue regeneration in clinical trials and in vivo and in vitro studies. Polyphenols have been proven to be effective in managing hard-to-heal wounds, especially in diabetic and elderly populations. Polyphenols have shown significant benefits in promoting angiogenesis and stimulating collagen synthesis. Polyphenol treatment has been demonstrated to have therapeutic effects in wound healing and chronic wound management. Their ability to regulate key healing processes makes them suitable for new wound care products and treatments. Future research should enhance formulations and delivery methods to optimize polyphenols' bioavailability and therapeutic efficacy in wound management approaches.
Polyphenols Targeting MAP Kinase Signaling Pathway in Neurological Diseases: Understanding Molecular Mechanisms and Therapeutic Targets
(2024-05-24) Islam, Fahadul; Roy, Sumon; Zehravi, Mehrukh; Paul, Shyamjit; Sutradhar, Hriday; Yaidikar, Lavanya; Kumar, B Raj; Dogiparthi, Lakshman Kumar; Prema, S; Nainu, Firzan; Bin Emran, Talha; Rab, Safia Obaidur; Doukani, Koula
Polyphenols are a class of secondary metabolic products found in plants that have been extensively studied for how well they regulate biological processes, such as the proliferation of cells, autophagy, and apoptosis. The mitogen-activated protein kinase (MAPK)-mediated signaling cascade is currently identified as a crucial pro-inflammatory pathway that plays a significant role in the development of neuroinflammation. This process has been shown to contribute to the pathogenesis of several neurological conditions, such as Alzheimer's disease (AD), Parkinson's disease (PD), CNS damage, and cerebral ischemia. Getting enough polyphenols through eating habits has resulted in mitigating the effects of oxidative stress (OS) and lowering the susceptibility to associated neurodegenerative disorders, including but not limited to multiple sclerosis (MS), AD, stroke, and PD. Polyphenols possess significant promise in dealing with the root cause of neurological conditions by modulating multiple therapeutic targets simultaneously, thereby attenuating their complicated physiology. Several polyphenolic substances have demonstrated beneficial results in various studies and are presently undergoing clinical investigation to treat neurological diseases (NDs). The objective of this review is to provide a comprehensive summary of the different aspects of the MAPK pathway involved in neurological conditions, along with an appraisal of the progress made in using polyphenols to regulate the MAPK signaling system to facilitate the management of NDs.
Polyphenols Targeting MAP Kinase Signaling Pathway in Neurological Diseases: Understanding Molecular Mechanisms and Therapeutic Targets
(Springer, 2023-11-03) Islam, Fahadul; Roy, Sumon; Zehravi, Mehrukh; Paul, Shyamjit; Sutradhar, Hriday; Yaidikar, Lavanya; Kumar, B Raj; Dogiparthi, Lakshman Kumar; Prema, S.; Nainu, Firzan; Rab, Safia Obaidur; Doukani, Koula; Emran, Talha Bin
Polyphenols are a class of secondary metabolic products found in plants that have been extensively studied for how well they regulate biological processes, such as the proliferation of cells, autophagy, and apoptosis. The mitogen-activated protein kinase (MAPK)-mediated signaling cascade is currently identified as a crucial pro-inflammatory pathway that plays a significant role in the development of neuroinflammation. This process has been shown to contribute to the pathogenesis of several neurological conditions, such as Alzheimer's disease (AD), Parkinson's disease (PD), CNS damage, and cerebral ischemia. Getting enough polyphenols through eating habits has resulted in mitigating the effects of oxidative stress (OS) and lowering the susceptibility to associated neurodegenerative disorders, including but not limited to multiple sclerosis (MS), AD, stroke, and PD. Polyphenols possess significant promise in dealing with the root cause of neurological conditions by modulating multiple therapeutic targets simultaneously, thereby attenuating their complicated physiology. Several polyphenolic substances have demonstrated beneficial results in various studies and are presently undergoing clinical investigation to treat neurological diseases (NDs). The objective of this review is to provide a comprehensive summary of the different aspects of the MAPK pathway involved in neurological conditions, along with an appraisal of the progress made in using polyphenols to regulate the MAPK signaling system to facilitate the management of NDs.
Potential Inhibitors from Natural Compounds against SARS-CoV-2 Main Protease: A Systematic Molecular Modelling Approach
(2024-02-12) Raman, Kannan; Kalirajan, Rajagopal; Islam, Fahadul; Zehravi, Mehrukh; Singh, Laliteshwar Pratap; Rana, Ritesh; Murugesan, Sankaranarayanan; Jupudi, Srikanth; Akash, Shopnil; Byran, Gowramma; Nainu, Firzan; Bin Emran, Talha; Dawoud, Turki M.; Bourhia, Mohammed; Barua, Rashu
The COVID-19 outbreak poses a significant threat to the world‘s human population in 2020. Finding new drugs rapidly during this pandemic is quite challenging. Thus, in silico drug screening experiments may provide effective therapeutic alternatives for better assessing natural remedies in preventing and treating COVID-19. The main protease (Mpro) is an important drug target that is essential and ubiquitous for the survival of SARS-CoV-2. In this study, we performed in silico high-throughput virtual screening to identify potential hits employing a database of 3 million natural compounds (supernatural-II database). The initially obtained top 100 virtual hits were subjected to a standard SP and XP docking protocol, achieving the top 30 hits. Compounds SN00340755 (glide score: −16.0 kcal/mol and ΔGbind: −134.29 kcal/mol) and SN00213037 (glide score: −13.30 kcal/mol and ΔGbind: −81.18 kcal/mol) exhibited significant binding energy against Mpro (PDB ID: 6XQS). The ligands SN00340755 and SN00213037 formed multiple hydrogen bonds with the catalytic residues, especially with the functionally important residue GLU166, which plays a significant role in protomer dimerization. Further post-docking minimization studies (MM-GBSA) were performed to estimate the ligand-protein affinity. From MM-GBSA studies, it was observed that Coulombic (−140.70 to −37.66 kcal/mol) and van der Waals (−79.32 to −20.59 kcal/mol) energies, favoring the binding of ligands to the Mpro target protein. The ADMET properties were predicted using Qikprop, Chem Axon, and Data Warrior tools, demonstrating the beneficial pharmacokinetic parameters of these natural compounds. The 100 ns molecular dynamics simulation study revealed minor protein fluctuations, indicating the stability of the protein-ligand complex.