Browsing by Author "Nainu, Firzan"

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A Renewed Concept on Diabetic Retinopathy: Polyphenols as a Choice of Solution
(Biointerface research, 2021-04-07) Emran, Talha Bin; Haque, M. Akiful; Guntaka, Purnachandra Reddy; Singh, Laliteshwar Pratap; Khan, Mohd. Washid; Unnisa, Aziz; Nafady, Mohammed H.; Kazi, Aasim A.; Doukani, Koula; Nainu, Firzan
Diabetic retinopathy (DR) is the widespread microvascular consequence of diabetes mellitus and the most common effect of blindness in people with diabetes. Existing drugs are only effective in advanced stages of DR, and long-term efficacy and safety results for these treatments have yet to be clarified in multiple clinical trials. Furthermore, a more trustworthy and effective medication that may be deemed more advantageous in managing DR is unavoidable. Polyphenols, which are plant-derived chemical compounds, may be helpful in the initial stages of DR treatment. Compounds rich in polyphenols have been shown to slow the progression of long-term consequences of diabetes, for example, heart disease, nerve damage, kidney damage, and retinopathy. Polyphenols could be used instead of traditional treatments to halt the disease's progression. It has been proposed that in vitro investigations on the effects of polyphenols on ocular vision physiology and antioxidant protection have a substantial bearing on this assertion. Among the benefits of polyphenols are scavenging the free radicals, lowering the production of advanced glycation end products, inhibiting aldose reductase, anti- inflammatory activity, and affecting ocular blood flow. The present review discussed the significance of polyphenols in preclinical and clinical research of DR-affected cellular and molecular pathways.
Anti-Inflammatory Activities of Flavonoid Derivates
(International Association of Physical Chemists, 2023-07-26) Ysrafil, Ysrafil; Sapiun, Zulfiayu; Slamet, Nangsih Sulastri; Mohamad, Fihrina; Hartati, Hartati; Damiti, Sukmawati A; Alexandra, Francisca Diana; Rahman, Sudarman; Masyeni, Sri; Harapan, Harapan; Mamada, Sukamto S.; Emran, Talha Bin; Nainu, Firzan
Background and purpose Flavonoids are a group of phytochemicals found abundantly in various plants. Scientific evidence has revealed that flavonoids display potential biological activities, including their ability to alleviate inflammation. This activity is closely related to their action in blocking the inflammatory cascade and inhibiting the production of pro-inflammatory factors. However, as flavonoids typically have poor bioavailability and pharmacokinetic profile, it is quite challenging to establish these compounds as a drug. Nevertheless, progressive advancements in drug delivery systems, particularly in nanotechnology, have shown promising approaches to overcome such challenges. Review approach This narrative review provides an overview of scientific knowledge about the mechanism of action of flavonoids in the mitigation of inflammatory reaction prior to delivering a comprehensive discussion about the opportunity of the nanotechnology-based delivery system in the preparation of the flavonoid-based drug. Key results Various studies conducted in silico, in vitro, in vivo, and clinical trials have deciphered that the anti-inflammatory activities of flavonoids are closely linked to their ability to modulate various biochemical mediators, enzymes, and signalling pathways involved in the inflammatory processes. This compound could be encapsulated in nanotechnology platforms to increase the solubility, bioavailability, and pharmacological activity of flavonoids as well as reduce the toxic effects of these compounds. Conclusion In Summary, we conclude that flavonoids and their derivates have given promising results in their development as new anti-inflammatory drug candidates, especially if they formulate in nanoparticles.Z
Cruciferous Vegetables as a Treasure of Functional Foods Bioactive Compounds
(Daffodil International University, 2022-08-09) Mitra, Saikat; Emran, Talha Bin; Chandran, Deepak; Zidan, B M Redwan Matin; Das, Rajib; Mamada, Sukamto S.; Masyita, Ayu; Salampe, Mirnawati; Nainu, Firzan; Khandaker, Mayeen Uddin; Idris, Abubakr M; Simal-Gandara, Jesus
In the past few years, phytochemicals from natural products have gotten the boundless praise in treating cancer. The promising role of cruciferous vegetables and active components contained in these vegetables, such as isothiocyanates, indole-3-carbinol, and isothiocyanates, has been widely researched in experimental in vitro and in vivo carcinogenesis models. The chemo preventive agents produced from the cruciferous vegetables were recurrently proven to affect carcinogenesis throughout the onset and developmental phases of cancer formation. Likewise, findings from clinical investigations and epidemiological research supported this statement. The anticancer activities of these functional foods bioactive compounds are closely related to their ability to upregulate p53 and its related target genes, e.g., p21. As the "guardian of the genome," the p53 family (p53, p63, and p73) plays a pivotal role in preventing the cancer progression associated with DNA damage. This review discusses the functional foods bioactive compounds derived from several cruciferous vegetables and their use in altering the tumor-suppressive effect of p53 proteins. The association between the mutation of p53 and the incidence of gastrointestinal malignancies (gastric, small intestine, colon, liver, and pancreatic cancers) is also discussed. This review contains crucial information about the use of cruciferous vegetables in the treatment of gastrointestinal tract malignancies.
Diallyl Disulfide
(Daffodil International University, 2022-08-12) Mitra, Saikat; Das, Rajib; Emran, Talha Bin; Labib, Rafiuddin Khan; -E-Tabassum, Noor; Islam, Fahadul; Sharma, Rohit; Ahmad, Islamudin; Nainu, Firzan; Chidambaram, Kumarappan; Alhumaydhi, Fahad A.; Chandran, Deepak; Capasso, Raffaele; Wilairatana, Polrat
Cancer is a life-threatening disease caused by the uncontrolled division of cells, which culminates in a solid mass of cells known as a tumor or liquid cancer. It is the leading cause of mortality worldwide, and the number of cancer patients has been increasing at an alarming rate, with an estimated 20 million cases expected by 2030. Thus, the use of complementary or alternative therapeutic techniques that can help prevent cancer has been the subject of increased attention. Garlic, the most widely used plant medicinal product, exhibits a wide spectrum of biological activities, including antibacterial, hypo-lipidemic, antithrombotic, and anticancer effects. Diallyl disulfide (DADS) is a major organosulfur compound contained within garlic. Recently, several experimental studies have demonstrated that DADS exhibits anti-tumor activity against many types of tumor cells, including gynecological cancers (cervical cancer, ovarian cancer), hematological cancers (leukemia, lymphoma), lung cancer, neural cancer, skin cancer, prostate cancer, gastrointestinal tract and associated cancers (esophageal cancer, gastric cancer, colorectal cancer), hepatocellular cancer cell line, etc. The mechanisms behind the anticancer action of DADS include epithelial-mesenchymal transition (EMT), invasion, and migration. This article aims to review the available information regarding the anti-cancer potential of DADS, as well as summarize its mechanisms of action, bioavailability, and pharmacokinetics from published clinical and toxicity studies.
Drosophila melanogaster as a Versatile Model for Studying Medically Important Insect Vector-Borne Parasites
(Daffodil International University, 2022-06-02) Nainu, Firzan; Salim, Emil; Emran, Talha Bin; Sharma, Rohit
In the past decades, insect vector-borne parasitic diseases (VBDs), such as malaria, leishmaniasis, and lymphatic filariasis, have caused a devastating health problem, threatening for over 250 million lives worldwide (Wilson et al., 2020). While the causative parasites of VBDs together with their native insect vectors have been largely documented, much remains unknown. Global efforts are still needed to fully elucidate the parasites’ genes that are playing parts in the infectivity and mechanisms responsible in the modulation of host antiparasitic immune responses. In addition, characterization of important VBDs hallmarks and factors responsible in the vector and host susceptibility to parasitic transmission and infection remains underexplored. Once revealed, such information shall provide a vital role in the improvement of preventive actions to control the spread of VBDs and pharmacotherapeutic strategies to limit the disease burden. Several insects such as mosquitoes, flies (sand flies, black flies, and tsetse flies), and triatomine bugs, have all been implicated in the transmission of parasites to human (Wilson et al., 2020). While much has been done in the identification of insect(s) suitable for the parasites’ life cycle prior to infection in the human, it remains challenging to carry out experimental investigations in the native insect vectors (Schneider, 2000; Zolfaghari Emameh et al., 2015). Complexities in the vector rearing and the lack of genetic toolbox available for carrying out experimental procedures in the native vectors are two of the most encountered obstacles for anyone working in this field (Schneider, 2000; Zolfaghari Emameh et al., 2015). To address this issue, the use of insect model such as fruit fly Drosophila melanogaster to study the parasitic biology and other important knowledge related to the transmission and vector-parasite interaction can be seen as one of the alternative endeavors. In this opinion paper, we would like to propose the use of D. melanogaster to study the biology, immunology, and pathogenic characteristics of human parasites, and to some extent other vertebrate parasites, to reflect the situation occurred either during parasites’ lifecycle in the vector or during their infectious phase in their definitive vertebrate host. However, it is important to note that the results obtained from the Drosophila works shall be interpreted with caution once the results are translated into either the parasites’ native vectors or their vertebrate host.
Emergence of SARS-CoV-2 Omicron (B.1.1.529) Variant, Salient Features, High Global Health Concerns and Strategies To Counter It Amid Ongoing COVID-19 Pandemic
(Daffodil International University, 2022-01-21) Khandia, Rekha; Singhal, Shailja; Alqahtani, Taha; Kamal, Mohammad Amjad; El-Shall, Nahed A.; Nainu, Firzan; Desingu, Perumal Arumugam; Dhama, Kuldeep
Since the appearance in the late of December 2019, SARS-CoV-2 is rapidly evolving and mutating continuously, giving rise to various variants with variable degrees of infectivity and lethality. The virus that initially appeared in China later mutated several times, wreaking havoc and claiming many lives worldwide amid the ongoing COVID-19 pandemic. After Alpha, Beta, Gamma, and Delta variants, the most recently emerged variant of concern (VOC) is the Omicron (B.1.1.529) that has evolved due to the accumulation of high numbers of mutations especially in the spike protein, raising concerns for its ability to evade from pre-existing immunity acquired through vaccination or natural infection as well as overpowering antibodies-based therapies. Several theories are on the surface to explain how the Omicron has gathered such a high number of mutations within less time. Few of them are higher mutation rates within a subgroup of population and then its introduction to a larger population, long term persistence and evolution of the virus in immune-compromised patients, and epizootic infection in animals from humans, where under different immune pressures the virus mutated and then got reintroduced to humans. Multifaceted approach including rapid diagnosis, genome analysis of emerging variants, ramping up of vaccination drives and receiving booster doses, efficacy testing of vaccines and immunotherapies against newly emerged variants, updating the available vaccines, designing of multivalent vaccines able to generate hybrid immunity, up-gradation of medical facilities and strict implementation of adequate prevention and control measures need to be given high priority to handle the on-going SARS-CoV-2 pandemic successfully.
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.
Immunomodulatory Effect of Begonia Medicinalis Ethanolic Extract in Drosophila
(Biointerface research, 2023-02-24) Syamsidi, Armini; Rosa, Reski Amalia; Sulastri, Evi; Rahmah, Nur; Kamri, Reski Amelia; Rumata, Nur Rahma; Emran, Talha Bin; Sharma, Rohit; Rabaan, Ali A.; Nainu, Firzan; Zubair, Muhammad Sulaiman
Begonia medicinalis is an Indonesian endemic plant that has been reported to exert multiple pharmacological effects, including antiviral and anticancer activities. These activities have been suggested to be related to the immunomodulatory properties of dried B. medicinalis ethanolic extract (DBME). However, this notion remains unclear. This study was carried out aiming to investigate the immunomodulatory effect of DBME in Drosophila melanogaster model based on the expression of genes in the Toll, Imd, and JAK-STAT pathways. Phenotypical analysis on the survival and locomotor of D. melanogaster was carried out to reveal whether changes in the gene expressions were observable at the phenotypical level. Four groups of D. melanogaster were prepared and treated with DBME (0%, 0.25%, 0.5%, and 2%). The results demonstrated that DBME could modulate the expression of Drs (Toll pathway), Dpt (Imd pathway), and TotA (JAK-STAT pathway) in D. melanogaster. These molecular changes were accompanied by almost no changes in survival and locomotor activities. In brief, DBME can induce the humoral immune responses of D. melanogaster without significant phenotypical trade-offs.
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.
Investigating Potential Therapeutics for Bacterial and Cancerous Diseases: Silver Nanoparticles as a Choice
(2024-02-24) Nafady, Mohamed; Bin Emran, Talha; Pratap Singh, Laliteshwar; Suchitra, D; Akiful Haque, M; Joshi, Neha; B Parmar, Akil; Al Amin, Md; Shahriar, S. M. Shatil; Nainu, Firzan
Silver nanoparticles (AgNPs) have been identified as an efficient antibacterial representative capable of combating bacteria that cause infections. AgNPs have antibacterial properties against Gram-negative and Gram-positive bacteria and multidrug-resistant pathogens. AgNPs have various contemporary modes of action, and when used in conjunction with antibacterial agents such as chemical combinations or antibiotics, they have a synergic activity on bacteria pathogens. AgNPs have been extensively researched as components of sophisticated anti-cancer medications for improving cancer management in the clinic. The reduction of substances on silver ions often produces AgNPs. Living organisms and natural products, moreover, exceptional cascade for synthesizing AgNPs harbingers. AgNPs have properties that make them excellent for use in medical and healthcare goods, where they can effectively reduce the risk of developing infections. This review discusses the antibacterial and anti-cancer properties of AgNPs, and the benefits of using AgNPs as a novel, effective antibacterial combination with antibiotics, which will lessen the dosage required and avoid potential hazards.
Investigation of Scutellaria baicalensis for Potential Neuroprotective Effect on the Treatment of Parkinson's Disease
(2024-02-03) Zubair Baba, Mohammad; Subramanian, Gomathy; Chand, Jagdish; Nainu, Firzan; Wahedi, Umair; Potlapati, Varakumar; Jayanthi, Koppula; Azeemuddin, Mohammed; Bin Emran, Talha
Parkinson's disease (PD) is a progressive neurological disorder that lacks adequate treatment, and researchers have focused on rescuing or delaying neurodegeneration in PD. Scutellaria baicalensis has shown promising results in reducing oxidative stress and demonstrating a neuroprotective effect on PD animal models. However, the exact mechanism by which S. baicalensis treats PD is not yet fully understood. To investigate the potential molecular mechanisms underlying S. baicalensis antiparkinsonian efficacy, this study used network pharmacology. Open-source datasets were used to compile phytoconstituents, and virtual screening was conducted to identify hit phytoconstituents that target proteins involved in PD development. The drug-likeness value, ADMET analyses, and negative consequences of the phytochemical constituent were evaluated. Regulating pathways were anticipated with the Kyoto Encyclopedia of Genes (KEGG) record. 7 phytochemical constituents from S. baicalensis were found to alter the activity of proteins involved in PD occurrence, with 5-hydroxy-7,8- dimethoxyflavones having the highest docking result of -8.337 kcal/mol and active amino acids SER 91, as well as the drug-likeness value at the highest edge points. Through the networking of phytoconstituents, genes, and pathways, the study revealed that the neuroactive ligand-receptor interaction route was tightly synchronized.
Marine Macrolides To Tackle Antimicrobial Resistance of Mycobacterium tuberculosis
(Scopus, 22-11-01) S., Sukamto; Mamada, Sukamto S.; Nainu, Firzan; Masyita, Ayu; Frediansyah, Andri; Utami, Rifka Nurul; Salampe, Mirnawati; Emran, Talha Bin; Lima, Clara Mariana Gonçalves; Chopra, Hitesh; Gandara, Jesus Simal
Tuberculosis has become a major health problem globally. This is worsened by the emergence of resistant strains of Mycobacterium tuberculosis showing ability to evade the effectiveness of the current ant mycobacterial therapies. Therefore, the efforts carried out to explore new entities from many sources, including marine, are critical. This review summarizes several marine-derived macrolides that show promising activity against M. tuberculosis. We also provide information regarding the biosynthetic processes of marine macrolides, including the challenges that are usually experienced in this process. As most of the studies reporting the ant mycobacterial activities of the listed marine macrolides are based on in vitro studies, the future direction should consider expanding the trials to in vivo and clinical trials. In addition, in silico studies should also be explored for a quick screening on marine macrolides with potent activities against mycobacterial infection. To sum up, macrolides derived from marine organisms might become therapeutical options for tackling ant mycobacterial resistance of M. tuberculosis.
Mechanistic insights into anti-inflammatory and immunosuppressive effects of plant secondary metabolites and their therapeutic potential for rheumatoid arthritis
(2024-06-24) Yuandani; Jantan, Ibrahim; Salim, Emil; Septama, Abdi Wira; Rullah, Kamal; Nainu, Firzan; Fasihi Mohd Aluwi, Mohd Fadhlizil; Bin Emran, Talhah; Roney, Miah; Khairunnisa, Nur Aini; Raina Nasution, Halimah; Fadhil As'ad, Muh; Shamsudin, Nur Farisya; Abdullah, Maryam Aisyah; Marwa Rani, Haya Luthfiyyah; Mahabbah Al Chaira, Diany
The anti-inflammatory and immunosuppressive activities of plant secondary metabolites are due to their diverse mechanisms of action against multifarious molecular targets such as modulation of the complex immune system associated with rheumatoid arthritis (RA). This review discussed and critically analyzed the potent anti-inflammatory and immunosuppressive effects of several phytochemicals and their underlying mechanisms in association with RA in experimental studies, including preliminary clinical studies of some of them. A wide range of phytochemicals including phenols, flavonoids, chalcones, xanthones, terpenoids, alkaloids, and glycosides have shown significant immunosuppressive and anti-inflammatory activities in experimental RA models and a few have undergone clinical trials for their efficacy and safety in reducing RA symptoms and improve patient outcomes. These phytochemicals have potential as safer alternatives to the existing drugs in the management of RA, which possess a wide range of serious side effects. Sufficient preclinical studies on safety and efficacy of these phytochemicals must be performed prior to proper clinical studies. Further studies are needed to address the barriers that have so far limited their human use before the therapeutic potential of these plant-based chemicals as anti-arthritic agents in the treatment of RA is fully realized.
Multidrug Resistance in Cancer
(Daffodil International University, 2022-06-23) Emran, Talha Bin; Shahriar, Asif; Mahmud, Aar Rafi; Rahman, Tanjilur; Abir, Mehedy Hasan; Siddiquee, Mohd. Faijanur - Rob; Ahmed, Hossain; Rahman, Nova; Nainu, Firzan; Wahyudin, Elly; Mitra, Saikat; Dhama, Kuldeep; Habiballah, Mahmoud M.; Haque, Shafiul; Islam, Ariful; Hassan, Mohammad Mahmudul
Cancer is one of the leading causes of death worldwide. Several treatments are available for cancer treatment, but many treatment methods are ineffective against multidrug-resistant cancer. Multidrug resistance (MDR) represents a major obstacle to effective therapeutic interventions against cancer. This review describes the known MDR mechanisms in cancer cells and discusses ongoing laboratory approaches and novel therapeutic strategies that aim to inhibit, circumvent, or reverse MDR development in various cancer types. In this review, we discuss both intrinsic and acquired drug resistance, in addition to highlighting hypoxia- and autophagy-mediated drug resistance mechanisms. Several factors, including individual genetic differences, such as mutations, altered epigenetics, enhanced drug efflux, cell death inhibition, and various other molecular and cellular mechanisms, are responsible for the development of resistance against anticancer agents. Drug resistance can also depend on cellular autophagic and hypoxic status. The expression of drug-resistant genes and the regulatory mechanisms that determine drug resistance are also discussed. Methods to circumvent MDR, including immunoprevention, the use of microparticles and nanomedicine might result in better strategies for fighting cancer.
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.
Natural Products Targeting Inflammation-Related Metabolic Disorders: A Comprehensive Review
(Elsevier, 2023-06-02) Nainu, Firzan; Frediansyah, Andri; Mamada, Sukamto S.; Permana, Andi Dian; Salampe, Mirnawati; Chandran, Deepak; Emran, Talha Bin; Simal-Gandara, Jesus
Currently, the incidence of metabolic disorders is increasing, setting a challenge to global health. With major advancement in the diagnostic tools and clinical procedures, much has been known in the etiology of metabolic disorders and their corresponding pathophysiologies. In addition, the use of in vitro and in vivo experimental models prior to clinical studies has promoted numerous biomedical breakthroughs, including in the discovery and development of drug candidates to treat metabolic disorders. Indeed, chemicals isolated from natural products have been extensively studied as prospective drug candidates to manage diabetes, obesity, heart-related diseases, and cancer, partly due to their antioxidant and anti-inflammatory properties. Continuous efforts have been made in parallel to improve their bioactivity and bioavailability using selected drug delivery approaches. Here, we provide insights on recent progress in the role of inflammatory-mediated responses on the initiation of metabolic disorders, with particular reference to diabetes mellitus, obesity, heart-related diseases, and cancer. In addition, we discussed the prospective role of natural products in the management of diabetes, obesity, heart-related diseases, and cancers and provide lists of potential biological targets for high throughput screening in drug discovery and development. Lastly, we discussed findings observed in the preclinical and clinical studies prior to identifying suitable approaches on the phytochemical drug delivery systems that are potential to be used in the treatment of metabolic disorders.
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.