Natural products play a crucial role in drug discovery, whether as drugs, lead compounds, or cytotoxic payloads of antibody-drug conjugates. Cyclohexadepsipeptides, a class of microbial secondary metabolites, are primarily synthesized by nonribosomal peptide synthetases. They consist of a six-moiety macrocycle with alternating amide and ester bonds between amino acid and hydroxy acid moieties. Notably, compared to their bacterial counterparts, cyclohexadepsipeptides exhibit greater diversity in non-proteinogenic amino acids and more complex post-translational modifications, resulting in richer chemical structures and bioactivities. This review adopts a structure-based classification system, categorizing known fungal-derived cyclohexadepsipeptides into three types according to the number of hydroxy acid moieties (one to three). This study summarizes the source organisms, extraction conditions, and bioactivities of these natural compounds. Analysis reveals that cyclohexadepsipeptides with five amino acids and one hydroxy acid are primarily isolated from marine fungi and most commonly exhibit insecticidal activity, while those cyclohexadepsipeptides with three amino acids and three hydroxy acids are primarily isolated from entomopathogenic or plant endophytic fungi and mainly display anticancer properties. Ethyl acetate, ethanol, and methanol is the most frequently employed extraction solvents. Furthermore, the study attempts to analyze the structure-activity relationships of these natural products. It is not difficult to find that the quantity and arrangement of hydroxy acid moieties in cyclohexadepsipeptides directly affect the bioactivities of these compounds, and the length and type of side chains outside the ring also have an impact on the maintenance of their bioactivities. It is hoped that this work will provide a valuable reference for the application of this type of natural compound in drug discovery.
Introduction: Paracetamol is the most common cause of drug- induced liver injury, which is associated with oxidative stress, cytokine release, and apoptosis. Boswellic acid (BA), with anti- inflammatory and antioxidant effects, can ameliorate liver injury but has poor solubility and bioavailability. The objective of this study was to design boswellic acid nanoparticles (BA-NPs) and test their protective effect against paracetamol-induced liver injury in mice. Methods: BA-NPs were prepared by a surfactant-assisted emulsion method and characterized by UV-Vis spectroscopy, FT-IR analysis, dynamic light scattering (DLS), zeta potential measurements, and transmission electron microscopy (TEM). Acute oral toxicity (LD₂⁽) was assessed in healthy mice. Liver- intoxicated mice were treated with paracetamol (1 g/kg, po) and pretreated for 14 days with BA- NPs (75 mg/kg, po) or silymarin (50 mg/kg). Measurements included serum liver enzymes (ALT, AST, and ALP), lipid profile markers (TC, TG, and HDL), oxidative stress indicators (GSH, CAT, GPx, SOD, and MDA), inflammatory cytokines and their markers (IL- 6 and TNF–α), the apoptotic marker p 53, caspase- 8 and STAT 3 mRNA expression measured by qPCR, and molecular docking simulations to predict boswellic acid's binding affinity to target proteins. Results: The formulated BA- NPs were spherical and monodisperse (54. 54.54 ± 2. 76 nm) with colloidal stability (zeta potential:- 18. 84 mV; PDI: 0. 26). The LD50 was estimated to be 1500 mg/kg, indicating relatively low acute toxicity. BA-NP pretreatment alleviated paracetamolinduced increases in ALT, AST, and ALP; normalized dyslipidemia; restored antioxidant activity; and decreased MDA levels. We observed that the levels of pro- inflammatory cytokines (IL- 6, TNF- α) and p 53 were strongly downregulated. The expression of both caspase-8 and STAT3 was also downregulated by BA-NPs. Molecular docking data showed that boswellic acid bound significantly to caspase-8 (ΔG = -7.97 kcal/mol) and STAT3 (ΔG = -7.95 kcal/mol), supporting its mechanism of hepatoprotection. Discussion: Our results indicate that BA- NPs prepared by Span 60/Tween 80 emulsification provide potent hepatoprotection against paracetamol- induced liver injury through synergistic, multi- mechanistic action, significantly protecting against hepatic injury by concurrently suppressing oxidative stress, inflammatory signaling pathways, and apoptosis, three interconnected molecular events critical to the pathogenesis of paracetamol hepatotoxicity. Conclusion: BA-NPs prepared via emulsification of Span 60/Tween 80 offer potent hepatoprotection against paracetamol-induced liver injury by primarily modulating oxidative stress, inflammation, and apoptosis. This approach not only highlights a potentially novel therapeutic for drug- induced hepatotoxicity but also overcomes the pharmacokinetic barriers of the native boswellic acid agent and provides an improved alternative to currently available drugs.
Background: Curculigo latifolia is a valuable natural resource in Brunei Darussalam with high phytochemical potential and ethnobotanical importance. Methods: The present study investigates the antioxidant activity of C. latifolia Leaves (CL) and C. latifolia Roots (CR) ethanolic extracts using the Oxygen Radical Absorbance Capacity (ORAC) chemical assay and on hydrogen peroxide (H2O2)-induced human keratinocyte (Ha- CaT) cells. The anticancer activity was tested against human colon (HT-29/CD63_nluc) and Pancreatic (PANC-1) cancer cell lines. Gas Chromatography-Mass Spectrometry (GC-MS) was used to identify chemical compounds. Results and Discussion: The GC-MS analysis identified phytol, γ-Tocopherol, vitamin E, and stigmasterol in the extracts. Antioxidant activity of CL and CR extracts evaluated using the ORAC assay was minimal, with values at 28.80 μmol Trolox Equivalent (TE)/L and 25.84 μmol TE/L, respectively, compared to the positive control, ascorbic acid, which reached 97.1 μmol TE/L. Additionally, in H2O2-induced HaCaT cells, pre-treatment with the extracts did not provide significant cellular protection. Moreover, the CL and CR extracts did not exhibit anticancer activities against HT-29/CD63_nluc and PANC-1 cancer cell lines under the conditions tested. Conclusion: CL and CR extracts exhibited promising antioxidant activity via electron donation, but showed limited cytoprotective and anticancer effects, with CR showing a potential response to anti-austerity conditions.
Background: XieRiGa-4 (XRG-4) is a widely used formulation in Mongolian medicine for the treatment of kidney dysfunction, yet its active constituents and underlying mechanisms of action remain poorly characterized. This study aims to identify active constituents, key targets, and potential pharmacological mechanisms of XRG-4 in protecting against kidney injury using network pharmacology, molecular docking, and in vivo and in vitro validation. Methods: A rat kidney injury model was established by pylorus ligation to evaluate XRG-4 efficacy. Active components of XRG-4 were characterized by liquid chromatography-mass spectrometry (LCMS), and candidate targets were obtained from public databases. Network pharmacology analyses, including protein-protein interaction (PPI), Gene Ontology (GO), and Kyoto Encyclopedia of Genes and Genomes (KEGG) analyses, were conducted to identify core bioactive components, potential targets, and signaling pathways. Molecular docking assessed binding affinities between active compounds and core targets, and Western blot analysis validated expression of key targets. Results: Biochemical analysis revealed that serum creatinine (CRE) and urea (URE) levels were significantly higher in the model group than in the normal group (P < 0.01) and were significantly reduced after XRG-4 treatment (P < 0.01), indicating a renal protective effect. Cell viability was markedly decreased in the model group (P < 0.01) and significantly improved in XRG-4-treated groups (P < 0.01). A total of 20 bioactive compounds, including the top 10 cationic and anionic constituents, and 253 overlapping targets associated with XRG-4 and kidney injury were identified. Network analysis indicated a central role of the EGFR signaling pathway in XRG-4 efficacy. Molecular docking revealed that five key compounds, 6- Hydroxypurine, Hymecromone, Gardenoside, Geniposide, and Phenprobamate, displayed strong binding affinities with three core targets, Slc22a5, Mrps9, and EGFR. Western blot analysis further confirmed that Slc22a5 (P < 0.05) and Mrps9 (P < 0.01) expression was significantly reduced in the model group and markedly upregulated following XRG-4 treatment. Discussion: This study confirms that Mongolian medicine XRG-4 improves renal function and alleviates kidney injury. Using network pharmacology, molecular docking, and experimental validation, its main active components were found to bind to core targets including EGFR, Slc22a5, and Mrps9, regulate the EGFR signaling pathway, and upregulate Slc22a5 and Mrps9 expression, thereby exerting a nephroprotective effect and providing a scientific basis for its clinical application. Conclusion: This study clarifies the nephroprotective effects of XRG-4 and demonstrates its capacity to attenuate kidney injury through the EGFR signaling pathway. These findings provide a scientific rationale for clinical use of XRG-4 in kidney diseases and support further development of XRG-4 as a potential nephroprotective agent in Mongolian medicine.
Introduction: Scutellaria barbata (Ban Zhi Lian) is a traditional Chinese herb commonly used for detoxification and heat-clearing. According to recent pharmacological research, it has anticancer potential. Bioactive molecules, flavonoids, diterpenoids, and polysaccharides, have been shown to control key molecular signalling pathways, such as PI3K/AKT, NF-κB, and TGF-β/Smad, to manage tumour growth, survival, and metastasis. Methodology: The review combines ethnopharmacological, phytochemical, and preclinical and clinical data on the anticancer activity of Scutellaria barbata. A literature search identified 246 studies, out of which 40 articles qualified as per the PRISMA guidelines. Systems biology and network pharmacology methods were also applied to determine the multitarget effects of the traditional Chinese medicine concepts and the current pharmacology. Results: Phytochemicals of Scutellaria barbata induce apoptosis by regulating Bax/Bcl-2 and activating caspase, preventing angiogenesis, and decreasing multidrug resistance by inhibiting the ABCG2 transporter. In vitro research exhibits tumour-suppressive activity in lung, liver, and colorectal cancer. There is limited clinical evidence of possible synergistic efficacy when used together with conventional chemotherapy. Discussion: Considering these findings, Scutellaria barbata has the potential to be used in integrative oncology by integrating traditional Chinese medicine principles with modern pharmacological knowledge, though clinical support is not yet strong. Conclusion: Scutellaria barbata is a botanical herb used in cancer therapy, but well-designed clinical trials are needed to verify its therapeutic efficacy and safety.
Introduction: Mimosa tenuiflora (Willd.) Poir., widely known as Jurema preta in Brazil and tepezcohuite in Mexico, is a perennial shrub or tree traditionally used in folk medicine across the Caatinga biome of northeastern Brazil and other regions of Central and South America. Tryptamine is an indole alkaloid naturally found in several species, with M. tenuiflora representing an important natural source of this compound. Additionally, it has derivatives such as N-methyltryptamine and N,N-dimethyltryptamine (DMT), which share similar structural features. Methods: In the present study, phytochemical investigations were conducted on extracts obtained from different parts of M. tenuiflora, including bark, stem, leaves, and branches, with the aim of identifying and characterizing its alkaloid constituents. Indole alkaloids were isolated primarily from the bark extract using solvent partitioning and column chromatography. Structural characterization was performed employing complementary analytical techniques, including HPLC, GC/MS, ATR-FTIR, and one- and two-dimensional NMR spectroscopy (¹H and HMBC). Results and Discussion: The analyses led to the identification of several bioactive amines, notably tryptamine, N-methyltryptamine, and N,N-dimethyltryptamine. The results confirm the chemical diversity of M. tenuiflora and highlight its relevance as a natural source of pharmacologically active alkaloids. Conclusions: These findings contribute to natural product chemistry and support the bioprospecting of plant-derived compounds with potential applications in central nervous system disorders. Moreover, this study reinforces the importance of conserving biodiversity and valuing traditional knowledge associated with medicinal plants native to the Brazilian Caatinga.
Introduction: Kunxian capsule (KX) is a Traditional Chinese Medicine widely used for the treatment of rheumatoid arthritis (RA) and other inflammatory diseases. However, its anti-inflammatory mechanism was unclear. Introduction: Kunxian capsule (KX) is a Traditional Chinese Medicine widely used for the treatment of rheumatoid arthritis (RA) and other inflammatory diseases. However, its anti-inflammatory mechanism was unclear. Methods: A combination of network pharmacology, molecular docking, and a CuSO4-induced zebrafish inflammation model was used. RT-qPCR was performed to analyze gene expression related to inflammation and the MAPK/dopamine pathways. Results: Network pharmacology identified 122 intersecting targets between KX and RA, and KEGG enrichment analysis highlighted the MAPK and dopamine signaling pathways. KX alleviated inflammation in zebrafish and regulated the expression of inflammatory cytokines (cox2, ptges, il8, il1β, il6, inos, il10, tgf-β) and MAPK/dopamine pathway genes (nfκb2, ikbaα, mapk8b, mapk14a, gria2, drd1b, drd2, ppp3ca, ddc). Molecular docking demonstrated that four key components-triptolide, anhydroicaritin, epimedin B, and kaempferol-exhibited stable binding to core targets such as MAPK14 (binding energy: -8.35 kcal/mol), MAPK8 (-8.2 kcal/mol), COX2 (-8.34 kcal/mol), and DRD1B (-7.79 kcal/mol). Discussion: The study reflected the multi-component, multi-target nature of traditional Chinese medicine, and highlighted the potential of traditional Chinese medicine to treat inflammatory diseases through multiple signaling pathways. Conclusion: The present study confirmed that KX plays a therapeutic role in RA by inhibiting the inflammatory response through the MAPK/dopamine pathway in the zebrafish model.
Introduction: Lung cancer, especially Non-Small Cell Lung Carcinoma (NSCLC), is one of the deadliest malignancies globally. Current therapeutic intervention approaches often cause serious side effects and are not sufficiently effective; thus, there is a renewed academic interest in naturally bioactive compounds such as flavonoids. These phytochemicals are polyphenols that have shown significant potential in oncologic therapy due to their antioxidant, antiinflammatory, and anti-proliferative abilities. Methods: The literature review was conducted using extensive databases, including PubMed, Scopus, Web of Science, ScienceDirect, and Google Scholar. The articles chosen were those published in English over the recent years that focused on the design, synthesis, and biological evaluation of flavonoid derivatives with reference to lung cancer therapeutics. Important inclusion criteria included the studies with original data and applicability to the treatment paradigms of NSCLC. Results: Artificial flavonoid derivatives, including artificially produced chalcones, apigenin, baicalein, and triazole analogues, were all shown to have a strong cytotoxic effect on A549 lung cancer cells. These compounds were found to have low micromolar IC 50 values and exceed the effectiveness of many traditional pharmacological agents. The most effective ones triggered apoptosis, cell-cycle arrest, reduced angiogenesis, reduced inflammation, and prevented metastatic progression. Discussion: The flavonoid derivatives have an impact on various cancer-related signalling pathways, such as PI3K/Akt, NF -4, and p53. Their favourable safety profile and structural adaptability make them useful candidates for future pharmacological development. However, there are still complications in improving their pharmacokinetic properties to use them in therapeutics. Conclusion: Synthetic flavonoid derivatives hold great potential in the therapy of lung cancer. Continued research on their mechanistic insights and optimization can help to derive new anticancer therapeutics that are less harmful.
Introduction: Cystic fibrosis (CF) is a life-threatening genetic disease with high mortality rates. The most common cause of death in CF is progressive damage to the lungs, leading to respiratory failure. Currently, there are few treatments, and these are ineffective. 6- gingerol could be a natural agent that could benefit in the treatment of this disease due to its medicinal properties. Aim: In this study, a pharmacological network analysis between 6-gingerol and CF was performed to understand the therapeutic targets. Methodology: From MalaCard, DisGeNET, Traditional Chinese Medicine Systems Pharmacology Database, and Swiss Target Prediction, target genes were obtained for comparison. We obtained 14 genes and analyzed them in DAVID-Bioinformatics. Subsequently, a protein-protein interaction network was performed in STRING from which we obtained the hub genes AKT1, BCL2, TP53, IL1β, MMP9, MAPK3, PTGS2, and HSP90AA1. From the proteins related to the central genes, molecular docking studies were carried out with 6-gingerol using the SwissDock database. Results: Enrichment analysis showed that 6-gingerol is linked to apoptotic, inflammatory processes, and cell signaling. Furthermore, a molecular docking study demonstrated that 6- gingerol has high protein binding. Discussion: This study highlights the potential therapeutic role of 6-gingerol in CF based on pharmacological network and molecular docking analyses; however, the results are limited by their in silico nature and require experimental validation. Possible biases from databases and the unclear pharmacokinetic profile of 6-gingerol in CF warrant further investigation to confirm these findings. Conclusion: These findings represent computational predictions and lay the foundation for future experimental studies to validate the therapeutic power of 6-gingerol as a possible natural adjuvant therapy for CF.
Introduction: Alzheimer’s disease is a neurodegenerative disease with no treatment. Costus spectabilis (Fenzl) K. Schum is a perennial rhizomatous herb traditionally used to treat several diseases. The aim of this study was to isolate antiradical and antiacetylcholinesterase compounds from Costus spectabilis (Costaceae), and to perform a molecular docking study of the active compound. Methods: Compounds were isolated using column chromatographic technics; structures of isolated compounds were determined using spectroscopic analysis and literature data. The antiradical scavenging potential was evaluated in vitro using DPPH as a free radical. The inhibition power of acetylcholinesterase was assessed in vitro using the Ellman reagent. Results: The phytochemical investigation of the studied extract led to four compounds : β- sitosterol (1), β-sitosterol-3-O-β-D-glucopyranoside (3), sucrose (2), and Isorhamnetin-3- rutinoside-7-rhamnoside (4). The extract showed a weak antiradical scavenging potential (IC50 : 0.2160 mg/mL). Among the tested compounds, compound 4 exhibited a very good antiradical scavenging activity (IC50 of 0.0012 mg/mL). Compound 4 also exhibited a good inhibition power of acetylcholinesterase with an inhibition percentage of 89% at 0.5mg/ml; this compound was followed by the hydro-ethanolic extract with an inhibition percentage of 87% at 2 mg/mL. Compound 4 exhibits high affinity for acetylcholinesterase and butyrylcholinesterase, key enzymes associated with Alzheimer’s disease, with binding energies of -9.8 kcal/mol and -10.8 kcal/mol, respectively. discussion: the antiradical evaluation of extract and compounds was performed. Among all the tested samples, compound 4 demostrated a very good antiradical potential with an IC50 of 0.0012 mg/ml very near of the IC50 of the ascorbic acid used as reference. This compound in terms of activity is followed by compound 2 and the crude extract with IC50 of 0.1240 mg/ml and 0.2160 mg/ml respectively. This result indicates that compounds in the extract act asynergistically. Compound 4 demostrated strong AChE inhibitory activity with inhibition percentages of 89% and 87% at 0.5mg/ml and 0.01 mg/mL respectively, with a very weak (4.12 and 4.88) activity of AChE. In term of activity, this compound was followed by the hydro-ethanolic extract which also demostrated strong inhibitory activity with an inhibiton percentage of 87% at 2 mg/mL. Compound 2 was the less active sample. These experimental results align well with molecular docking studies, which indicate that compound 4 exhibits high affinity for acetylcholinesterase and butyrylcholinesterase key enzymes associated with Alzheimer’s disease with binding energies of -9.8 kcal/mol and -10.8 kcal/mol respectively. Discussion: Results obtained for the two biological activities performed showed that in the extract studied, compounds react in the asynergically maner. Conclusion: The hydro-ethanolic extract studied can be considered a good inhibitor of AChE.
Background: Esophageal Squamous Cell Carcinoma (ESCC) is the most aggressive esophageal cancer subtype, with poor therapeutic outcomes due to chemoresistance to first-line chemotherapeutic agents, including cisplatin and 5-fluorouracil (5-FU). Swertiamarin (STM), a natural iridoid glycoside, possesses various pharmacological properties, including anticancer activity, but its chemosensitizing role in ESCC remains elusive. This study aimed to investigate the chemosensitizing potential of STM on cisplatin and 5-FU in ESCC KYSE-150 cells, supported by in silico molecular docking analyses. Methods: In silico drug-likeness and toxicological profile of STM were predicted. Cytotoxicity of STM, cisplatin, and 5-FU in ESCC cells (KYSE-150), normal esophageal epithelial cells (HET-1A), and Vero cells was assessed by MTT assay. STM’s chemosensitizing potential was investigated using a pre-treatment model with its 20% Inhibitory Concentration (IC20) and halfmaximal Inhibitory Concentration (IC50) for 2, 4, and 6 hours. Molecular docking was performed to examine STM’s binding affinity and interactions with target proteins. Results and Discussion: STM revealed favorable predicted drug-likeness properties and toxicological profile, alongside selective cytotoxicity against KYSE-150 cells. Although STM pretreatment slightly increased cisplatin’s IC50, the increased cytotoxic effects over time suggest its potential chemosensitizing activity. No notable interaction was observed with 5-FU. Docking analysis revealed strong binding affinity of STM to chemoresistance-associated proteins MAPK1 (–8.774 kcal/mol), mTOR (–8.764 kcal/mol), ABCC2 (–7.949 kcal/mol), and NF-κB (- 7.914 kcal/mol), supporting potential underlying molecular mechanisms. Conclusion: Cisplatin’s improved cytotoxic pattern over time with STM pre-treatment, alongside favorable preliminary in silico analyses, warrant further investigation into STM’s potential role as a chemosensitizer in ESCC chemotherapy.
Introduction: Schoutenia ovata Korth is a plant commonly found in Thailand; however, its chemical constituents and biological activities have not been previously reported. This study was initiated to perform the first phytochemical investigation and biological screening of S. ovata stems to evaluate their therapeutic potential. Materials and Methods: The dried stems of S. ovata were extracted by sequential maceration using hexane, ethyl acetate (EtOAc), and methanol (MeOH). The resulting extracts were screened for antibacterial activity (MIC/MBC) and anti-HIV-1 Reverse Transcriptase (RT) activity using standard methods. The isolation of compounds was performed using various chromatographic techniques, and their structures were elucidated by NMR spectroscopy. Additionally, the stereochemical nature of the isolated flavonoid was investigated using single-crystal X-ray diffraction Results: Three known compounds were isolated and identified: pinostrobin, β-sitosterol, and stigmasterol. The X-ray crystallographic analysis of pinostrobin revealed a discrepancy between the refined Sisomer model and the bulk specific rotation, indicating that the compound exists as a scalemic mixture due to partial racemization. In terms of biological activity, the crude EtOAc extract exhibited antibacterial activity against S. aureus and E. coli (ETEC) with MIC/MBC values of 25/25 mg/mL for both. The MeOH extract demonstrated specific activity against E. coli (ETEC) (MIC/MBC = 6.25/6.25 mg/mL) and S. flexneri (MIC/MBC = 25/100 mg/mL). The EtOAc extract also displayed weak antiHIV-1 RT activity. Discussion: The observed antibacterial activities are likely attributed to the presence of the isolated bioactive constituents. Pinostrobin and the mixture of sterols (β-sitosterol and stigmasterol) are known to possess antibacterial properties, aligning with the activity observed in the extracts. The activity of the methanol extract suggests the presence of other polar bioactive components that warrant further investigation Conclusion: This study constitutes the first phytochemical report on S. ovata, revealing that its stems are a valuable source of bioactive flavonoids and triterpenoids. These findings provide a scientific basis for the ethnomedicinal potential of this plant and suggest that the spontaneous racemization of pinostrobin should be considered in future isolation processes.
Abstract: The production of Taxol, a potent anticancer agent, has undergone significant advancements in biotechnology. Originally derived from the bark of the Pacific yew tree, Taxol has proven effective in treating various cancers, including breast and ovarian cancer. However, traditional extraction methods have posed ecological and economic challenges due to low yields and harm to yew tree populations. However, extracting paclitaxel from natural sources poses significant challenges due to low yields and environmental concerns. Alternative methods, such as semi-synthesis and total synthesis, have been explored but face economic and practical limitations. The development of paclitaxel has undergone significant milestones since its discovery in the 1960s. Despite initial success, the market for this anticancer agent has experienced fluctuations, prompting ongoing research into more sustainable production methods and formulations. Recent breakthroughs in biotechnology offer alternative approaches to Taxol production. Plant cell and suspension cultures aim to enhance production sustainably, mitigate environmental concerns, and deliver a more consistent, economically viable supply.
The rapid emergence of drug-resistant Mycobacterium tuberculosis and other bacterial pathogens has significantly reduced the effectiveness of conventional antimicrobial therapies. Single-target antibiotics are particularly vulnerable to resistance due to mutations, efflux mechanisms, and metabolic adaptation. This review highlights plant-derived secondary metabolites as promising multitarget antimicrobial agents that simultaneously disrupt key bacterial processes, including DNA replication, cell wall biosynthesis, energy metabolism, and virulence regulation. Evidence from experimental and computational studies demonstrates that major phytochemical classes, alkaloids, flavonoids, terpenoids, and phenolics, exhibit multitarget activity by inhibiting DNA gyrase, suppressing efflux pumps, disrupting membrane integrity, and inducing redox imbalance. Notably, compounds such as berberine, quercetin, curcumin, and thymol have been shown to enhance intracellular drug accumulation, inhibit biofilm formation, and restore antibiotic sensitivity in drug-resistant strains. Computational approaches, including molecular docking, molecular dynamics simulations, network pharmacology, and the Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) profiling, further support these findings by revealing strong binding affinities, stable ligand–target interactions, and favorable pharmacokinetic properties of selected phytochemicals against critical M. tuberculosis targets such as Enoyl-ACP reductase (InhA) and Decaprenylphosphoryl-β-D-ribose 2′-epimerase 1 (DprE1). Thus, these findings demonstrate that plant-derived multitarget inhibitors not only interfere with multiple essential and adaptive bacterial pathways but also reduce the likelihood of resistance development. This positions them as promising candidates for next-generation anti-infective therapies and adjuncts to existing treatment regimens.
Phytochemicals produced from plants have emerged as potential therapeutic candidates for regulating skeletal metabolism. This review presents a dualistic character of phytochemicals used in skeletal health, which can be a friend (beneficial) or a foe (harmful) of the bone mass. Anti-resorptive and osteoanabolic effects of bone-supportive phytochemicals (flavonoids, carotenoids, polyphenols, terpenoids, alkaloids, and polysaccharides) occur via multiple pathways, including the wingless-related integration site/ beta-catenin pathway, bone morphogenetic protein/SMAD (Sma and Mad related) protein pathway, and inhibition of receptor activator of nuclear factor kappa B ligand-mediated osteoclastogenesis, and regulation of oxidative stress and inflammation. The therapeutic efficacy of phytochemicals is supported by available preclinical and clinical data, specifically in postmenopausal osteoporosis. On the other hand, there are some phytochemicals that cause alteration in bone cell activity, which may block the availability of mineral and some may also result in decreased bone mass with long-term overconsumption. Nevertheless, to translate positive and negative outcomes into clinical practice is not yet an easy task because of poor standardization of botanical extracts, active compounds content variability, lack of bioavailability and pharmacokinetic information, and long-term safety assessment. In addition, the majority of clinical trials are based on surrogate endpoints, including bone turnover markers instead of the fractured outcome, and animal models are not always predictive of human reactions. Further characterization of phytochemicals into actual therapeutic and non-therapeutic nutrients will require standardization of phytochemicals, while studying their pharmacokinetic and toxicological profiles, after which doses can be optimized, on the basis of which structured trials with bone endpoints may help support the actual potential of the phytochemicals in bone health. This phytochemical dichotomy should be thoroughly understood in order to come up with safe and evidence-based, plant-based approaches to prevent osteoporosis and maintain bone health.
Background:: Inflammatory Bowel Diseases (IBD) are chronic inflammatory conditions of the intestine, including Crohn’s disease, which can affect any part of the gastrointestinal tract, and ulcerative colitis. Their etiology remains unknown, and their pathogenesis is complex and multifactorial, involving immune dysregulation, genetic and environmental factors, and alterations in the gut microbiota. Matricaria pubescens, categorized as a member of the Asteraceae taxonomic classification, has been used for a long time in traditional medicine for the treatment of various ailments, including inflammation and gastric disorders. The plant contains alkaloids with antibacterial, anti-inflammatory, and antioxidant effects. This research aims to evaluate the intestinal anti-inflammatory properties of the alkaloid extract derived from Matricaria pubescens (AMP) using a murine model of colitis induced by 2,4-dinitrobenzenesulfonic acid (DNBS). Methods:: Female BALB/c mice with colitis received an intrarectal injection of DNBS in 50% ethanol (v/v). Both AMP extract at doses of 25, 50, and 100 mg/kg and dexamethasone (2.4 mg/kg) were administered via oral gavage. Colon tissues were isolated to assess the development of the disease using Hematoxylin and Eosin (H&E) and Periodic Acid-Schiff (PAS) staining. In addition, biochemical markers were measured in colon samples, including Malondialdehyde (MDA), reduced Glutathione (GSH), and Myeloperoxidase Activity (MPO). Results:: Our results demonstrated that the AMP extract significantly reduced macroscopic colonic damage by 44–76% and microscopic lesion scores by 26–68% in a dose-dependent manner (p < 0.001), indicating restoration of tissue cytoarchitecture and improved mucosal integrity. The extract also significantly decreased MPO activity and MDA levels and increased GSH levels in a dose-dependent manner in colonic tissues; all changes were statistically significant (p <001). Discussion:: These results demonstrate that AMP reduces oxidative stress and neutrophil infiltration in the colon, which reinforces its potential as an intestinal protective agent. Conclusion:: Our results revealed that AMP exhibits intestinal anti-inflammatory and antioxidant properties, which suggest that AMP can be used to prevent inflammatory and oxidant conditions.
Introduction: Nuts are a rich source of vitamins, minerals, and calories, and they possess numerous health benefits. However, there are very few studies examining the correlation of the phytoconstituents of nut oils with their therapeutic and cosmetic uses. The current manuscript aims to present a systematic review that evaluates the relationship between the phytoconstituents of nut oils and their potential in pharmacology and cosmeceuticals. Methods: The author conducted scholarly searches on Google Scholar, PubMed, ScienceDirect (Elsevier), IngentaConnect, and Medline to obtain peer-reviewed research on nut oils and included all papers addressing nut oils that have therapeutic and cosmetic advantages. Results: The outcome of the systematic search led to an appraisal explaining the association between the components and pharmaco-cosmeceutical advantages of 23 distinct nut oils such as Argania spinosa, Pinus koraiensis, Arachis hypogaea, Jatropha curcas, and Pistacia vera. Discussion: Nut oils, rich in bioactive components like MUFAs, PUFAs, phytosterols, vitamin E, phenolic compounds, squalene, and lignans, have medicinal properties including cholesterol reduction, cardiovascular health promotion, immune system strengthening, and antioxidant activity. In personal care products, nut oils have long been prized for their ability to nourish, moisturize, and repair damaged skin. Conclusion: Owing to the presence of these incredible components, nut oils have remarkable pharmaco-cosmeceutical qualities. Continued research and development efforts will be essential to unlocking the full potential of nut oils and maximizing their benefits for human wellbeing and the environment.
Cancer remains one of the leading causes of mortality worldwide, mainly due to its capacity to evade apoptosis, a tightly regulated process essential for maintaining cellular homeostasis. The dysregulation of apoptotic pathways, involving key molecular regulators such as caspases, Bcl-2 family proteins, and inhibitor of apoptosis proteins (IAPs), contributes to cancer progression and therapeutic resistance. This review provides a comprehensive overview of apoptosis's intrinsic (mitochondrial) and extrinsic (death receptor-mediated) pathways, distinguishing them from necrotic cell death and highlighting their roles in tumour suppression. Amid growing interest in alternative and adjunctive therapies, medicinal plants have emerged as a rich source of bioactive compounds capable of selectively modulating apoptosis in cancer cells. We explore the therapeutic potential of phytochemicals, including alkaloids, flavonoids, terpenoids, and phenolics that exhibit pro-apoptotic activity across diverse cancer models. Special attention is given to the synergistic effects of plant-derived compounds in crude extracts and their combinatorial use with conventional chemotherapeutics, which may enhance efficacy and reduce toxicity. By integrating mechanistic insights with preclinical findings, this review underscores the strategic promise of plant-based agents in modern oncology. Incorporating natural products into cancer therapy represents a novel and rational therapeutic approach. We also address challenges such as compound standardization, bioavailability, and mechanistic validation, while proposing future directions for research to unlock the full potential of phytotherapy in precision cancer medicine.
Introduction: The rapidly growing evergreen trees of the genus Gmelina, a member of the Lamiaceae family, are important plantation species in many tropical regions worldwide. Since ancient times, medicinal plants of this genus have been prized for their therapeutic uses. This review compiles the traditional applications, phytochemical properties, and pharmacological potential of the genus Gmelina. Method: All relevant publications from 2000 to 2024 were considered. Using a variety of pertinent keywords, articles were identified through databases including Google Scholar, PubChem, ChemSpider, PubMed, Elsevier, Wiley, Web of Science, and ResearchGate. Results: This review summarises the literature on traditional knowledge, phytochemistry, and pharmacological activity of Gmelina. Gmelina arborea (Gambhari) is an important component of Dashamula. Its edible fruits have historically been associated with aphrodisiac, memoryenhancing, and rejuvenating properties. Discussion: This review categorizes phytochemicals from various parts of the plant into flavonoids, terpenoids, cyclic fatty acids, phenolic acids, glucosides, polysaccharides, esters, and glycosides. The pharmacological activities reported include antioxidant, anticancer, antimicrobial, neurotropic, anti-inflammatory, antiarthritic, antidiabetic, cardioprotective, hepatoprotective, and other effects. In addition, the review compiles ethnopharmacological information, botanical distribution, and taxonomy of the genus. Conclusion: Phytochemicals from Gmelina species exhibit numerous pharmacological effects, supporting their traditional and ethnobotanical uses. However, many species remain unexplored, and only a few studies have demonstrated the pharmacological efficacy of specific active compounds extracted from these plants. Further research is needed to fully realize their therapeutic potential.
