Current Chemical Biology - Online First
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A Systematic Review on Pharmacological Activity and Novel Delivery Advances of Lycopene
Authors: Zulfa Nooreen, Awani Kumar Rai, Preeti Sharma, Fariha Sumayya and Ankur VishwakarmaAvailable online: 11 November 2025More LessIntroductionLycopene is a lipophilic red carotenoid pigment made up of eight isoprene units (octaprene) that are normally bound together head to tail, with the exception of the central part of the compound, wherein tail to tail attachment results in a symmetrical structure. Several physiological modes of action for lycopene have been investigated and documented in scientific research; the impacts on heart health, antineoplastic activity, and defence against oxidative stress are among the most extensively researched. Biological sources like Citrullus lanatus, Psidium guajava, Citrus paradisi, Rosa canina, Carica papaya, and apricot all contain significant amounts of it.
MethodsCurrent data were collected from PubMed, Google Scholar, ACS, SciFinder, Springer Nature, Bentham Science, PLOS One, MDPI and MEDLINE.
ResultsMuch scientific evidence suggests that eating nutritious food can help avoid chronic illnesses. Novel drug formulation of lycopene has also been researched to increase stability and solubility. Nanoparticles, liposomes, neosomes, microparticles and other novel agents have been investigated after 2015. Here in the review, we also compiled the marketed formulation.
DiscussionLycopene possesses various pharmacological aspects like anti-oxidant, anticancer, anti-inflammatory, antiulcer, hepatoprotective and cardiovascular approaches. Novel formulations enhanced its potency.
ConclusionThe Present review summarises pharmacological activities, delivery approaches of lycopene and marketed formulations.
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Renoprotective Role of Thymol-loaded Chitosan Nanoparticles in Cholestatic Rats
Available online: 05 November 2025More LessIntroductionAcute kidney damage (AKI) in cirrhosis, encompassing hepatorenal syndrome (HRS), is a prevalent and severe complication among cirrhotic patients, resulting in considerable morbidity and mortality. Thymol is derived from thyme extract and has numerous advantageous qualities, including antifungal, anti-inflammatory, antioxidant, anticancer, and antibacterial activities. The current study aims to augment the therapeutic efficacy of thymol against acute renal injury generated by bile duct ligation (BDL) through its encapsulation in chitosan nanoparticles.
MethodsThirty rats were categorized into five groups: sham, BDL, and cholestatic rats administered chitosan NPs, thymol, and CS-thymol nanoparticles.
ResultsThe administration of CS-thymol nanoparticles significantly improved renal function, as indicated by decreased levels of urea, creatinine, and uric acid. Furthermore, CS-thymol nanoparticles induced an increase in glutathione reductase (GSH) and catalase (CAT), while simultaneously reducing the levels of malondialdehyde (MDA) and nitric oxide (NO). The administration of CS-thymol nanoparticles diminished DNA damage and partially rehabilitated the abnormal structure of renal tissues in cholestatic rats. The immunohistochemistry analysis revealed a significant reduction in tumor necrosis factor-alpha (TNF-α) and Caspase-3 expression.
DiscussionCS-thymol nanoparticles demonstrated their potential in antioxidant, anti-inflammatory, and anti-apoptotic capabilities that safeguard the kidneys against cholestatic damage.
ConclusionThe inclusion of thymol into chitosan nanoparticles improves their antioxidant, anti-inflammatory, and anti-apoptotic properties, ultimately enhancing kidney function and structure in cholestatic rats.
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Natural Polyphenols as Multi-Targeted Agents in Diabetic Foot Ulcer: A Comprehensive Systematic Review
Authors: V.S. Sajisha and Saurabh SinghAvailable online: 22 October 2025More LessIntroductionDiabetic foot ulcers (DFUs) are a debilitating complication of diabetes mellitus, with a prevalence of 4–10% and a high risk of infection and limb amputation. This review explores the therapeutic potential of polyphenols, plant-derived secondary metabolites, in promoting wound healing in DFUs.
MethodsA systematic literature review was conducted in accordance with the PRISMA guidelines. Databases including PubMed, ISI Web of Knowledge, Google Scholar, and Scopus were searched for relevant studies from 1999 to 2025. Articles evaluating polyphenol-rich medicinal plants and their role in diabetic wound healing were selected based on defined inclusion and exclusion criteria.
ResultsPolyphenols such as curcumin, quercetin, gallic acid, resveratrol, and kaempferol demonstrated strong antioxidant, anti-inflammatory, and pro-angiogenic properties. These compounds modulate key molecular pathways—including VEGF, TGF-β, and NF-κB—resulting in enhanced fibroblast proliferation, collagen synthesis, and tissue regeneration. Plants like Curcuma longa, Punica granatum, and Vitis vinifera showed promising efficacy in both preclinical and limited clinical studies.
DiscussionThe evidence highlights the multi-targeted actions of polyphenols in addressing the impaired wound healing typical of diabetic conditions. However, limitations include variability in bioavailability, formulation inconsistencies, and a lack of standardized clinical trials.
ConclusionPolyphenols offer a promising, natural approach to managing DFUs, particularly in resource-limited settings. Their integration into therapeutic regimens may improve wound healing outcomes, though further clinical validation is necessary to optimize their use in mainstream diabetic care.
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Thieno-quinoline Derivatives as Promising Antimicrobial Agents: In Vitro and In Silico Insights
Authors: Yasmine Fekih, Yazid Datoussaid, Hadjer Missoum, Imane Abdelli, Boulanouar Messaoudi and Tarik AttarAvailable online: 21 October 2025More LessIntroductionThe global rise in antimicrobial resistance demands innovative therapeutic approaches. This study investigates novel 2-Aryl-9-chloro-5,6,7,8-tetrahydrothieno[3,2-b]quinoline derivatives (2a-e) as potential dual-action agents, targeting both pathogenic microorganisms and the phospholipase C-γ (PLC-γ) signaling pathway implicated in inflammatory responses.
MethodsFive derivatives were synthesized through a single-step POCl3-catalyzed cyclocondensation of thiophene carboxylic acids with cyclohexanone, yielding 55-71% of purified products. Antimicrobial efficacy was evaluated against Gram-positive (Staphylococcus aureus ATCC 25923, Bacillus cereus ATCC 10876), Gram-negative (Escherichia coli ATCC 25922, Pseudomonas aeruginosa clinical isolate), and Candida albicans ATCC 10231 strains using standardized CLSI protocols. Computational studies employed molecular docking (MolDock) and binding free energy calculations against PLC-γ (PDB ID:5EG3).
ResultsAmong the tested compounds, compounds 2-c and 2-e showed strong antibacterial activity against Staphylococcus aureus, even surpassing gentamicin. Compounds 2-b and 2-d, on the other hand, showed significant antifungal activity against Candida albicans, equivalent to that of DEPTIL BFC. Molecular docking revealed compound 2d (L4) as the most potent PLC-γ inhibitor (ΔG=-116.127 kcal/mol), forming π-alkyl interactions with Ala 567 in the catalytic pocket.
DiscussionThe structure-activity relationship demonstrates that chloro-substitution at position 9 enhances antimicrobial potency, while aryl modifications at position 2 influence PLC-γ binding affinity. These findings suggest a unique dual mechanism of action distinct from conventional antimicrobials.
Conclusionhis study highlights the biological potential of [Aryl-CTTQ] derivatives (2a-e), in particular their marked antibacterial activity and, for some, moderate antifungal activity. Compound 2d (L4) is distinguished by its high affinity for phospholipase C-γ, identified through in vitro and in silico analyses. These results validate the effectiveness of a computer-aided design approach to develop new therapeutic agents.
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The Potential of Iranian Medicinal Plants in Combating Candida Albicans, A Major Cause of Oral Candidiasis: A Systematic Review
Authors: Asma Sepahdar, Behnoush Selahbarzin, Kheyrie Baji, Pegah Shakib and Fatemeh AhmadpourAvailable online: 16 September 2025More LessIntroductionThe weaknesses of traditional drugs against fungi, such as resistance and adverse reactions highlight the urgent need for alternative therapies. Plant extracts offer great potential for developing alternative antifungal therapies against Candida albicans. The current systematic study aimed to introduce medicinal plants native to Iran that could effectively combat Candida albicans, the primary cause of oral candidiasis.
MethodIn this systematic review study, a search was performed for articles published in English from 2000 onwards in databases including PubMed, Google Scholar, ScienceDirect, Web of Sciences, and Scopus with keywords (“Herbal medicines” or “Extract” or “Essential oil” or ” Iran” or “Plant”) and “In vitro”, “In vivo”, and “Clinical trials,” considering the inclusion and exclusion criteria.
ResultsFrom 170 studies initially retrieved from ScienceDirect, PubMed, Scopus, Ovid, and Cochrane databases, 124 duplicates were removed, and after this, 75 studies were transferred to EndNote software.
DiscussionUsing the inclusion and exclusion criteria, 49 irrelevant studies were eliminated during the screening step once each study's title and abstract were assessed. Based on the availability of their full texts, the 45 remaining studies were evaluated. Finally, 37 studies were selected.
ConclusionsThe study examined the impact of native plants from Iran on C. albicans, a common cause of oral candidiasis, and suggests that by conducting more extensive research in the future, these plants could be used to develop new compounds for the treatment of oral candidiasis.
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Role of Chitosan Nanoparticles loaded with Pomegranate Peels Extract on High Fat Diet-Induced Obesity in Rats
Available online: 16 September 2025More LessIntroductionObesity is a chronic disease that is widespread throughout the world. Pomegranate is a fruit that has proven to provide beneficial health effects due to its high nutritional content and bioactive antioxidants. The current study aims to investigate the effect of chitosan nanoparticles loaded with pomegranate peel extract (PPE-CSNPs) on high-fat diet (HFD) induced obesity in male rats.
MethodsObesity was induced by feeding a high-fat diet for 4 weeks. Thirty rats were assigned into five main groups (6 rats/group) as follows: control (dist. water, orally), HFD control (dist. water, orally), HFD + pomegranate peel extract (PPE) (500 mg/kg, orally), HFD + chitosan-NP (60 mg/kg, orally), and HFD + PPE-CSNPs (60 mg/kg, orally).
ResultsThe treatment of PPE-CSNPs decreased body weight, glucose, alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, creatinine, urea, total cholesterol, triglycerides, low density lipoprotein-cholesterol, malondialdehyde, and nitric oxide, while high density lipoprotein-cholesterol, glutathione reduced and catalase levels increased. The histological examination revealed a significant enhancement in the structures of the liver and kidneys.
DiscussionThe antioxidant and hypolipidemic activities of PPE-CS surpassed those of PPE or CS individually, confirming the synergistic effect in obesity.
ConclusionThe combination of pomegranate extract with chitosan in the form of nanoparticles enhances their hypolipidemic efficacy in the treatment of obese rats. PPE-CSNPs are promising nanonatural products that could be used in obesity management.
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Phytopharmacology of Commiphora wightii (Guggulu): A Mini Review
Authors: Shreya Rawat, Urmi Chaurasia, Ishu Garg, Tushar Negi, Shivani Rawat and Raj KumariAvailable online: 16 September 2025More LessIntroductionGuggulu, an oleo gum resin obtained from the bark of Commiphora wightii, has been extensively researched for various medicinal and pharmacological applications, especially within the Indian Ayurvedic system. For human consumption, guggulu undergoes a shodhana process to create Shoddhit Guggulu. This refined form of guggulu contains several active phytomolecules that contribute to its pharmacological effects. Historically, guggulu has been used to address numerous health issues, including cardiovascular, dental, neurological, endocrine, reproductive, and infectious conditions.
MethodsReview articles and research papers from reputable journals regarding Commiphora wightii have been thoroughly analyzed. Extensive readings and discussions were conducted to summarize researchers' findings concerning the pharmacology and medicinal properties of the phytoconstituents present in the oleo gum.
ResultThe review explores research discussing the ethnobotanical uses of Commiphora wightii. With the rise in clinical studies and knowledge, guggulu has been thoroughly investigated for its anti-inflammatory, antioxidant, platelet-regulating, thyroid-stimulating, anti-cancer, anti-diabetic, hypolipidemic, neuroprotective, pulmonary-protective, cardioprotective, wound-healing, antimicrobial, and skin-healing properties.
DiscussionThe resin comprises a complex mixture of volatile oils, terpenoid constituents, minerals, amino acids, polysaccharides, and steroidal derivatives. Safety studies on guggulu have identified specific contraindications and drug interactions, particularly with blood thinners, hypolipidemic agents, and cardiovascular medications. However, the safety profile of guggulu remains limited regarding dosing and clinical studies in pregnant women.
ConclusionGuggulu from Commiphora wightii shows significant pharmacological potential, especially in inflammatory, metabolic, and cardiovascular disorders. While its traditional use is well-documented, more clinical studies are needed to confirm its safety, efficacy, and to establish standardized dosing for broader therapeutic use.
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Phytomolecules, Pharmacology, and Medicinal Values of the Butea Monosperma (Palash) Flower
Authors: Ishu Garg, Shivani Rawat, Urmi Chaurasia and Veerma RamAvailable online: 21 August 2025More LessIntroductionButea monosperma, or Palash or Flame of the Forest, is a plant with medicinal versatility. Every morphological structure of the plant has a unique medicinal value. The stems, bark, roots, leaves, and flowers all contain distinct compositions of phytoconstituents with varying pharmacological activities and medicinal uses. The flowers of Butea monosperma, commonly known as “tesu ka phool” or “palash flowers,” possess many unambiguous phytoconstituents with superior medicinal values. The flowers consist of numerous phytoconstituents, among which Butrin, Isobutrin, Butein, Formononetin, Isoliquiritigenin, Liquiritigenin, and Flavone glycoside are the most prominent.
MethodsReview articles and research papers from reputable journals regarding Butea monosperma flowers have been thoroughly analyzed. Extensive readings and discussions were conducted to summarize researchers' findings concerning the pharmacology and medicinal properties of the phytoconstituents present in palash flowers.
ResultsThis review examines various types of research that discuss the ethnomedicinal uses of Butea monosperma flowers. Additionally, the pharmacology and medical applications of its phytoconstituents are addressed. Furthermore, the chemical structures and classifications of the phytoconstituents are examined.
DiscussionAmong several phytoconstituents, Butrin, Isobutrin, Butein, Formononetin, Isoliquiritigenin, Liquiritigenin, and Flavone glycoside were prominently studied, highlighting the medicinal values of the palash flowers. Various researchers have concluded that these phytoconstituents are responsible for the flower’s anti-inflammatory, antioxidant, anti-dopaminergic, anti-neoplastic, and antifungal activities. Despite a long list of pharmacological activities and medicinal properties, the flower has been minimally explored for treating various health issues.
ConclusionThe review examined the various active phytoconstituents of palash flowers and their associated medicinal properties. They provide benefits for ailments such as vitiligo and psoriasis, possess anti-cancer properties, exhibit neuroprotective effects, and address reproductive issues. However, the accurate interpretation of the mechanism of the plash flower extract and its phytoconstituents is limited by the absence of pharmacokinetic and pharmacodynamic research. The review directs the formulation of phytopharmaceuticals.
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Liquid Chromatography-Mass Spectrometry-Guided Isolation of Bioactive Solvent Fractions Derived from Oyster (Magallana Bilineata) Powder Residue
Available online: 11 August 2025More LessIntroductionThe slipper-shaped oyster Magallana bilineata, a species commonly farmed in the Philippines, is being processed into oyster extract powder, a shelf-stable product that can be easily incorporated into various food applications. Oyster powder residue, a by-product of oyster extract processing, is rich in essential amino acids and proteins. Our innovative study, which is the first of its kind, focuses on the potential bioactivity of M. bilineata residue, a promising novel metabolite source with significant biomedical applications.
MethodsOur approach, which included solvent extraction, fractionation by octadecylsilyl (ODS) column chromatography, and liquid chromatography-mass spectrometry (LC-MS)-guided profiling of the active fractions, was meticulously designed to be robust and reliable. The crude and active fractions, including those with antimicrobial, antioxidant, and cytotoxic activities, were rigorously studied in bioactivity assays, further ensuring the reliability of our findings.
ResultsThe results indicated that the solvent fractions of oyster M. bilineata residue may contain several bioactive compounds, such as alkaloids, terpenoids, peptides, and cytotoxic macrolides, which are responsible for their notable biological activities. The 80% methanol fraction exhibited better anticancer activity against MCF-7 human breast cancer cells, with an IC50 value of 58.77 ± 1.26 µg/mL, compared to the positive control, cisplatin (97.56 ± 0.31 µg/mL). Moreover, the fractions also exhibited strong antibacterial activities against some pathogenic microorganisms and showed scavenging activity against the diphenyl-1-picrylhydrazyl (DPPH) radical.
DiscussionThe significant bioactive characteristics exhibited by the methanol fractions may be due to the existence and availability of the essential chemical components within each fraction. Oysters, as filter feeders, can accumulate bioactive compounds from their environment as they actively filter water by absorbing and concentrating a variety of substances, including biologically active ones.
ConclusionOur study has demonstrated the competency of LC-MS profiling in conjunction with bioassays in identifying bioactive components in oyster powder residue. This approach offers a reliable and promising perspective on utilizing waste from oyster processing as a rich and untapped source of bioactive compounds with significant pharmaceutical potential, opening new avenues for research and application.
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Identification of Leukemia Enzyme Inhibitors by Molecular Modeling and Machine Learning Approaches
Available online: 07 August 2025More LessIntroductionAcute Myeloid Leukemia (AML) is characterized by uncontrolled proliferation of aberrant white blood cells, contributing to high morbidity and mortality rates, particularly among males. Targeting key enzymes involved in AML progression represents a promising therapeutic strategy.
MethodsThis study applied computational drug discovery techniques to identify potential AML inhibitors targeting Tyrosine Kinase (TK), Protein Kinase C Beta (PKC), Myeloid Cell Leukemia 1 (MCL-1), and Histone Acetyltransferase (HAT). Inhibitors were retrieved from the ChEMBL database, molecular descriptors computed using PaDEL, and machine learning models evaluated via LazyPredict. QSAR modeling with a Random Forest Regressor achieved >90% accuracy in predicting pIC50 values. Lead compounds underwent molecular docking (PyRx), ADMET profiling (ADMETlab2.0), and molecular dynamics simulations (NMSim) to assess binding affinity, pharmacokinetics, and stability.
ResultsThe QSAR model showed a strong correlation between predicted and experimental pIC50 values. Docking studies and ADMET analysis identified a novel compound with favorable pharmacokinetic properties and strong inhibitory potential. MD simulations confirmed stable binding conformations within target enzymes.
DiscussionThe integration of QSAR modeling, docking, and ADMET screening efficiently identified promising AML enzyme inhibitors, demonstrating the value of computational pipelines in early-stage drug discovery.
ConclusionThis study highlights a novel lead compound with potential as a multi-target AML therapeutic candidate, warranting further in vitro and in vivo validation.
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Incredible Facts about the Potential Role of Tinospora cardifolia as Medicinal Use: A Review
Authors: Saurabh Kumar Chhonker, Alka Gupta and Akhil Pratap SinghAvailable online: 28 July 2025More LessIntroductionIndia glorifies an extensive array of plant species, many of which have been employed for medicinal purposes since ancient times, owing to the country's rich diversity of natural resources and remedies. Tinospora cordifolia, commonly known as Guduchi or Giloy, possesses several constituents, including flavonoids, alkaloids, steroids, glycosides and terpenes, which contribute to its pharmacological properties and therapeutic benefits. Furthermore, in contrast to other pharmaceuticals and allopathic treatments, these medicines are recognized for their distinctive characteristics, which include minimal side effects and a lack of toxicity.
ObjectiveThe goal of this review is to raise awareness and share more information, the pharmacological importance and benefits of giloy in humans to safeguard various health issues.
MethodsOur research involved a comprehensive exploration, reviewing and systematize significant information from the published literature and scientific databases.
ResultsThe improvement of human life reliance is achieved by utilizing T. cordifolia in therapeutics to improve metabolic, endocrine and other ailments. The current review is a description of the therapeutic employments of T. cordifolia against various types of disorders. It acts as an anti-HIV, anti-microbial agent, anti-diarrheal, anti-cancer, anti-oxidant, anti-hyperglycaemic, hepatoprotective and as cardiovascular protective, neuroprotective and so on.
ConclusionThe present review highlights the pharmacological importance of T. cordifolia viz anticancer anti-HIV potential, immunomodulatory activity, antitoxic effects, Parkinson's disease, antimicrobial activity, antioxidant activity and hepatic disorder. The information given would be helpful for researchers, healthcare professionals, and Pharmaceutical companies in the design and development of effective medications, drugs, and healthcare products that influence the diverse and specific mode of action of T. cordifolia. Additionally, it would assist in the promotion and popularization of this valuable herb, which holds significant potential for the prevention and treatment of various health conditions. It may be an incredible opportunity for anticipation and treatment of different illnesses by using T. cordifolia.
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Therapeutic Potential of the Plants Ailanthus Excelsus, Allium Sativum, and Cymbopogon Flexuosus in the Treatment of Hyperlipidemia and Oxidative Stress: An Overview
Authors: Ankur Agrawal, Subodh Dubey and Shikha SharmaAvailable online: 17 July 2025More LessCardiovascular disease (CVDs) has a major effect on global mortality rates. Increased blood lipids have been associated with the development of cardiovascular disease, which is an urgent health issue. Controlling blood lipid levels can reduce the risk of cardiovascular disease. Hyperlipidemia is a group of genetic and acquired disorders that cause high levels of lipids in the body. The condition is characterized by an abnormal increase in blood lipid levels, including cholesterol and triglycerides. Statins are commonly used to treat hyperlipidemia. Constraints exist in the utilization of these therapies, notwithstanding their efficacy. Statin therapy may face treatment resistance, leading to poor responses in some patients. Medication discontinuation may result from intolerance caused by adverse effects. The study indicates that boosting antioxidant levels in individuals with elevated lipid levels could potentially aid in halting disease progression. The study emphasizes the significance of maintaining a proper equilibrium of antioxidants in the body to avoid the development of hyperlipidemia. An inherent mechanism in the body counters oxidative damage to plasma lipoproteins. Oxidative stress can occur due to alterations in system activity or ROS generation. Cellular dysfunction and health problems can be caused by ROS. Achieving equilibrium between oxidants and antioxidants is essential for mitigating health hazards associated with oxidative stress. Plants with medicinal properties have been effective, well-tolerated, and economically valuable in treating various ailments. Studies suggest that medicinal plants may have comparable effectiveness to traditional medications, with fewer negative side effects. Natural options have the potential to manage dyslipidemia and oxidative stress.
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