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Background: The treatment of gastric cancer (GC) is still quite challenging. Yet, marine invertebrates have been found to produce a wide range of anticancer bioactive compounds that show promise in fighting cancer. The present study aimed to evaluate whether saponin derived from Holothuria leucospilata (H. Leucospilota), a species of sea cucumber, possesses anticancer activity against GC cells. Method: In this experimental study, the cytotoxic effect of H. Leucospilota-derived n-butanol fraction saponins (HLBS) sourced from the Persian Gulf on MKN45 GC cells was evaluated through tetrazolium salt and colony formation assays. The effect of HLBS on MKN45 cell migration, cell cycle, and apoptosis was assessed using a scratch assay, and flow cytometry, respectively. Hub genes of GC were identified through bioinformatics analysis. The effects of HLBS on the expression of the two top-ranked GC hub genes were measured using real-time polymerase chain reaction. Comparisons between groups were performed using the ANOVA test by GraphPad Prism software at the statistically significant P-value <0.05. Results: HLBS with an IC50 concentration of 75 µg/ml at 48 hours resulted in a significant decrease in cell viability, clonogenic ability (46.63% reduction, P < 0.01), and migration of MKN45 cells (74.5% reduction, P < 0.01). Moreover, HLBS led to an increase of approximately 21 and 13% in the S-phase and apoptotic cell populations, respectively. HLBS also upregulated the expression of CDH1, as a highly ranked hub gene associated with GC (P < 0.05). Conclusion: The inhibitory effect of HLBS on MKN45 cells suggests HLBS as a candidate for further drug discovery programs in GC research, and paves the way to introduce new anticancer HLBS synthetic derivatives. [ABSTRACT FROM AUTHOR]

Chromobacterium violaceum is a pathogenic bacterium that can infect humans and animals, yet the role of its outer membrane vesicles (OMVs) in mediating pathogenicity remains underexplored. This study evaluated the effects of linoleic acid (LA) and stearic acid (SA) on quorum sensing (QS)-mediated violacein production, biofilm formation, and OMV biogenesis in C. violaceum. Our findings revealed that 2 mM LA and 1 mM SA effectively quench QS, leading to a significant reduction in violacein production, biofilm formation, and OMV biogenesis. Gene expression analysis confirmed the downregulation of QS-related genes, including cviI, cviR, vioA, vioB, and vioC, in fatty acid-treated C. violaceum. Additionally, we assessed the antimicrobial activity of C. violaceum-derived OMVs on Rhizobium sp., a PGPR and observed a marked reduction in bactericidal activity in the treated OMVs. This study suggests that LA and SA have potential as anti-infective agents to mitigate OMV-mediated virulence and combat antibiotic resistance in pathogens. [ABSTRACT FROM AUTHOR]

Soft corals produce a diverse range of natural products with pharmaceutical potential, such as antiproliferative and anti-inflammatory effects. The Alcyoniidae family, particularly the genera Sarcophyton and Sinularia, is rich in bioactive terpenoids. However, despite extensive research, their anti-biofouling properties against the mussel Mytilus galloprovincialis remain underexplored. This study investigates these compounds as potential eco-friendly antifouling agents. A new cembrane-type diterpenoid, 11,12-epoxycembrene A (1), and 15 known compounds were isolated from three soft corals distributed in Okinawa, Japan. The chemical structures of these secondary metabolites were elucidated based on spectroscopic analysis. Moreover, an anti-biofouling assay of potential anti-biofouling agents against M. galloprovincialis was performed and their toxicities were assessed by means of the brine shrimp mortality test. In conclusion, this study identifies new and known bioactive compounds from soft corals, introduces an improved anti-biofouling assay, and highlights the potential of dimethylamine-containing diterpenes as environmentally friendly antifouling agents. [ABSTRACT FROM AUTHOR]

The main components, [6]-shogaol (6) and [6]-gingerol (7), were obtained from the rhizome of Zingiber officinale. Both natural phenolic compounds were modified at C4′ position to get new sixteen derivatives. All derivatives were screened for their HDAC inhibitory activity at 50 µM using HeLa nuclear extract. Among the synthesized compounds, derivatives 6b, 6e, 6f and 6g were the most effective against HDACs with the IC50 values as 44.60 ± 1.40 µM, 49.23 ± 1.13 µM, 50.55 ± 4.25 µM and 48.52 ± 1.52 µM, respectively. In addition, the selected derivatives were investigated against HDAC8 inhibitory activity. The results demonstrated that among them, 6b was selective with HDAC8 (IC50 = 23.19 ± 1.57 µM). The molecular docking study via MOE docking program also revealed that compound 6b bound into the active pocket of HDAC8 with ΔG value as −6.92 kcal/mol. Moreover, the in vitro antiproliferative activity of four most potent compounds were evaluated against nine cancer cell lines with MTT assay. The results showed that all selected derivatives were most effective against lung (A549), colon (HCT116 and HT29) and human cervical (HeLa) cancer cell lines. Especially, compound 6g was the most potent against A549 cancer cell line with the IC50 value as 8.41 ± 0.04 µM. Therefore, compound 6b and 6g are considered as promising HDACs-inhibitor-anticancer agents. [ABSTRACT FROM AUTHOR]

The roots of Litsea cubeba (Lour.) Pers have been used for the treatment of rheumatism. We previously extracted and isolated the natural product dibenzylbutane lignan LCA with anti-inflammatory activity. In the current study, using LCA as the lead compound, two series of LCA derivatives with an imide structure and butadiene structure were designed and synthesized. Among them, compounds 10c and 16a showed stronger inhibitory effects on LPS-induced NO and ROS production in RAW264.7 cells. Further study showed that compound 16a not only reduced the levels of inflammatory cytokines, including IL-6, TNF-α, and IL-1β, but it also significantly reduced the expression of iNOS and COX-2. Preliminary mechanism of action studies suggested that 16a exerts anti-inflammatory effects by inhibiting the NF-κB signaling pathway. Overall, our results suggest that compound 16a may be used as a promising anti-inflammatory drug to enrich the compound library. Further study into compound 16a could provide research ideas and methods for developing anti-inflammatory drugs. [ABSTRACT FROM AUTHOR]

Introduction: An abundance of experimental evidence indicates that icariin (ICA) could potentially exert an anti-tumor effect on ovarian cancer (OC). Nevertheless, the reliability of this evidence remains ambiguous. This study aimed to explore the impact of ICA on OC and the underlying mechanisms. Methods: Bioinformatics analysis was employed to pinpoint ICA-targeted genes and signaling pathways implicated in OC, utilizing network pharmacology. Subsequently, PubMed, EMBASE, and Web of Science databases were systematically searched from 2001 through June 2023 for in vitro trials evaluating the anti-tumor efficacy of conventional ICA versus placebo in OC. The pathways and genes identified in the literature were recorded, and the therapeutic targets were statistically analyzed and compared with the predicted targets from network pharmacology to confirm the precision of the targets. Results and Discussion: Fourteen target genes were validated with success. The pathways corresponding to the remaining genes—excluding these 14—were analyzed and found to be primarily associated with cell apoptosis, anti-tumor, and other related pathways. Out of the 76 studies retrieved, eight fulfilled the inclusion criteria. The subsequent meta-analysis suggested that ICA treatment was significantly correlated with reduced cell growth and induced apoptosis. This study demonstrated a certain efficacy of ICA compared to placebo in enhancing anti-tumor outcomes, characterized by increased abilities in reducing cell growth and inducing apoptosis. The pathways involved in the therapeutic effect may be linked to cell apoptosis and anti-tumor mechanisms. [ABSTRACT FROM AUTHOR]

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Saponins are compounds composed of lipophilic aglycones linked to hydrophilic sugars. Natural saponins are isolated from plants and some Marine organisms. As important cholesterol-lowering drugs, natural saponins have attracted wide attention for their therapeutic potential in a variety of cholesterol-related metabolic diseases. To review the effects of natural saponins on cholesterol-related metabolic diseases, and to deepen the understanding of the cholesterol-lowering mechanism of saponins. The literature related to saponins and cholesterol-lowering diseases was collected using keywords "saponins" and "cholesterol" from PubMed, Web of Science, and Google Scholar from January 2000 to May 2024. The total number of articles related to saponins and cholesterol-lowering diseases was 240 after excluding irrelevant articles. Natural saponins can regulate cholesterol to prevent and treat a variety of diseases, such as atherosclerosis, diabetes, liver disease, hyperlipidemia, cancer, and obesity. Mechanistically, natural saponins regulate cholesterol synthesis and uptake through the AMPK/SREBP2/3-hydroxy-3-methyl-glutaryl coenzyme A reductase pathway and PCSK9/LDLR pathway, and regulate cholesterol efflux and esterification targeting Liver X receptor/ABC pathway and ACAT family. Natural saponins have broad application prospects in regulating cholesterol metabolism, for the development of more cholesterol-lowering drugs provides a new train of thought. However, it is still necessary to further explore the molecular mechanism and expand clinical trials to provide more evidence., (© 2025 John Wiley & Sons Ltd.)

Anticancer drug discovery needs serious attention to overcome the high mortality rate caused by cancer. There are still many obstacles to treating this disease, such as the high cost of chemotherapeutic drugs, the resulting side effects from the drug, and the occurrence of multidrug resistance. Herbaceous plants are a reservoir of natural compounds that can be anticancer drugs with novel mechanisms of action. Piperine, a bioactive compound derived from Piper species, is gaining attention due to its unique dual role in directly inhibiting tumor growth and enhancing the bioavailability of chemotherapeutic drugs. Unlike conventional treatments, Piperine exhibits a novel mechanism of action by modulating multiple signaling pathways, including apoptosis and autophagy, with low toxicity. Additionally, Piperine acts as a bioenhancer by improving the absorption and effectiveness of other anticancer agents, reducing the required dosage, and minimizing side effects. Therefore, this review aims to visualize a summary of Piperine sources, phytochemistry, chemical structure-anticancer activity relationship, anticancer activities of semi-synthetic derivatives, pharmacokinetic and bioavailability, in vitro and in vivo preclinical studies, mechanism of antitumor action, human clinical trials, toxicity, side effects, and safety of Piperine. References were collected from the Pubmed/MedLine database (https://pubmed.ncbi.nlm.nih.gov/) with the following keywords: "Piperine anticancer," "Piperine derivatives," "Piperine antitumor mechanism" and "Piperine pharmacokinetic and bioavailability," after filter process by inclusion and exclusion criteria, 101 were selected from 444 articles. From 2013 to 2023, there were numerous studies regarding preclinical studies of Piperine of various cell lines, including breast cancer, prostate cancer, lung cancer, melanoma, cervical cancer, gastric cancer, osteosarcoma, colon cancer, hepatocellular carcinoma, ovarian cancer, leukemia, colorectal cancer, and hypopharyngeal carcinoma. In vivo, the anticancer study has also been conducted on some animal models, such as Ehrlich carcinoma-bearing mice, Ehrlich ascites carcinoma cells-bearing Balbc mice, hepatocellular carcinoma-bearing Wistar rat, A375SM cells-bearing mice, A375P cells-bearing mice, SNU-16 cells-bearing BalbC mice, and HGC-27-bearing baby mice. Treatment with this compound leads to cell proliferation inhibition and induction of apoptosis. Piperine has been used for clinical trials of diseases, but no cancer patient report exists. Various semi-synthetic derivatives of Piperine show efficacy as an anticancer drug across multiple cell lines. Piperine shows promise for use in cancer clinical trials, either as a standalone treatment or as a bioenhancer. Its bioenhancer properties may enhance the efficacy of existing chemotherapeutic agents, providing a valuable foundation for developing new anticancer therapies., (© 2024 International Union of Biochemistry and Molecular Biology.)

Phenyl amino pyrimidine attracts researchers due to its versatile scaffold and medicinal significance. This significant moiety present in the Imatinib contributed to medicinal chemistry. In this manuscript, we reviewed various derivatives of Imatinib containing 2-phenylaminopyrimidine, which has a variety of roles, especially in the anti-cancer category. This manuscript aims to prepare a scientific report that underscores the novel Imatinib derivatives in the field of chemistry for various activities such as anti-cancer, anti-microbial, and miscellaneous focused on cardiovascular, anti-platelets, and anti-parasitic, etc. Finally, this manuscript may attract researchers for new structure design, and the development of novel phenyl amino pyrimidine scaffolds that are more active and less harmful. We propose a compilation and analysis of around 100 Imatinib derivatives having main chromatophores, such as phenylaminopyrimidine. A large number of researchers are interested in Imatnib-based analogs as they have wide biological potential in the largely developing chemical world of the heterocyclic moiety. The phenylamino pyrimidine moiety became an important moiety for researchers to discover combinational libraries and implement the efforts in search of the lead entities. Phenylaminopyrimidine has been manifesting to be an effective moiety in the current respective disease scenario. It has been discovered that phenylaminopyrimidine and its derivatives have an extensive spectrum of pharmacological potential with numerous applications in academic interest, in the pharmaceutical industry, medicinal chemistry, etc. Imatinib containing phenylaminopyrimidine and its novel synthetic derivatives are a prominent heterocyclic compound class with intriguing use in medicinal chemistry. Thus, in brief, attention should be given to other chemical approaches for synthesizing novel compounds containing phenylaminopyrimidine moiety, hence potentiating their efficacy., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

In women globally, breast cancer ranks as the second most frequent cause of cancer-related deaths, making up about 25% of female cancer cases, which is pretty standard in affluent countries. Breast cancer is divided into subtypes based on aggressive, genetic and stage. The precise cause of the problem is still unknown. However, the following significant risk factors have been found: sex, age, heredity, not having children, breastfeeding, elevated hormone levels, and personal lifestyle. The presence or lack of three nuclear receptors ER, PR, and HER2/ERBB2 (triple negative) and the amplification of the HER2/ErbB2 gene are the clinical criteria used to classify breast cancer. Chemotherapy is still the cornerstone of treatment for triple-negative breast cancer (TNBC), even. If, for the first two groups of patients,receptor-specific therapy is used. The most often prescribed chemotherapy agents for the treatment of breast cancer include doxorubicin (DOX), curcumin paclitaxel (PTX), docetaxel (DCX), thioridazine (THZ), disulfiram (DSF), and camptothecin (CPT). Monoclonal antibodies (mAbs) were used in antibody-drug conjugates (ADCs) to bind tumor-associated target antigens selectively and deliver very effective cytotoxic agents. According to recent research, synthetic derivatives effectively combat both MCF- 7 and breast cancer cell lines that are resistant to many drugs. This review provides a wealth of information on the mechanism of action of synthetic derivatives on multidrug-resistant cell lines. This review includes information about how synthetic derivatives affect cancer cells that have developed multidrug resistance during chemotherapy. These mechanisms have been linked to factors such as increased drug efflux, genetic factors, growth factors, increased DNA repair capacity, and elevated xenobiotic metabolism. Because of this, more research is necessary to learn more about the effectiveness of synthetic derivatives against breast cancer and cell lines that are resistant to several drugs. This review aims to find recent prospects of various types of cellular signaling pathways (JAK/STAT, Akt, MAPK, etc.) involved in the progression of breast cancer disorder, and we also study different synthetic and natural drugs that are applied for treating breast cancer., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)