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  • Research Article
  • 10.1007/s00210-026-05492-6
Calcium hydroxide nanoparticles-induced oxidative stress and mitochondrial impairment drive genomic instability and programmed cell death in colorectal cancer cells.
  • Jun 4, 2026
  • Naunyn-Schmiedeberg's archives of pharmacology
  • Hanan R H Mohamed + 7 more

The high aggressiveness, metastatic potential, and mortality of colorectal cancer, together with the limitations of conventional chemotherapy, highlight the urgent need for safer and more effective therapeutic alternatives. Nanotherapies offer promising advantages through improved bioavailability and tumor targeting. In particular, calcium hydroxide nanoparticles (Ca(OH)2NPs) possess unique physicochemical properties, yet their anticancer potential in colorectal cancer remains fully unexplored. This study was consequently undertaken to estimate the cytotoxic effects and underlying molecular mechanisms of Ca(OH)2NPs in human colorectal HCT-116 cancer cells, while also exploring their impact on the viability of normal human HFB4 melanocytes. Normal HFB4 and cancerous HCT-116 cells were exposed to serial two-fold concentrations of Ca(OH)2NPs ranging from 7.80 to 1000 mg/ml for 72 h, and cell viability was assessed using the MTT assay. Intracellular reactive oxygen species (ROS) generation and mitochondrial membrane potential were measured using 2',7'-dichlorodihydrofluorescein diacetate (DCFH-DA) and rhodamine-123 staining, respectively. Genomic DNA damage was evaluated by the alkaline comet assay, whereas apoptosis induction was analyzed using DAPI staining and the chromatin diffusion assay. The expression levels of mitochondria- and apoptosis-related genes were quantified by quantitative real-time PCR (qRT-PCR). Results of the MTT assay demonstrated that Ca(OH)2NPs exerted significant, dose-dependent cytotoxicity on colorectal HCT-116 cancer cells, as evidenced by a markedly low IC50 value of 35.04 µg/ml and a substantial reduction in cell viability. In contrast, the viability of normal HFB4 melanocytes was only slightly affected, and only at the highest Ca(OH)2NPs concentration tested, as indicated by a comparatively high IC50 value of 190.80 µg/ml. The resulting selectivity index of 5.44 further supports the notable cytotoxicity of Ca(OH)2NPs toward HCT-116 colorectal cancer cells. Furthermore, treatment of HCT-116 cells with Ca(OH)2NPs at the IC50 concentration (35.04 µg/ml) led to a significant increase in intracellular ROS generation level, dramatic loss of mitochondrial membrane potential, and pronounced oxidative DNA damage, ultimately culminating in apoptotic cell death. qRT-PCR analysis also demonstrated significant downregulation of both the apoptotic p53 and the anti-apoptotic Bcl-2 gene expression, alongside significant upregulation of the mitochondrial ND3 gene expression. These molecular alterations support the involvement of mitochondrial dysfunction and apoptosis-related gene modulation in the observed Ca(OH)2NPs-induced cytotoxic effects. Conclusion: Ca(OH)2NPs demonstrate notable anticancer activity against human colorectal HCT-116 cancer cells, primarily through ROS-mediated oxidative stress, genomic DNA damage, mitochondrial dysfunction, and apoptosis induction. These findings highlight Ca(OH)2NPs as a potent nanotherapeutic candidate for colorectal cancer management. However, the current study was limited to in vitro experimental conditions, and the precise molecular mechanisms underlying these effects remain incompletely understood. Therefore, further mechanistic investigations, advanced in vitro and in vivo studies, and comprehensive biocompatibility and safety evaluations are required to validate their therapeutic potential and clinical applicability.

  • Research Article
  • 10.1016/j.bioorg.2026.109647
Repurposing amide-based drugs unveils inhibition mechanisms of plasmodium falciparum Plasmepsin V enzymatic activity for antimalarial therapy.
  • Jun 1, 2026
  • Bioorganic chemistry
  • Anitadevi K Prajapati + 3 more

Repurposing amide-based drugs unveils inhibition mechanisms of plasmodium falciparum Plasmepsin V enzymatic activity for antimalarial therapy.

  • Research Article
  • 10.2174/0118715206453560260313042524
Bioactive Constituents and Potential Cytotoxic Activities of Green Microalgae: Desmodesmus spp. from a Jordanian Isolate.
  • May 20, 2026
  • Anti-cancer agents in medicinal chemistry
  • Lidia K Al-Halaseh + 5 more

Conventional anticancer agents have numerous limitations, and developing innovative agents to treat cancer places a heavy burden on the global health economy. The current study aims to explore sustainable and alternative sources for cancer therapy. This study aims to investigate the phytoconstituents and biologically active compounds in green microalgae and to explore their potential cytotoxicity. Algae were isolated from a Jordanian aquatic region, purified, and identified based on the 18S rRNA and Internal Transcribed Spacer (ITS) DNA markers. The lyophilized biomass was extracted by maceration and ultrasonication-assisted shaking, and then the phytoconstituents were identified via HPLC/MS-MS. Cytotoxicity and cell viability assays were performed to evaluate the cytotoxicity of the algal crude extract against normal Human Umbilical Vein Endothelial cell line EA (HUVEC; cat. no. CRL-1730; ATCC), grade IV Prostatic Adenocarcinoma cell line PC3 (CRL-1435), and Human Pancreatic Ductal Adenocarcinoma cell line (PANC1, CRL-1469). The results revealed the presence of several biologically active compounds in the algal aqueous extract, such as fatty acids, amino acids, nucleic acids, terpenoids, coumarins, flavonoids, and polyphenols such as scopoletin, gingerol, and tanacetol. The MTT assays revealed a biocompatibility of the natural remedy with the normal cell line HUVEC, and a dose-related response pattern was observed against cancerous Pancreatic and Prostatic Adenocarcinoma cell lines. The computed IC50 for Pancreatic, Prostatic, and Normal Epithelial cells was 47.7, 56.3, and 217.5 mg/mL, respectively. The richness of bioactive compounds that are classified into diverse secondary metabolite families indicates their potential biological and pharmacological activities. The MTT assay results indicate selective cytotoxicity of the extract against Prostatic and Pancreatic cancer cell lines, with the latter showing more sensitivity to the treatment. The high IC50 values of the normal epithelial cell line express its resistance; therefore, the treatment is biocompatible. Green microalgae, with their bioactive components, could be a promising approach for a sustainable, innovative therapy for Prostatic and Pancreatic cancers; further, advanced research is highly recommended.

  • Research Article
  • 10.1016/j.isci.2026.115546
Functionalized boron nitride nanomaterials: Exploring antioxidant and antitumor activities for advanced therapeutic applications.
  • May 1, 2026
  • iScience
  • Jialin Zang + 6 more

Functionalized boron nitride nanomaterials: Exploring antioxidant and antitumor activities for advanced therapeutic applications.

  • Research Article
  • 10.3390/foods15091480
Mechanistic Insights into Pancreatic Lipase Inhibition by Sugarcane Polyphenols: A Structural and Kinetic Study
  • Apr 23, 2026
  • Foods
  • Qiyan Liu + 3 more

Pancreatic lipase (PL) inhibition is a promising dietary strategy for obesity management. In this study, the inhibitory mechanisms and structural basis of polyphenols extracted from different sugarcane fractions were investigated using in vitro enzyme assays, spectroscopy, and molecular docking analyses. PL inhibitory activity was evaluated using p-nitrophenyl laurate (pNPL) as the substrate, with all assays performed in triplicate and results statistically analyzed. Among the extracts, sugarcane peel polyphenols (SP) exhibited the strongest inhibition, with a half-maximal inhibitory concentration (IC50) of 31.56 mg/mL, significantly lower than that of sugarcane juice polyphenols (SJ, 55.86 mg/mL) and sugarcane bagasse polyphenols (SB, 65.31 mg/mL). Enzyme kinetic analyses revealed a reversible mixed-type inhibition mechanism. In contrast to crude extracts, individual phenolic monomers showed substantially lower IC50 values (0.13–1.33 mg/mL), highlighting the intrinsic dilution. Compositional analysis identified ferulic acid, gallic acid, chlorogenic acid, and schaftoside as key contributors to PL inhibition. Fourier transform infrared (FTIR) and fluorescence spectroscopy demonstrated that polyphenols altered PL secondary structure by modulating α-helix and β-sheet contents and perturbed the microenvironment of tryptophan (Trp) and tyrosine (Tyr) residues. Molecular docking further indicated that these compounds bind within or near the substrate-binding channel via hydrogen bonding and hydrophobic interactions, engaging critical residues including Ser152, His263, and Phe77, and potentially influencing conformational elements involved in active-site accessibility. Collectively, these results suggest that sugarcane, particularly its peel, represents a valuable natural source of PL inhibitors. Despite the relatively high IC50 values of crude extracts, their inhibitory activity arises from multicomponent contributions and supports their potential application as dietary modulators of fat digestion rather than as pharmaceutical lipase inhibitors.

  • Research Article
  • 10.1002/fsn3.71800
Polyphenolic Diversity, Antioxidant Activity, and Anticancer Potential of Celtis australis L. Fruits: New Insights.
  • Apr 1, 2026
  • Food science & nutrition
  • Jihane Touhtouh + 9 more

Celtis australis L. was selected for investigation due to its traditional medicinal use and the limited number of studies available, particularly concerning its anticancer potential. This study examined the phenolic composition, the antioxidant activity, and the anticancer effects of methanolic, ethanolic, and aqueous extracts of C. australis L. The invitro cytotoxic efficacy was assessed with the MTT assay on six tumor cell lines (HeLa, MV4-11, OCI-AML3, DAOY, OSN-76, and U-138-MG) and two non-cancerous cell lines (HEK293T and hCMEC/D3). C. australis L. extracts exhibited moderate antioxidant activity, as evidenced by their high IC50 values (110-436 μg/mL). The FRAP reducing power was low (2.09-6.24 mg AAE/g), and the aqueous extract was least active, with IC50 values ranging from 152 to 207 μg/mL in the ABTS assay. The HPLC-ESI-MS/MS analysis indicated that the extracts contain a variety of phenolic compounds dominated by neochlorogenic acid, chlorogenic acid, procyanidin B2, (-)-epicatechin, isoquercitrin, rutin, phloretin, and delphindin-3,5-diglucoside. Cytotoxicity assays demonstrated a dose-dependent reduction in cell viability, with DAOY cells exhibiting the highest sensitivity. Water extract exhibited significant inhibitory effects at elevated concentrations, whereas ethanol extract showed greater potency at intermediate doses (7.5%-50%) for specific cancer cell lines. Methanol extract exhibited a more gradual impact and showed reduced potency at elevated doses. According to IC50 values, the ethanolic extract was the most efficacious in four out of the six cancer cell lines, whereas water extract demonstrated notable potency for OCI-AML3 and OSN-76 but were less effective on normal cells, suggesting selectivity based on cell type. The selectivity index indicated that methanol exhibited the highest selectivity, especially against OSN-76, MV4-11, OCI-AML3, and HeLa cell lines, implying its predilection for cancer cells over normal cells. Ethanol demonstrated notable selectivity, particularly toward OSN-76 and MV4-11. Conversely, water extracts exhibited minimal selectivity across all strains. In summary, methanol and ethanol extracts demonstrate the best potential for selective anticancer efficacy.

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  • Research Article
  • 10.21474/ijar01/22918
EXPLORING THE PHARMACOLOGICAL POTENTIAL OF SYNECHOCOCCUS SP. PGDR2 THROUGH PHYTOCHEMICAL AND IN VITRO BIOACTIVITY STUDIES
  • Mar 31, 2026
  • International Journal of Advanced Research
  • Gomathi U + 2 more

Cyanobacteria are recognized as promising sources of bioactive compounds with pharmaceutical potential. The present study evaluated the phytochemical composition and biological activities of Synechococcus sp. PGDR2. Qualitative screening revealed the presence of tannins and proteins, while other major secondary metabolites were absent. Antioxidant activity assessed by DPPH and ABTS assays showed weak radical scavenging capacity with IC50 values >320 ug/mL. In contrast, ascorbic acid exhibited strong antioxidant activity with IC50 values of 19.97 ug/mL (DPPH) and 20.46 ug/mL (ABTS). Cytotoxicity against MG-63 osteosarcoma cells using the MTT assay demonstrated minimal growth inhibition, with an IC50 value >100 ug/mL, compared to doxorubicin (IC50 = 9.52 ug/mL). The anti-inflammatory activity evaluated by the protein denaturation assay showed moderate inhibition with an IC50 of 235.11 ug/mL, whereas diclofenac sodium exhibited an IC50 of 29.43 ug/mL.The comparatively high IC50 values suggest limited bioactivity of the crude extract. The observed anti-inflammatory potential may be attributed to tannins and proteinaceous compounds. Overall, Synechococcus sp. PGDR2 exhibited mild biological activity, indicating the need for further purification and LC MS profiling to identify potential bioactive constituents. These findings contribute to understanding the pharmacological potential of freshwater cyanobacteria.

  • Research Article
  • 10.3760/cma.j.cn112152-20250608-00265
Glutathione-responsive AP site captor Probe-NEt for anaplastic thyroid cancer: in vitro and in vivo experimental studies
  • Mar 23, 2026
  • Zhonghua zhong liu za zhi [Chinese journal of oncology]
  • M X Su + 9 more

Objective: To exploit the elevated glutathione (GSH) levels in the tumor microenvironment and investigate the therapeutic efficacy of a novel glutathione-responsive apurinic/apyrimidinic (AP) site captor, Probe-NEt, against anaplastic thyroid cancer (ATC). Methods: Fluorescence imaging compared Probe-NEt uptake and activation in normal thyroid (Nthy ori 3-1), ATC (THJ-16T, CAL-62), and lung cancer (H1299) cells. Half maximal inhibitory concentration (IC50) values were determined by cytotoxicity assays; DNA damage was evaluated using appropriate assays. Flow cytometry analyzed cell cycle distribution and apoptosis following treatment with low (5 μmol/L) or high (20 μmol/L) Probe-NEt concentrations. BALB/c nude mice bearing subcutaneous ATC xenografts received low (0.025 mg) or high (0.05 mg) dose injections. Tumor volumes were monitored; HE staining assessed biosafety in major organs; immunohistochemistry detected apoptosis-related protein expression. Results: ATC cells demonstrated significantly higher Probe-NEt activation than normal thyroid cells. Probe-NEt exhibited selective cytotoxicity (higher IC50 in normal vs. ATC cells; all P<0.01) with time-dependent characteristics; the selectivity ratio increased from 1.7 at 24 h (62.4 vs. 37.7 μmol/L) to 2.4 at 48 h (32.7 vs. 13.5 μmol/L). Probe-NEt induced DNA damage, G2/M arrest (THJ-16T: from 5% to 43%; CAL-62: from 19% to 37%), and dose-dependent late apoptosis. In THJ-16T cells, late apoptotic rates rose from 5.49% (control) to 13.95% (low-dose) and 63.43% (high-dose), with viable cells decreasing accordingly (89.42%, 76.01%, 20.45%). CAL-62 cells showed similar trends (16.72%, 40.19%, 69.88%). In vivo, Probe-NEt significantly suppressed tumor growth without hepatorenal toxicity (all P>0.167). Immunohistochemistry revealed upregulated pro-apoptotic proteins, downregulated anti-apoptotic proteins, and decreased Ki-67 expression. Conclusion: The glutathione-responsive AP site captor Probe-NEt significantly inhibits ATC cell growth, induces G2/M phase cell cycle arrest, promotes late apoptosis, and exhibits high selectivity and favorable biosafety profiles.

  • Research Article
  • 10.52711/0974-360x.2026.00158
In-vitro Antioxidant Activity of Bio-guided Fraction of Artemisia pallens
  • Mar 16, 2026
  • Research Journal of Pharmacy and Technology
  • Rajendra O Ganjiwale + 1 more

Background: The researcher reported that phenolic and flavonoid compounds are the major contributors to antioxidant activity, acting through the inhibition of enzymes responsible for increasing oxidative stress. Objectives: The present study aimed to evaluate the in vitro antioxidant activity of the bio-guided fraction of Artemisia pallens by the DPPH method. Methods: The bio-guided fractionation of the ethanolic extract was done using Hexane, Chloroform, Ethyl acetate, and Water. The phytochemical investigation, qualitative and quantitative analysis, and Chromatographic analysis were done. The IC₅₀ value was calculated by the regression method. Result: The phytochemical analysis of Artemisia pallens reveals the presence of flavonoids, phenolic compounds, glycosides, terpenoids, and alkaloids in different solvent fractions. Ethyl acetate and water fractions showed significant activity (IC₅₀ = 171.17 and IC₅₀ = 16.76µg/ml, respectively). The water fraction, having a low IC₅₀ value (16.76µg/mL) indicates more antioxidant activity, but the ethyl acetate fraction, having a higher IC₅₀ (171.17µg/mL), was selected as an effective fraction for further analysis due to its moderate polarity and feasible extraction yield, . Though the water fraction showed potent in vitro activity, in contrast, the highly polar constituents of the water fraction may exhibit limited absorption and bioavailability in vivo. lipophilic fractions exhibited superior in vivo antioxidant effects compared to highly polar fractions, despite weaker in vitro performance. Conclusion: The phytochemical analysis and in-vitro DPPH assay of the ethyl acetate fraction showed promising antioxidant activity, probably due to the higher concentration of flavonoids and phenolic compounds. Therefore, the ethyl acetate fraction was considered more suitable for antioxidant activity, as it represents bioactive constituents capable of effective in vivo antioxidant defence rather than radical scavenging. Therefore, these findings support that Artemisia pallens may be useful as an option for the management of stress as an antioxidant agent. Further in-vivo studies are needed to correlate antioxidant potential with possible neuroprotective outcomes.

  • Research Article
  • 10.1016/j.ijpharm.2026.126646
Excipient toxicity and tolerability in self-emulsifying drug delivery systems: insights from cell-based assays.
  • Mar 1, 2026
  • International journal of pharmaceutics
  • Marlene Ramona Schmidt + 5 more

The toxicological evaluation of excipients plays a crucial role in the development of SEDDS. This study examined key formulation components to identify critical factors influencing cellular tolerance and supports the design of biocompatible SEDDS. Physicochemical properties of various oils, co-solvents, co-surfactants, non-ionic and charged surfactants formulated in SEDDS were determined via dynamic light scattering, while oxidative stability of selected surfactants was assessed through hydroperoxide quantification. Biological compatibility was evaluated by analyzing hemolytic effects on human erythrocytes and cell viability in CaCo-2 and HEK-293 cells. Metabolic activity and proliferation were additionally measured photometrically via MTT test. Cellular compatibility varied markedly among individual excipients, depending on their chemical structure and formulation role. In lipid-based systems, saturated triglycerides yielded up to sixfold higher viability than free fatty acids. Co-solvent toxicity correlated with lipophilicity and functional groups: isopropanol induced early membrane stress in CaCo-2 cells, while glycerol caused delayed hemolysis after 48h. A clear structure-activity relationship emerged across surfactant types. PEG-based surfactants outperformed fatty alcohols and sugar-based formulations, which reached IC50 values below 0.01% after 24h and triggered early proliferation loss. This trend aligned with peroxide levels, as surfactants<10mM consistently maintained high CaCo-2 viability and stable IC50 values, exemplified by polyoxyl 40 hydrogenated castor oil. Among zwitterionic surfactants, phosphatidylcholine showed highest biocompatibility, causing only a twofold reduction in hemolytic activity after 48h, whereas cocoamidohydroxypropyl sulfobetaine induced an 12-fold decrease within 3h. These findings underscore the role of excipient selection in minimizing cellular stress and adverse drug reactions in oral lipid-based drug delivery.

  • Research Article
  • 10.22271/chemi.2026.v14.i3a.12666
Integrated molecular simulation, in vitro antioxidant evaluation, and in silico ADMET profiling of perylene-2,8-dione derivatives as potential therapeutics targeting oxidative stress in CNS disorders
  • Mar 1, 2026
  • International Journal of Chemical Studies
  • Sweta Rai + 3 more

The current study sought to confirm the antioxidant qualities of the serotonergic receptor for the successful treatment of neurodegenerative diseases and investigate the molecular interaction of the receptor with a derivative of perylene 2,8-dione. Oxidative Stress (OS) is the primary cause of degeneration of cholinergic cells in Alzheimer's disease and dopaminergic cells in Parkinson's Disease (PD) through multiple cascades. It is also closely linked to other mechanisms that lead to neurodegeneration, such as NO-induced excitotoxicity, neuroinflammation, and mitochondrial failure. The present study investigated how the bioactive perylene derivative interacts molecularly with serotonergic target receptors to alleviate a range of CNS disorders. Antioxidant activity against nitric oxide (•NO) and hypochlorous acid (HOCl) was confirmed using in vitro models. Our results indicate that a derivative of perylene 2, 8-dione with binding energy can interact with the 5HT1A receptor. It can also neutralise all the different free radicals under consideration and has high IC50 values against HOCl and •NO. These findings suggest that the perylene derivative may serve as a promising candidate for mitigating oxidative stress-mediated neurodegenerative conditions.

  • Research Article
  • 10.1128/aac.01390-25
A Fe-incorporated bioreactor platform exhibiting antimalarial activity and enhanced response to artemisinin
  • Feb 20, 2026
  • Antimicrobial Agents and Chemotherapy
  • Yinyue Li + 11 more

While malaria parasites rely on labile Fe2+ pools for survival, excess Fe2+ acts as a Fenton reagent, inducing cytotoxicity via reactive oxygen species and membrane disruption, highlighting iron homeostasis as a key therapeutic vulnerability. To test the feasibility of iron ions in inhibiting Plasmodium parasites, we developed Fe2+-loaded polydopamine nanoparticles (PDA@Fe/P) that exploit the parasite's iron-dependent vulnerabilities through dual mechanisms: (i) sustained Fe2+ release triggers Fenton reactions, generating cytotoxic hydroxyl radicals that overwhelm antioxidant defenses, and (ii) restoration of artemisinin (ART) activation in resistant parasites by supplementing the diminished Fe2+ pool. In vitro testing against five P. falciparum strains (including chloroquine- and ART-resistant variants) demonstrated potent, antimalarial activity, with efficacy 20-fold higher than free FeCl2 due to enhanced solubility and controlled release. While in vivo studies in P. berghei-infected mice showed transient parasite suppression without toxicity, the relatively high IC50 precludes standalone use. Crucially, PDA@Fe/P enhanced the activity of ART against P. falciparum strain with partial ART resistance conferred by Kelch13 mutation, by counteracting mutation-induced impairments in hemoglobin endocytosis and heme bioavailability-key determinants of ART activation. Analysis of lipid peroxidation levels revealed that Fe2+ delivered via PDA@Fe/P amplifies oxidative stress responses in resistant parasites, indicating its ability to enhance the sensitivity of ART-resistant strains to ART. Our findings establish iron-based delivery strategies as a promising approach to potentiate existing antimalarials and combat resistance through the targeted disruption of redox homeostasis.

  • Research Article
  • 10.1093/jacamr/dlag015
Plasmodium falciparum field isolates drug susceptibility in Mali
  • Feb 12, 2026
  • JAC-Antimicrobial Resistance
  • Fatoumata Ousmane Maiga + 11 more

Background and objectivesThe emergence and spread of antimalarial drug resistance threaten malaria control efforts in sub-Saharan Africa. Monitoring the susceptibility of circulating Plasmodium falciparum isolates is essential to inform national treatment guidelines and guide the development of new therapies. To assess the ex vivo susceptibility of P. falciparum field isolates to 14 antimalarials, including withdrawn/unused and currently used drugs, and next-generation agents in Mali.MethodsTwenty-six isolates collected from patients with uncomplicated malaria at three endemic sites (Faladje, Kolle and Bougoula-Hameau) were cultured ex vivo under standardized conditions. Parasites were exposed to 14 drugs, including tafenoquine, N-desethyl-amodiaquine, chloroquine, dihydroartemisinin, lumefantrine, pyronaridine, quinine, sulfadoxine, pyrimethamine, amodiaquine, atovaquone, GNF179, KDU691 and cabamiquine. Susceptibility was measured using fluorescence-based assays with SYBR Green I and Mitotracker dyes, and IC50 values were derived from dose–response curves.ResultsTafenoquine showed a very low potency (IC50 > 1500 nM). Chloroquine exhibited marked inter- and intra-site variability (IC50 ∼50–1300 nM), while N-desethyl-amodiaquine potently inhibited isolates (median IC50 < 20 nM in Faladje and Bougoula-Hameau). Current frontline drugs, dihydroartemisinin (median IC50 < 6 nM), lumefantrine (median IC50 < 50 nM) and pyronaridine (median IC50 < 10 nM), remained highly potent. Quinine showed variable efficacy (IC50 ∼75–1000 nM). Chemoprevention agents sulfadoxine and pyrimethamine displayed high IC50 values (median IC50 > 1000 and >2000 nM). Atovaquone and amodiaquine consistently inhibited all isolates (IC50 < 10 nM). Next-generation compounds cabamiquine and GNF179 demonstrated consistently strong activity (IC50 < 10 nM), while KDU691 showed moderate activity (median IC50 18–22 nM).ConclusionsWhile current frontline therapies remain effective, reduced activity of chemopreventive antimalarials supports the need for continued surveillance to detect early signs of resistance in Mali. The potent activity of next-generation candidates (cabamiquine and GNF179) supports their potential for further clinical development and field deployment.

  • Research Article
  • 10.69951/proceedingsbookoficeonimeri.v9i-.326
Flavonoids and Antioxidant Profiles of Centella asiatica Serum Cosmetic Products versus Ethanol Extract
  • Feb 6, 2026
  • Proceedings Book of International Conference and Exhibition on The Indonesian Medical Education Research Institute
  • Sutan Farrell Habibie + 2 more

The cosmetic industry is currently leaning toward herbal skincare products due to strong consumer preference for natural ingredients. Centella asiatica (CA) is frequently used as it contains flavonoids and centelloids known for their beneficial antioxidant properties. This study aimed to assess the efficacy of CA extract when incorporated into cosmetic formulations by comparing the total flavonoid content (TFC) and antioxidant activity of five commercial serums (A-E) against a pure CA ethanol extract. The experimental study was conducted in vitro, utilizing the CA extract, Vitamin C (as a positive control), and the five commercial serum products. TFC was determined quantitatively using UV-Visible spectrophotometry and quercetin standard. Antioxidant activity was measured using DPPH assay to calculate the IC50 value. Pure CA extract showed a mean TFC of 37.10 ± 0.21 mg QE/g, with serum samples showing high variability; the highest being Sample C with a TFC of 216.6 (99.89 - 246.1) mg QE/g and the lowest being sample E with a TFC of 24.75 ± 1.88 mg QE/g. Crucially, the pure CA extract demonstrated strong antioxidant activity with a mean IC50 of 52.45 ± 4.96 ppm. In contrast, all serum products exhibited significantly weaker antioxidant activities. Samples C and D resulted in extremely high IC50 values of 244100 ± 116700 ppm and 319300 ± 95700 ppm respectively, categorized as lower than weak, while samples A, B, and E were unable to reach 50% inhibition, indicating an antioxidant capacity below the measurable range. In conclusion, despite the pure Centella asiatica ethanol extract showing robust antioxidant activity, the commercial cosmetic serums demonstrated a significantly lower range of activity and highly inconsistent TFC, suggesting that the raw extract's potency does not reliably transfer to the final product formulation.

  • Research Article
  • 10.48191/medfarm.v14i2.682
Computational Investigation of α-Glucosidase Inhibition by Phytochemical Compounds from Muntingia calabura L. Leaves: Insights into Potential Antidiabetic Agents
  • Dec 30, 2025
  • MEDFARM: Jurnal Farmasi dan Kesehatan
  • Syaiful Prayogi + 3 more

Diabetes Mellitus (DM) is a degenerative disease that poses a major global health problem. It is characterized by increased blood glucose levels (hyperglycemia). Common therapeutic agents for DM include sulfonylureas, biguanides, and α-glucosidase inhibitors. However, the use of α-glucosidase inhibitors is often associated with several issues such as the presence of non-intestinal α-glucosidase in various body cells, gastrointestinal side effects (diarrhea, bloating, abdominal discomfort), and high IC₅₀ values indicating low potency and efficacy against the α-glucosidase enzyme. This study aims to explore the potential of flavonoid compounds from Muntingia calabura L. (kersen) leaves as α-glucosidase inhibitors through in silico analysis. The study was conducted using molecular docking to evaluate the binding affinity and interaction of flavonoid compounds with the α-glucosidase enzyme. The docking results showed that 8 ligands test exhibited strong binding affinities, inhibitors constants, and stable interactions with the active site of α-glucosidase, comparable to standard inhibitors (acarbose). The two most promising ligands as α-glucosidase inhibitors were identified as 20,40-Dihydroxy-30-methoxydihydrochalcone (50) and (-)-30-Methoxy-20,40,β-trihydroxydihydrochalcone (51), exhibiting binding affinities and inhibition constants of –7.33 kcal/mol; 4.27 μM and –7.30 kcal/mol; 4.45 μM, respectively, have promising potential as natural α-glucosidase inhibitors and may serve as lead compounds for the development of new antidiabetic agents. Their inhibitory potential was further supported by favorable ADMET parameters and compliance with Lipinski’s rule of five. Further in vitro and in vivo studies are needed to confirm these findings.

  • Research Article
  • 10.3390/plants15010069
Chemical Profile and In Vitro Protective Effects of Minthostachys verticillata (Griseb.) Epling Aqueous Extract in Intestinal Inflammatory Environments.
  • Dec 25, 2025
  • Plants (Basel, Switzerland)
  • Angeles Gloria Rodríguez-Basso + 7 more

Minthostachys verticillata (Griseb.) Epling, commonly known as peperina, is an aromatic species endemic to Argentina and traditionally used for gastrointestinal ailments. Despite its extensive folkloric use and inclusion in the Argentine Pharmacopoeia, its aqueous extract (the most commonly consumed preparation) has been described in terms of major phytochemical groups, and, currently, no studies have investigated its effects on key intestinal epithelial mechanisms. This plant is also employed in the production of beverages and herbal blends, and its massive consumption highlights the importance of its scientific study. Here, the aqueous extract of M. verticillata was characterized by liquid chromatography-tandem mass spectrometry, leading to the identification of fourteen polyphenolic compounds. In intestinal cell models, the extract displayed high IC50 values, supporting its safety, and exhibited concentration-dependent bioactivity. In HT-29 cells, it modulated NF-κB activation induced by TNF-α and reduced LPS-stimulated IL-8 production. Pretreatment of Caco-2 monolayers prevented the decrease in transepithelial electrical resistance, increased FITC-dextran permeability, and nitric oxide production triggered by an inflammatory cocktail. Additionally, the extract inhibited HT-29 cell migration. These results demonstrate that M. verticillata aqueous extract exerts anti-inflammatory, barrier-protective, and anti-migratory effects in vitro, providing novel insights into how its polyphenolic composition may underlie these biological activities, supporting its traditional use and potential applications in intestinal health.

  • Research Article
  • 10.29303/jbt.v25i4a.11048
Antioxidant Activity of Methanol Extract Leaves of Neem (Azadirachta indica)
  • Dec 23, 2025
  • Jurnal Biologi Tropis
  • Syamsul Bahri + 2 more

Azadirachta indica Juss. (neem), a medicinal plant belonging to the Meliaceae. The leaves of this species contain bioactive compounds such as flavonoids, alkaloids, steroids, saponins, tannins, and azadirachtin. These compounds exhibit antimicrobial activity against Salmonella and Escherichia coli. This study aimed to determine the antioxidant activity of the neem leaves' methanol extract by using the DPPH method. The research method used phytochemical screening by separating chemical compounds from samples using 70% methanol solvent. The result showed that the antioxidant activity of the neem leaves' methanol extract is classified in the weak category with an IC50 score of 426.15 mg/mL. One of the main factors explaining the high IC50 values is the differences in the chemical structure and molecular shape of the secondary metabolites contained in the extracts. The antioxidant activity of flavonoids and phenolics is greatly influenced by the number and position of hydroxyl groups, the degree of conjugation, and the presence of sugar groups.

  • Research Article
  • 10.35516/jjps.v18i4.3218
Formulation, characterization, and cytotoxicity evaluation of doxorubicin loaded niosomes prepared by microfluidic mixing
  • Dec 18, 2025
  • Jordan Journal of Pharmaceutical Sciences
  • Dr Mohammad A Obeid + 3 more

Doxorubicin (DOX) is one of the common anticancer agents used for treating various types of cancer. One limitation of DOX is the development of cancer cell resistance and its wide range of toxicity. Niosomes are type of nanoparticles that consist of non-surfactants and cholesterol in the form of a bilayer structure. The aim of the present study was to develop and optimize DOX-loaded niosomes using microfluidic mixing through buffer exchange strategy to overcome DOX limitations such as unwanted distribution and toxicity. Two niosome formulations (F1 and F2) were prepared using T85 as a non-ionic surfactant. F1 was composed of TW85: CHOL (40:60)/DOX, while F2 was composed of TW85: CHOL: DDAB (40:40:20)/DOX. F1 had an anionic surface charge of around -13 mV, while F2 had a cationic charge of around +20 mV. DOX was successfully entrapped in both formulations with entrapment efficiencies of approximately 11% for F1 and 79% for F2, respectively. Loading DOX into F1 resulted in a significant reduction in the IC50 value in both MCF7 and A549 cells. However, loading DOX into F2 resulted in a higher IC50 in both cell lines compared to the free DOX. In conclusion, the optimized DOX niosomes formulation F1 improved the anticancer activity of DOX compared to free DOX drug. These results demonstrate that optimized niosomes can be effective tools for delivering DOX to target breast and lung cancer cells.

  • Research Article
  • 10.31942/jiffk.v22i2.12398
Antioxidant Activity of Facial Gel Moisturizer Formulation From Various Plants: A Literature Review
  • Dec 17, 2025
  • Jurnal Ilmu Farmasi dan Farmasi Klinik
  • Adhitya Ilham Mukti + 3 more

Antioxidants are compounds that can neutralize free radicals, which can damage normal cells, fats, and proteins. Various methods, such as DPPH, ABTS, and FRAP, are used to evaluate the capacity of antioxidant compounds against reactive oxygen species (ROS). Skin ageing, caused by free radicals, pollution, and ultraviolet rays, can be mitigated by using antioxidants, one of which is found in cosmetic preparations such as moisturizers. This study aims to determine the antioxidant activity of various plant extracts in the formulation of a moisturizer gel. The method used is a literature review, with sources from the Google Scholar and PubMed databases, which includes articles from 2014 to 2024, resulting in 9 eligible articles out of 20 screened. The review result showed that plants such as star fruit leaf extract (Averrhoa bilimbi L.) and green tea leaf (Camellia sinensis) have potent antioxidant activity. Starfruit Wuluh (Averrhoa bilimbi L.) extracted with 70% ethanol had an IC50 value of 24.78 ppm, while green tea leaf extract (Camellia sinensis) with 70% ethanol showed an IC50 value of 5.62 ppm in the gel moisturizer preparation. A high IC50 indicates that the compound contains antioxidants that can protect the skin from free radicals, which are formulated into a moisturizing gel. In conclusion, star fruit leaf extract (Averrhoa bilimbi L.) and green tea leaf extract (Camellia sinensis) are highly effective ingredients in moisturiser gel products, as they provide significant antioxidant protection to the ski

  • Research Article
  • 10.1007/s10470-025-02551-5
High voltage gate driver IC with integrated bootstrap circuits for floating channels supply
  • Dec 12, 2025
  • Analog Integrated Circuits and Signal Processing
  • Guanning Wang + 3 more

High voltage gate driver IC with integrated bootstrap circuits for floating channels supply

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