Current Topics in Medicinal Chemistry - Current Issue
Volume 25, Issue 8, 2025
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Targeting Various Pathogenic Pathways for the Development of Anti-alzheimer’s Drugs: An Update
Authors: Subiya Ambreen, Naurin Fatima, Mohammad Umar, Mohd Shaququzzaman, Mohammad Mumtaz Alam and Ruhi AliAlzheimer’s disease (AD) has been recognized as the most important cause of dementia, which is estimated to contribute more than 2 trillion USD in medical costs. AD patients encounter progressive neurodegenerative dementia associated with behavioural, linguistic, and visuospatial deficits. Although studies on the discovery of amyloid β (Aβ) and tau (the essential elements of plaques and tangles in AD) have shed light on the molecular pathological processes of AD, the exact cause of the condition is still largely unknown. The involvement of various proteins, such as amyloid-β, prion protein, tau, and α-synuclein has been linked to AD pathogenesis. The current AD treatments are mainly based on symptomatic management and restoration of neurotransmitters’ balance. There is a significant need to develop medications that can alter the underlying disease process and prevent its progression. The present manuscript provides a review of various hypotheses that have been proposed for AD pathogenesis. The manuscript has also explored the development of novel anti-AD drugs based on various pathogenic pathways, which are recently under various clinical trial phases.
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Targeted Cancer Stem Cell Therapeutics: An Update
Cancer stem cells (CSCs) have become a key player in the growth of tumors, the spread of cancer, and the resistance to therapeutic interventions. Targeting these elusive cell populations has the potential to fundamentally alter cancer treatment plans. CSCs, also known as tumor-initiating cells (TICs), are thought to play a role in both medication resistance and cancer recurrence. This is explained by their capacity to regenerate themselves and change into different kinds of cancer cells. Due to their higher expression of ATP-binding cassette (ABC) membrane transporters, enhanced epithelial to mesenchymal (EMT) characteristics, improved immune evasion, activation of survival signaling pathways, and improved DNA repair mechanisms, CSCs exhibit extraordinary resistance to therapies. This comprehensive analysis delves into advancements in the domain of Targeted Cancer Stem Cell Therapeutics, concentrating on unraveling the distinctive traits of CSCs and the therapeutic methods devised to eliminate them.
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Phytochemicals for Cancer Treatment: An Update on Plant-derived Anti-cancer Compounds and their Mechanisms of Action
Cancer remains one of the major causes of morbidity and mortality worldwide. Scientists from different fields are working to devise an efficient treatment strategy in order to reduce the global burden of cancer. Commonly used treatment approaches for cancer treatment include chemotherapy, immunotherapy, photodynamic therapy, radiation, surgery, etc. These treatment procedures have several pitfalls, such as toxicity, limited bioavailability, rapid elimination, poor specificity, and high cost. On the other side, plant-derived anticancer compounds exhibit several advantages and can overcome these shortcomings. Plant-based anticancer compounds are safer, potent, easily available, and comparatively cost-effective. The current review discusses pure plant-based compounds that are used as a therapeutic remedy for anticancer application. The proposed mechanisms of action, through which these compounds inhibit cancer cell growth, tumor growth, angiogenesis, instigate apoptosis, cytotoxicity, mitochondrial membrane degradation, and reduce cell viability as well as cell cycle progression, are also reviewed. These naturally occurring compounds exhibit great therapeutic potential and could be used as candidate drugs in clinical applications.
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Pharmacological and Therapeutic Potential of Berbamine: A Potent Alkaloid from Genus Berberis
Berbamine (Ber) is an active medicinal bisbenzylisoquinoline alkaloid, which is usually obtained from different plants of the genus Berberis (family Berberidaceae) and is used to cure various disorders in traditional Chinese and Ayurvedic systems of medicine. Numerous in-vitro and in-vivo studies revealed the apoptotic and cytotoxic potential of Ber against different cell lines (SMMC-7721, A549, MDA-MB-231, and K562) by upregulating pro-apoptotic (Bax, p53) and downregulating anti-apoptotic (Bcl-2, survivin) proteins. Other pharmacological attributes ascribed to Ber included cardioprotective, anti-diabetic, anti-inflammatory, antimalarial, antioxidant, anti-hypercholesterolemic, and anti-allergic. Moreover, the synergistic effect of Ber improved the therapeutic potential of different drugs (paclitaxel (PTL), gemcitabine, dexamethasone, doxorubicin (DOX), and celecoxib) in different models. Various attempts could fabricate biologically active derivatives of Ber, such as 4-chlorobenzoyl berbamine (CBB) and O-4-ethoxyl-butyl-berbamine (EBB). The review focuses on the medicinal applications of Ber, particularly anti-cancer, cardioprotective, and anti-inflammatory, along with the mechanism of action.
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Literature-based Survey of Medicinal Plants Since 1900: A Case Study to Treat Cancer in the Sultanate of Oman
Ethnopharmacological RelevanceDue to the high prevalence of cancer, researchers for the past decades have made considerable efforts for its management and treatment. Medicinal plants have always been exploited to discover novel anticancer agents. Oman’s huge biodiversity has created a rich source of traditional medicine.
ObjectiveThe current survey has aimed to document the traditionally used medicinal plants of Oman and their therapeutic role in the treatment of cancer.
Materials and MethodsThis study comprises of literature-based survey through different databases, including Google, Scopus, Google Scholar, Web of Science, Science Direct, Springer Link, BioMed Central and PubMed.
ResultsThe current review revealed a total of 57 plant species that belong to 35 families that are used in the treatment of cancer in Oman. Most documented plants belong to Solanaceae (6 sp.), Apocyanaceae (5 sp.) and Lamiaceae (4 sp.). The literature reveals that the residents of the area mostly use leaves (38.5%) and prepare their recipes in the form of decoction (40.3%). Moreover, herbs are the most dominant life form (43.85%). Among all forms of cancer in Oman, breast (47%), wound (26), and lung cancer (0.5%) were found dominantly. A literature study confirmed that the medicinal plants used for cancer in Oman are rich in phytochemicals such as quercetin, allicin, coumarin, alliin, kaempferol, solamargine, rutin, lupeol, ursolic acid and luteolin that have shown significant biological activities including anti-cancer potential. It reflects the efficacy of these plants to be used as a medicine in clinical trials. Among all, Boswellia sacra Flueck. is of key importance due to the presence Boswellic acid being used for the treatment of different types of cancer.
ConclusionThe residents of Oman have great knowledge about the traditional use of medicinal plants for the treatment of various diseases like cancer. The therapeutic potential and physiological efficacy of Omani medicinal plants should be further explored at a molecular level via in vivo and in vitro experiments.
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Galegine, a Bioprivileged Alkaloid from Tithonia tubaeformis: Antipyretic Activity Insights
BackgroundIn continuation of our chemical and biological work on Tithonia tubaeformis, we evaluated the antipyretic activity of its extract which on fractionation gives a pure alkaloid galegine. Galegine a bioprivileged compound, is a hemiterpene bearing a guanidine group, which holds significant importance in medicinal chemistry. Biological activities such as antimicrobial, antidiabetic, anti-inflammatory, cardiovascular, anticancer, and antihypertensive, are often associated with guanidine-containing molecules.
ObjectiveGiven the biological importance of guanidine and in search of safe antipyretic agents from natural resources, an in vivo antipyretic activity of methanolic extract of T. tubaeformis and galegine was conducted to discover a potential hypothermic drug candidate from the plant.
MethodsIn vivo, the antipyretic activity of galegine (5, 25, and 50 mg/kg doses) and methanolic extract of T. tubaeformis (50, 100, and 200 mg/kg doses) was investigated by employing yeast-induced pyrexia in mice model. In silico molecular docking analysis involving target enzymes cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2), and microsomal prostaglandin E synthase-1 (mPGES-1) was conducted. Additionally, galegine underwent ADME/T profiling using SwissADME and Protox-II tools to evaluate its bioavailability and safety profiles.
ResultsBoth the extract and galegine showed a progressive dose-dependent reduction in body temperatures of the hyperthermic test animals. Moreover, in silico molecular docking analysis revealed significant binding affinities ranging from -3.58 to -5.41 kcal/mol. ADME/T analyses of galegine predicted its high drug-likeness and good safety profile.
ConclusionThese biological and computational approaches supported T. tubaeformis in addressing pyrexia, with the isolated compound galegine emerging as a promising antipyretic agent.
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Ethnobotanical Study of Knowledge and Herbal Recipes of Medicinal Plants in Ancient Izki, Al Dakhliya Region, Sultanate of Oman
IntroductionThe medicinal plants of Izki hold significant ethnopharmacological relevance, serving as primary healthcare resources for generations. These plants exhibit known pharmacological properties, making them crucial for traditional and modern therapeutic applications.
ObjectivesThe primary goal of this study was to record, conserve, and analyze the traditional knowledge of medicinal plants in Izki. It also aimed to evaluate the therapeutic potential of these plants for treating various ailments while identifying their pharmacological relevance for modern applications.
Materials and MethodsThe study involved interviews with 300 local residents to record their traditional knowledge of therapeutic herbs. Quantitative methods were employed. Plant specimens were collected, identified, and submitted to the herbarium.
ResultsThe study recorded 65 medicinal plants (22 cultivated, 43 wild) used for 62 disease categories. Eye diseases (0.721; 13 taxa) and bone fractures (0.700; 13 taxa) showed higher consensus among respondents. FL% analysis highlighted Tephrosia apollinea (69.2%), Trachyspermum ammi (62.5%), and Azadirachta indica (53.3%) as culturally significant. Rhazya stricta emerged as an antirheumatic agent, reflecting shared ethnobotanical practices between India and Oman. Plants like Rhazya stricta, Fagonia indica, Trachyspermum ammi, and Ziziphus spina-christi demonstrated consistent regional applications, underscoring their potential for pharmacological investigation.
ConclusionThis study underscores Izki's rich ethnobotanical knowledge, with extensive use of leaves, fruits, and whole plants for medicinal, dietary, and hygienic purposes. Conservation efforts, sustainable harvesting, and collaborations with pharmaceutical sciences are essential to validate the pharmacological potential of Rhazya stricta, Fagonia indica, Trachyspermum ammi, and Ziziphus spina-christi and bridge traditional knowledge with modern medicine.
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Volumes & issues
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Volume 25 (2025)
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Volume 24 (2024)
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Volume 23 (2023)
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Volume 22 (2022)
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Volume 21 (2021)
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Volume 20 (2020)
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Volume 19 (2019)
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Volume 18 (2018)
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Volume 17 (2017)
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Volume 16 (2016)
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Volume 15 (2015)
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Volume 14 (2014)
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Volume 13 (2013)
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Volume 12 (2012)
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Volume 11 (2011)
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Volume 10 (2010)
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Volume 9 (2009)
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Volume 8 (2008)
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Volume 7 (2007)
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Volume 6 (2006)
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Volume 5 (2005)
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Volume 4 (2004)
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Volume 3 (2003)
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Volume 2 (2002)
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Volume 1 (2001)
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