Browsing by Author "Emran, Talha Bin"

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A Comprehensive Discussion in Vaginal Cancer Based on Mechanisms, Treatments, Risk Factors and Prevention
(Daffodil International University, 2022-07-18) Baral, Sumit Kumar; Biswas, Partha; Kaium, Md. Abu; Islam, Md. Aminul; Dey, Dipta; Saber, Md Al; Rahaman, Tanjim Ishraq; A. M.; Emran, Talha Bin; Hasan, Md. Nazmul; Jeong, Mi-Kyung; Han, Ihn; Rahman, Md. Ataur; Kim, Bonglee
Vaginal cancer is a rare and uncommon disease that is rarely discussed. Although vaginal cancer traditionally occurs in older postmenopausal women, the incidence of high-risk human papillomavirus (HPV)-induced cancers is increasing in younger women. Cervical cancer cells contain high-risk human papillomavirus (HPV) E6 and E7 proteins and inhibiting HPV gene expression leads the cells to stop proliferating and enter senescence. As E6, and E7 protein promoted the carcinogenesis mechanism, and here not only regulate the cellular degradation of P53, and pRb but also enhances the cell proliferation along with E6 protein targets the p53 for breakdown and subsequently promote the apoptotic cell death, and DNA repair inhibition, that is indispensable to the continue the lifecycle of the HPV. As a synchronous or metachronous tumor, vaginal cancer is frequently found in combination with cervical cancer. It is uncertain what causes invasive female vaginal organ cancer. HPV type 16 is the most often isolated HPV type in female vaginal organ cancers. Due to cancer’s rarity, case studies have provided the majority of etiologic findings. Many findings demonstrate that ring pessaries, chronic vaginitis, sexual behavior, birth trauma, obesity, vaginal chemical exposure, and viruses are all risk factors. Because of insufficient understanding and disease findings, we are trying to find the disease’s mechanism with the available data. We also address different risk factors, therapy at various stages, diagnosis, and management of vaginal cancer in this review.
A Comprehensive Discussion in Vaginal Cancer Based on Mechanisms, Treatments, Risk Factors and Prevention
(Daffodil International University, 2022-07-18) Baral, Sumit Kumar; Biswas, Partha; Kaium, Md. Abu; Islam, Md. Aminul; Dey, Dipta; Saber, Md Al; Rahaman, Tanjim Ishraq; M, A.; Emran, Talha Bin; Hasan, Md. Nazmul; Jeong, Mi-Kyung; Han, Ihn; Rahman, Md. Ataur; Kim, Bonglee
Vaginal cancer is a rare and uncommon disease that is rarely discussed. Although vaginal cancer traditionally occurs in older postmenopausal women, the incidence of high-risk human papillomavirus (HPV)-induced cancers is increasing in younger women. Cervical cancer cells contain high-risk human papillomavirus (HPV) E6 and E7 proteins and inhibiting HPV gene expression leads the cells to stop proliferating and enter senescence. As E6, and E7 protein promoted the carcinogenesis mechanism, and here not only regulate the cellular degradation of P53, and pRb but also enhances the cell proliferation along with E6 protein targets the p53 for breakdown and subsequently promote the apoptotic cell death, and DNA repair inhibition, that is indispensable to the continue the lifecycle of the HPV. As a synchronous or metachronous tumor, vaginal cancer is frequently found in combination with cervical cancer. It is uncertain what causes invasive female vaginal organ cancer. HPV type 16 is the most often isolated HPV type in female vaginal organ cancers. Due to cancer’s rarity, case studies have provided the majority of etiologic findings. Many findings demonstrate that ring pessaries, chronic vaginitis, sexual behavior, birth trauma, obesity, vaginal chemical exposure, and viruses are all risk factors. Because of insufficient understanding and disease findings, we are trying to find the disease’s mechanism with the available data. We also address different risk factors, therapy at various stages, diagnosis, and management of vaginal cancer in this review.
A Comprehensive Perspective of Traditional Arabic or Islamic Medicinal Plants as an Adjuvant Therapy Against COVID-19
(Elsevier, 2023-01-13) Ahmed, Shabina Ishtiaq; Jamil, Sehrish; Ismatullah, Humaira; Hussain, Rashid; Bibi, Shabana; Khandaker, Mayeen Uddin; Naveed, Aisha; Idris, Abubakr M.; Emran, Talha Bin
COVID-19 is a pulmonary disease caused by SARS-CoV-2. More than 200 million individuals are infected by this globally. Pyrexia, coughing, shortness of breath, headaches, diarrhoea, sore throats, and body aches are among the typical symptoms of COVID-19. The virus enters into the host body by interacting with the ACE2 receptor. Despite many SARS-CoV-2 vaccines manufactured by distinct strategies but any evidence-based particular medication to combat COVID-19 is not available yet. However, further research is required to determine the safety and effectiveness profile of the present therapeutic approaches. In this study, we provide a summary of Traditional Arabic or Islamic medicinal (TAIM) plants' historical use and their present role as adjuvant therapy for COVID-19. Herein, six medicinal plants Aloe barbadensis Miller, Olea europaea, Trigonella foenum-graecum, Nigella sativa, Cassia angustifolia, and Ficus carica have been studied based upon their pharmacological activities against viral infections. These plants include phytochemicals that have antiviral, immunomodulatory, antiasthmatic, antipyretic, and antitussive properties. These bioactive substances could be employed to control symptoms and enhance the development of a possible COVID-19 medicinal synthesis. To determine whether or if these TAIMs may be used as adjuvant therapy and are appropriate, a detailed evaluation is advised.
A Computational Simulation Appraisal of Banana Lectin as a Potential Anti-SARS-CoV-2 Candidate by Targeting the Receptor-Binding Domain
(Springer, 2023-11-28) Hessel, Sofia Safitri; Dwivany, Fenny Martha; Zainuddin, Ima Mulyama; Wikantika, Ketut; Celik, Ismail; Emran, Talha Bin; Tallei, Trina Ekawati
Background The ongoing concern surrounding coronavirus disease 2019 (COVID-19) primarily stems from continuous mutations in the genome of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), leading to the emergence of numerous variants. The receptor-binding domain (RBD) in the S1 subunit of the S protein of the virus plays a crucial role in recognizing the host’s angiotensin-converting enzyme 2 (hACE2) receptor and facilitating cell membrane fusion processes, making it a potential target for preventing viral entrance into cells. This research aimed to determine the potential of banana lectin (BanLec) proteins to inhibit SARS-CoV-2 attachment to host cells by interacting with RBD through computational modeling. Materials and methods The BanLecs were selected through a sequence analysis process. Subsequently, the genes encoding BanLec proteins were retrieved from the Banana Genome Hub database. The FGENESH online tool was then employed to predict protein sequences, while web-based tools were utilized to assess the physicochemical properties, allergenicity, and toxicity of BanLecs. The RBDs of SARS-CoV-2 were modeled using the SWISS-MODEL in the following step. Molecular docking procedures were conducted with the aid of ClusPro 2.0 and HDOCK web servers. The three-dimensional structures of the docked complexes were visualized using PyMOL. Finally, molecular dynamics simulations were performed to investigate and validate the interactions of the complexes exhibiting the highest interactions, facilitating the simulation of their dynamic properties. Results The Banec proteins were successfully modeled based on the RNA sequences from two species of banana (Musa sp.). Moreover, an amino acid modification in the BanLec protein was made to reduce its mitogenicity. Theoretical allergenicity and toxicity predictions were conducted on the BanLecs, which suggested they were likely non-allergenic and contained no discernible toxic domains. Molecular docking analysis demonstrated that both altered and wild-type BanLecs exhibited strong affinity with the RBD of different SARS-CoV-2 variants. Further analysis of the molecular docking results showed that the BanLec proteins interacted with the active site of RBD, particularly the key amino acids residues responsible for RBD’s binding to hACE2. Molecular dynamics simulation indicated a stable interaction between the Omicron RBD and BanLec, maintaining a root-mean-square deviation (RMSD) of approximately 0.2 nm for a duration of up to 100 ns. The individual proteins also had stable structural conformations, and the complex demonstrated a favorable binding-free energy (BFE) value. Conclusions These results confirm that the BanLec protein is a promising candidate for developing a potential therapeutic agent for combating COVID-19. Furthermore, the results suggest the possibility of BanLec as a broad-spectrum antiviral agent and highlight the need for further studies to examine the protein’s safety and effectiveness as a potent antiviral agent.
A Critical Review on the Potency of Phytoconstituents in the Management of COVID-19
(JPAM, 2023-09-02) Raman, Kannan; Rajagopal, Kalirajan; Swaminathan, Gomathi; Jupudi, Srikanth; Dhama, Kuldeep; Barua, Rashu; Emran, Talha Bin; Osman, Hamid; Khandaker, Mayeen Uddin
Natural products and their derivatives have traditionally been used as a source of therapeutic agents. Their beneficial properties are due to large varieties in their chemical structures and biochemical actions. The discovery of natural products such as phytoconstituents have crucial role in the development of less toxic and more effective drugs. Phytoconstituents have shown to be beneficial in treating viral diseases such as the previous chikungunya virus, hepatitis C virus, SARS, and MERS viral diseases. Flavonoids, alkaloids, terpenoids, and other group of compounds combat against COVID-19 in several ways like by protease inhibition, spike protein inhibition, Nrf2 inhibition. The accumulation of NRF2 inhibits the development of the SARS-CoV-2 virus and stimulates anti-inflammatory action. The present review highlights the therapeutic importance of compounds isolated from medicinal plants and/or herbs, such as crude extracts of Curcumin I-III, Leptodactylone, Ginsenoside-Rb1, Lycorine, Reserpine, Saikosaponin B2, Cepharanthine, Withanoside V, Gingerol, Piperanine, chromans, flavonoids, Amentoflavone etc. against SARS-CoV-2. Natural products are typically safe, stable, and dependable source for finding drugs to control the current pandemic. Antiviral secondary metabolites many medicinal plants have given ingredients that were isolated. The selected plants based phytoconstituents may potentially be used against viruses’ development on anti-SARS-CoV-2 to offer a reference point in this field.
A Decade's Worth of Impact Dox Loaded Liposomes in Anticancer Activity
(Daffodil International University, 22-11-01) Ghosh, Puja; Tiwari, Himja; Lakkakula, Jaya; Roy, Arpita; Emran, Talha Bin; Rashid, Summya; Alghamdi, Saad; Rajab, Bodour S.; Almehmadi, Mazen; Allahyani, Mamdouh; Aljuaid, Abdulelah; Alsaiari, Ahad Amer; Sharma, Rohit; Babalghith, Ahmad O.
Clinically approved therapeutics associated with cancer are limited to mostly chemotherapy, surgery and radiotherapy in spite of the advancements in the biomedical field. Due to the cardiotoxicity and uncountable side effects brought by the prevailing treatment strategies, demands are growing for targeted drug delivery using nanomaterials. For this the most commonly used drug, doxorubicin (DOX) is encapsulated within several type of nanovesicles to observe their anticancer activity. Among them, DOX encapsulated liposomes gained popularity because of their clinical success and lower toxicity. To enhance their efficiency and site specific delivery, attempts are made to modify the liposomes by combining them with peptides, aptamers, antibodies etc to develop pH, thermal, UV-sensitive and electro-magnetic liposomal nanocarriers for controlled drug release. The novel strategies for the treatment of Breast, Lung, Liver, Pancreatic, Prostate, Ovarian, Cervical, Blood, Brain and Colon cancer using modified liposomes encapsulating DOX are illustrated in this review.
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.
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.
A Spotlight on Alkaloid Nanoformulations for the Treatment of Lung Cancer
(Scopus, 22-10-18) Sindhoor, S. M.; Naveen, Raghavendra; Rao, GSN Koteswara; Gopan, Gopika; Chopra, Hitesh; Park, Moon Nyeo; Alshahrani, Mohammed Merae; Jose, Jobin; Emran, Talha Bin; Kim, Bonglee
Numerous naturally available phytochemicals have potential anti-cancer activities due to their vast structural diversity. Alkaloids have been extensively used in cancer treatment, especially lung cancers, among the plant-based compounds. However, their utilization is limited by their poor solubility, low bioavailability, and inadequacies such as lack of specificity to cancer cells and indiscriminate distribution in the tissues. Incorporating the alkaloids into nanoformulations can overcome the said limitations paving the way for effective delivery of the alkaloids to the site of action in sufficient concentrations, which is crucial in tumor targeting. Our review attempts to assess whether alkaloid nanoformulation can be an effective tool in lung cancer therapy. The mechanism of action of each alkaloid having potential is explored in great detail in the review. In general, Alkaloids suppress oncogenesis by modulating several signaling pathways involved in multiplication, cell cycle, and metastasis, making them significant component of many clinical anti-cancerous agents. The review also explores the future prospects of alkaloid nanoformulation in lung cancer. So, in conclusion, alkaloid based nanoformulation will emerge as a potential gamechanger in treating lung cancer in the near future.
Acridine as an Anti-Tumour Agent: A Critical Review
(MDPI, 2023-12-26) Varakumar, Potlapati; Rajagopal, Kalirajan; Aparna, Baliwada; Raman, Kannan; Byran, Gowramma; Lima, Clara Mariana Gonçalves; Rashid, Salma; Nafady, Mohammed H; Emran, Talha Bin; Wybraniec, Sławomir
This review summarized the current breakthroughs in the chemistry of acridines as anti-cancer agents, including new structural and biologically active acridine attributes. Acridine derivatives are a class of compounds that are being extensively researched as potential anti-cancer drugs. Acridines are well-known for their high cytotoxic activity; however, their clinical application is restricted or even excluded as a result of side effects. The photocytotoxicity of propyl acridine acts against leukaemia cell lines, with C1748 being a promising anti-tumour drug against UDP-UGT's. CK0403 is reported in breast cancer treatment and is more potent than CK0402 against estrogen receptor-negative HER2. Acridine platinum (Pt) complexes have shown specificity on the evaluated DNA sequences; 9-anilinoacridine core, which intercalates DNA, and a methyl triazene DNA-methylating moiety were also studied. Acridine thiourea gold and acridinone derivatives act against cell lines such as MDA-MB-231, SK-BR-3, and MCF-7. Benzimidazole acridine compounds demonstrated cytotoxic activity against Dual Topo and PARP-1. Quinacrine, thiazacridine, and azacridine are reported as anti-cancer agents, which have been reported in the previous decade and were addressed in this review article.
Acute Hepatitis of Unknown Origin in Pediatric Age Group
(MDPI Publications, 2022-12-20) Patel, Neil; Sethi, Yashendra; Kaka, Nirja; Kaiwan, Oroshay; Gupta, Ishita; Shaheen, Rahma Sameh; Sapoor, Shady; Chopra, Hitesh; Popoviciu, Mihaela Simona; Emran, Talha Bin; Cavalu, Simona
Acute hepatitis has always been a public health concern, but the recent clustering of cases in various parts of the world has drawn some special attention. The sudden rise in cases has mainly been among the pediatric population of around 35 countries around the world, including developed countries such as the United States, the United Kingdom, and European countries. The outbreaks have had a devastating impact, with around 10% of the affected patients developing liver failure. The clinical presentation of patients resembles any other case of acute hepatitis, with the major symptoms being: jaundice (68.8%), vomiting (57.6%), and gastrointestinal symptoms such as abdominal pain (36.1%) and nausea (25.7%). Interestingly, the cases have tested negative for hepatotropic viruses Hep A, B, C, and E, thus giving rise to the terms Hepatitis of Unknown Origin or non-HepA–E hepatitis. Many causes have been attributed to the disease, with major evidence seen for adenovirus and SARS-CoV-2. International agencies have stressed on establishing diagnostic and management protocols to limit these outbreaks. As the understanding has evolved over time, diagnostic and management faculties have found more shape. The current review was designed to comprehensively compile all existing data and whittle it down to evidence-based conclusions to help clinicians.
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.
Ammodaucus Leucotrichus Seed Extract as a Potential Therapy in Animal Models of Rheumatoid Arthritis Induced by Complete Freund Adjuvant and Chicken Cartilage Collagen
(Scopus, 2024-05-28) Djehiche, Cheima; Benzidane, Nadia; Djeghim, Hanene; Tebboub, Mehdi; Mebrek, Saad; Abdelouhab, Katia; Baghiani, Abderrahmane; Charef, Noureddine; Messaoudi, Mohammed; Bensouici, Chawki; Lebsir, Rabah; Emran, Talha Bin; Alsalme, Ali; Cornu, David; Bechelany, Mikhael; Arrar, Lekhmici; Barhoum, Ahmed
This study assessed the efficacy of an Ammodaucus leucotrichus seed extract to treat rheumatoid arthritis in rat models of this disease. Rheumatoid arthritis was induced in rats using two methods: immunization with 100 µL of Complete Freund Adjuvant (CFA) and immunization with 100 µL of a 3 mg/ml solution of type II collagen (CII) from chicken cartilage. The therapeutic potential of the extract was assessed at different doses (150, 300, and 600 mg/kg/day for 21 days in the CII-induced arthritis model and for 14 days in the CFA-induced arthritis model) and compared with methotrexate (MTX; 0.2 mg/kg for the same periods), a commonly used drug for rheumatoid arthritis treatment in humans. In both models (CII-induced arthritis and CFA-induced arthritis), walking distance, step length, intra-step distance and footprint area were improved following treatment with the A. leucotrichus seed extract (all concentrations) and MTX compared with untreated animals. Both treatments increased the serum concentration of glutathione and reduced that of complement C3, malondialdehyde and myeloperoxidase. Radiographic data and histological analysis indicated that cartilage destruction was reduced already with the lowest dose of the extract (100 mg/kg/dose) in both models. These results show the substantial antiarthritic potential of the A. leucotrichus seed extract, even at the lowest dose, suggesting that it may be a promising alternative therapy for rheumatoid arthritis and joint inflammation. They also emphasize its efficacy at various doses, providing impetus for more research on this extract as a potential therapeutic agent for arthritis.
An In-Silico Identification of Potential Flavonoids against Kidney Fibrosis Targeting TGFβR-1
(Scopus, 22-11-02) Rahman, MD. Hasanur; Biswas, Partha; Dey, Dipta; Hannan, Md. Abdul; Sahabuddin, Md.; Araf, Yusha; Kwon, Youngjoo; Emran, Talha Bin; Ali, Md. Sarafat; Uddin, Md Jamal
Fibrosis is a hallmark of progressive kidney diseases. The overexpression of profibrotic cytokine, namely transforming growth factor β (TGF-β) due to excessive inflammation and tissue damage, induces kidney fibrosis. The inhibition of TGF-β signaling is markedly limited in experimental disease models. Targeting TGF-β signaling, therefore, offers a prospective strategy for the management of kidney fibrosis. Presently, the marketed drugs have numerous side effects, but plant-derived compounds are relatively safer and more cost-effective. In this study, TGFβR-1 was targeted to identify the lead compounds among flavonoids using various computational approaches, such as ADME/T (absorption, distribution, metabolism, and excretion/toxicity) analysis, molecular docking, and molecular dynamics simulation. ADME/T screening identified a total of 31 flavonoids with drug-like properties of 31 compounds, a total of 5 compounds showed a higher binding affinity to TGFβR-1, with Epicatechin, Fisetin, and Luteolin ranking at the top three (-13.58, -13.17, and -10.50 kcal/mol, respectively), which are comparable to the control drug linagliptin (-9.074 kcal/mol). The compounds also exhibited outstanding protein-ligand interactions. The molecular dynamic simulations revealed a stable interaction of these compounds with the binding site of TGFβR-1. These findings indicate that flavonoids, particularly Epicatechin, Fisetin, and Luteolin, may compete with the ligand-binding site of TGFβR-1, suggesting that these compounds can be further evaluated for the development of potential therapeutics against kidney fibrosis. Further, in-vitro and in-vivo studies are recommended to support the current findings.
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.
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
Anti-Pathogenic, Anti-Diabetic, Anti-Inflammatory, Antioxidant, and Wound Healing Efficacy of Datura metel L. Leaves
(Daffodil International University, 22-07-09) Prasathkumar, Murugan; Anisha, Salim; Khusro, Ameer; Essa, Musthafa Mohamed; Chidambaram, Saravana Babu; Qoronfleh, M. Walid; Sadhasivam, Subramaniam; Sahibzada, Muhammad Umar Khayam; Alghamdi, Saad; Abdulaziz, Mazen Almehmadi j, Osama; Khandaker, Mayeen Uddin; Faruque, Mohammad Rashed Iqbal; Emran, Talha Bin
Datura metel L. is an important medicinal plant of Solanaceae family which has extensive pharmacological properties. The present investigation was aimed to identify the presence of phytoconstituents and assess in vitro antibacterial, anti-biofilm, anti-diabetic, anti-inflammatory, antioxidant, cytotoxicity, and wound healing efficacy of D. metel leaves extract. Among different solvent extracts, methanolic extract showed higher amount of phenolic (124.61 ± 0.68 mg GAE/g), alkaloid (88.77 ± 1.01 mg AE/g), flavonoids (42.24 ± 0.18 mg QE/g), and tannins contents (38.72 ± 0.51 mg GAE/g). The extract exhibited not only significantly (P < 0.05) different antibacterial activities against pathogens tested but also showed maximum biofilm inhibition of 94, 88, and 92% against B. subtilis, MRSA, and E. coli, respectively. Anti-diabetic assay depicted 22.55 ± 0.62–79.41 ± 1.13% and 24.31 ± 1.47–72.59 ± 0.22% of α-amylase and α-glucosidase inhibition abilities of methanolic extract, respectively at varied concentrations. The methanolic extract showed potential anti-inflammatory effect (P < 0.05) by showing 28.11 ± 0.13, 34.94 ± 1.11, 55.73 ± 0.42, 73.28 ± 0.72, and 92.62 ± 1.33% of inhibition of protein denaturation at different concentrations with an IC50 value of 52.45 µg/mL. The extract revealed significant (P < 0.05) rate of ABTS scavenging, DPPH degradation, and reducing power assay in a concentration dependent manner. The cytotoxicity assay was demonstrated on L929 mouse fibroblast cell line and found > 90% of cell viability in the presence of methanolic extract, thereby indicating its non-toxicity effect. Wound healing assay indicated that methanolic extract at 50 µg/mL closed 100% of wound gap after 24 h with high rate of migration and proliferation. Furthermore, GC–MS chromatogram revealed the presence of several components in methanolic extract, including neophytadiene, hexadecanoic acid, and hentriacontane as principal phytoconstituents. In conclusion, methanolic extract of D. metel leaves could be used as potent therapeutic agent not only for treating metabolic diseases but also superficial chronic diabetic wounds.
Antibacterial and antibiotic-modifying activity of the commercialized essential oil of Copaifera spp. Associated with LED lights against a Staphylococcus aureus strain
(Scopus, 2024-03-30) Sampaio, Milena Alves de Lima; Araújo, Ana Carolina Justino de; Borges, Joao Oliveira; Lima, Clara Mariana Gonçalves; Coutinho, Henrique Douglas Melo; Freitas, Priscilla Ramos; Emran, Talha Bin; Obaidullah, Ahmad J.; Silva, Rakel Olinda Macedo da
Copaiba oil is widely used in medicine due to its antibacterial, anti-inflammatory, healing, antiviral, antiseptic and analgesic properties. Thus, the main objective of the study is to evaluate the antibacterial activity and modifier of the antibiotic action of the commercialized essential oil of four species of Copaifera spp. in combination with Ampicillin and LED lights against the multidrug-resistant strain of S. aureus (SA 10). The essential oil was obtained commercially through the doTERRA ¯ ® company. The evaluation of the antibacterial and modulating activity was performed using the microdilution methodology in a 96-well plate, using blue 415 nm, red 620 nm and yellow 590 nm LEDs and Ampicillin at an initial concentration of 1.024 µg/mL. The experiments were carried out in triplicate and submitted to ANOVA statistical analysis, considering a significant value of p < 0,05. The essential oil of Copaifera spp. did not show antibacterial activity alone, but showed significant modifying activity when combined with Ampicillin in the absence of LED and with red LED. However, the yellow LED and the blue LED had no significant modulating effect. The results suggest the presence of an enzymatic mechanism of resistance, indicating relevance for the development of future scientific research, aiming to help in the treatment of lesions caused by multiresistant pathogens.
Anxiolytic, Antidepressant and Antioxidant Activity of the Methanol Extract of Canarium resiniferum Leaves
(Scopus, 22-08-03) Shah, Md Shahin; Tayab, Mohammed Abu; Rahman, Anisur; Hasan, Muhammad Nazmul; Talukder, Md Saddam Hossain; Uddin, A.M. Kafil; Jabed, Md; Chy, Md Nazim Uddin; Paul, Arkajyoti; Rahman, Md Masudur; Emran, Talha Bin; Seide, Veronique
Background and aim This study evaluated the anxiolytic, antidepressant, and antioxidant activity of the methanol extract of Canarium resiniferum (MECR) leaves, and determined the total phenolic and flavonoid contents in this extract. Experimental procedure The anxiolytic effect of MECR (100, 200, 400 mg/kg, p. o.) was tested in mice using the elevated plus-maze (EPM) test, the hole-board test (HBT), and the light-dark box (LDB) test. Its antidepressant effect was evaluated in the tail suspension (TST) and the forced swim (FST) tests. The total phenolic (TPC) and flavonoid (TFC) content was measured using standard colorimetric assays. Antioxidant activity was determined using the DPPH radical scavenging and ferric reducing antioxidant power (FRAP) assays. Results and conclusion MECR, at all doses, showed dose-dependent anxiolytic activity. At 400 mg/kg, it significantly increased the time spent and number of entries in the open arms (EPM test), the number of head-dips (HBT), and the time spent into the light compartment (LDB) test compared to the control. In the TST and FST, MECR dose-dependently reduced the duration of immobility compared to untreated animals. This was significant for all doses except for 100 mg/kg in the FST model. MECR showed high TPC and TFC (90.94 ± 0.75 mg GAE/g and 51.54 ± 0.78 mg QE/g of dried extract, respectively) and displayed potent activity in the DPPH radical scavenging (IC50 = 177.82 μg/mL) and FRAP assays. These findings indicate that C. resiniferum has the potential to alleviate anxiety and depression disorders, which merits further exploration.