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An appealing strategy for finding novel bioactive molecules in Nature consists in exploring underrepresented and -studied microorganisms. Here, we investigated the antimicrobial and tumoral anti-proliferative bioactivities of twenty-three marine and estuarine bacteria of the fascinating phylum Planctomycetota. This was achieved through extraction of compounds produced by the Planctomycetota cultured in oligotrophic medium followed by an antimicrobial screening against ten relevant human pathogens including Gram-positive and Gram-negative bacteria, and fungi. Cytotoxic effects of the extracts were also evaluated against five tumoral cell lines. Moderate to potent activities were obtained against Enterococcus faecalis, methicillin-sensitive and methicillin-resistant Staphylococcus aureus and vancomycin-sensitive and vancomycin-resistant Enterococcus faecium. Anti-fungal effects were observed against Trichophyton rubrum, Candida albicans and Aspergillus fumigatus. The highest cytotoxic effects were observed against human breast, pancreas and melanoma tumoral cell lines. Novipirellula caenicola and Rhodopirellula spp. strains displayed the widest spectrum of bioactivities while Rubinisphaera margarita ICM_H10T affected all Gram-positive bacteria tested. LC-HRMS analysis of the extracts did not reveal the presence of any known bioactive natural product, suggesting that the observed activities are most likely caused by novel molecules, that need identification. In summary, we expanded the scope of planctomycetal species investigated for bioactivities and demonstrated that various strains are promising sources of novel bioactive compounds, which reenforces the potential biotechnological prospects offered by Planctomycetota. [ABSTRACT FROM AUTHOR]

Epimedium Folium has been extensively utilized for medicinal purposes in China for a significant period. This review undertakes a comprehensive examination of literature pertaining to Epimedium and its metabolites over the past decade, drawing from databases such as PubMed. Through meticulous organization and synthesis of pertinent research findings, including disease models, pharmacological effects, and related aspects, this narrative review sheds light on the principal pharmacological activities and associated mechanisms of Epimedium in safeguarding the reproductive system, promoting bone health, mitigating inflammation, and combating tumors and viral infections. Consequently, this review contributes to a more profound comprehension of the recent advances in Epimedium research. [ABSTRACT FROM AUTHOR]

Simple Summary: The repurposing of drugs is an important and rapidly growing field in the treatment of cancer. The main advantage of drug repurposing is using currently established drugs for various diseases and testing them on newer diseases, such as cancer. This strategy allows drug developers to reduce the time for a drug to be made available after clinical trials and testing by using drugs that have already gone through the process. The key to its use is to target the intricate signalling pathways in cancer, which contribute to the initiation, progression, and severity of cancer. Such pathways, if targeted correctly using repurposed drugs, could result in the regression of the tumour or, in some cases, a potential curative effect. The repurposing of previously clinically approved drugs as an alternative therapeutic approach to treating disease has gained significant attention in recent years. A multitude of studies have demonstrated various and successful therapeutic interventions with these drugs in a wide range of neoplastic diseases, including multiple myeloma, leukaemia, glioblastoma, and colon cancer. Drug repurposing has been widely encouraged due to the known efficacy, safety, and convenience of already established drugs, allowing the bypass of the long and difficult road of lead optimization and drug development. Repurposing drugs in cancer therapy is an exciting prospect due to the ability of these drugs to successfully target cancer-associated genes, often dysregulated in oncogenic signalling pathways, amongst which are the classical cancer signalling pathways; WNT (wingless-related integration type) and Hippo signalling. These pathways play a fundamental role in controlling organ size, tissue homeostasis, cell proliferation, and apoptosis, all hallmarks of cancer initiation and progression. Prolonged dysregulation of these pathways has been found to promote uncontrolled cellular growth and malignant transformation, contributing to carcinogenesis and ultimately leading to malignancy. However, the translation of cancer signalling pathways and potential targeted therapies in cancer treatment faces ongoing challenges due to the pleiotropic nature of cancer cells, contributing to resistance and an increased rate of incomplete remission in patients. This review provides analyses of a range of potential anti-cancer compounds in drug repurposing. It unravels the current understanding of the molecular rationale for repurposing these drugs and their potential for targeting key oncogenic signalling pathways. [ABSTRACT FROM AUTHOR]

Reproductive toxicity from food and environmental contaminants has greatly affected human life. Plants are a fundamental source of bioactive components for relieving the harmful effects of pollutants. Hydrazine metabolites pose health threats when they enter the food chain. Croton tiglium (C. tiglium) exhibits anti-inflammatory and anti-tumor properties. Silver nanoparticles enhance the chemical stability of C. tiglium. Reproductive toxicity of Azoxymethane (AOM) and anticancer effects of silver C. tiglium were evaluated. Thirty-six adult female rats were divided into six groups (n = 6) and treated with AOM with or without silver C. tiglium nano-extract as pre- and post-treatment. Sexual hormones and proteins were assessed under silver C. tiglium nano-extract and AOM. Histopathologically, AOM caused metaplastic myometrial endometriotic cysts and endometrial metaplasia. Silver C. tiglium in pre- and post-treated rats mitigated the carcinogenic effects of AOM. Immunohistochemically, AOM carcinogenicity was evident through moderate detection of the CK-7 tumor marker in the ovaries and uterus of the AOM-, simultaneous-, and post-treated groups. C. tiglium ameliorated this, with CK-7 slightly expressed in the pre-treated group. Furthermore, C. tiglium alleviated the negative impact on FSH, LH, and 17-β estradiol hormones. In conclusion, Silver C. tiglium nano-extract successfully prevented tumors in the ovaries and uterus of AOM-treated rats.

Background: Epidemiological studies suggest that metformin reduces the risk of developing several types of cancer, including gliomas, and improves the overall survival in cancer patients. Nevertheless, while the effect of metformin on cancer cells has been extensively studied, its impact on other components of the tumour microenvironment, such as macrophages, is less understood. Results: Metformin-treated mouse bone marrow cells differentiate into spindle-shaped macrophages exhibiting increased phagocytic activity and tumour cell cytotoxicity coupled with modulated expression of co-stimulatory molecules displaying reduced sensitivity to inflammatory cues compared with untreated cells. Transcriptional analyses of metformin-treated mouse bone marrow-derived macrophages show decreased expression levels of pro-tumour genes, including Tgfbi and Il1β, related to enhanced mTOR/HIF1α signalling and metabolic rewiring towards glycolysis. Significance: Our study provides novel insights into the immunomodulatory properties of metformin in macrophages and its potential application in preventing tumour onset and in cancer immunotherapy.

Medicinal herbs have been used since the time of the Vedas. The plants have therapeutic qualities in every part. Secondary metabolites of extensive variety are present in medicinal plants and are utilised in the production of medications as well as in the treatment of many different ailments. Withania somnifera is a medicinal plant, have various properties. 'Ashwagandha' is the popular name of Withania somnifera. It is offered as churna, a finely sieved powder that can be combined with ghee, water or honey. It has memory-enhancing, anti-oxidant, anti-stress, anti-venom, anti-inflammatory and anti-tumor effects. It is employed to treat a variety of clinical problems. In addition to being used as a suppressant in HIV/AIDS patients, Withania somnifera is used to treat ulcers, emaciation, colds, coughs, diabetes, conjunctivitis, insomnia, senile dementia, epilepsy, leprosy, Parkinson's disease, nervous disorders, rheumatism, arthritis, intestinal infections, bronchitis and asthma. The review article concentrates on the Withania somnifera plant's different pharmacological qualities. [ABSTRACT FROM AUTHOR]

This study has reviewed the many roles of lumican as a biomarker of tissue pathology in health and disease. Lumican is a structure regulatory proteoglycan of collagen-rich tissues, with cell instructive properties through interactions with a number of cell surface receptors in tissue repair, thereby regulating cell proliferation, differentiation, inflammation and the innate and humoral immune systems to combat infection. The exponential increase in publications in the last decade dealing with lumican testify to its role as a pleiotropic biomarker regulatory protein. Recent findings show lumican has novel roles as a biomarker of the hypercoagulative state that occurs in SARS CoV-2 infections; thus, it may also prove useful in the delineation of the complex tissue changes that characterize COVID-19 disease. Lumican may be useful as a prognostic and diagnostic biomarker of long COVID disease and its sequelae. [ABSTRACT FROM AUTHOR]

The synthesis of 3H-1,2-benzoxaphosphepine 2-oxides and evaluation of their inhibitory activity against human carbonic anhydrase (hCA) isoforms I, II, IX, and XII are described. The target compounds were obtained via a concise synthesis from commercial salicylaldehydes and displayed low to sub-micromolar inhibition levels against the tumour-associated isoforms hCA IX and XII. All obtained benzoxaphosphepine 2-oxides possess remarkable selectivity for inhibition of hCA IX/XII over the off-target cytosolic hCA isoforms I and II, whose inhibition may lead to side effects.

Ganoderma capense is a precious medicinal fungus in China. In this study, a novel fungal immunomodulatory protein gene, named as FIP-gca, was cloned from G. capense by homologous cloning. Sequencing analysis indicated that FIP-gca was composed of 336 bp, which encoded a polypeptide of 110 amino acids. Protein sequence blasting and phylogenetic analysis showed that FIP-gca shared homology with other Ganoderma FIPs. FIP-gca was effectively expressed in Pichia pastoris GS115 at an expression level of 166.8 mg/L and purified using HisTrap™ fast-flow prepack columns. The immunomodulation capacity of rFIP-gca was demonstrated by that rFIP-gca could obviously stimulate cell proliferation and increase IL-2 secretion of murine spleen lymphocytes. Besides, antitumor activity of rFIP-gca towards human stomach cancer AGS cell line was evaluated in vitro. Cell wound scratch assay proved that rFIP-gca could inhibit migration of AGS cells. And flow cytometry assay revealed that rFIP-gca could significantly induce apoptosis of AGS cells. rFIP-gca was able to induce 18.12% and 22.29% cell apoptosis at 0.3 μM and 0.6 μM, respectively. Conclusively, the novel FIP-gca gene from G. capense has been functionally expressed in Pichia and rFIP-gca exhibited ideal immunomodulation and anti-tumour activities, which implies its potential application and study in future. [ABSTRACT FROM AUTHOR]

The synthesis of 3H-1,2-benzoxaphosphepine 2-oxides and evaluation of their inhibitory activity against human carbonic anhydrase (hCA) isoforms I, II, IX, and XII are described. The target compounds were obtained via a concise synthesis from commercial salicylaldehydes and displayed low to sub-micromolar inhibition levels against the tumour-associated isoforms hCA IX and XII. All obtained benzoxaphosphepine 2-oxides possess remarkable selectivity for inhibition of hCA IX/XII over the off-target cytosolic hCA isoforms I and II, whose inhibition may lead to side effects. [ABSTRACT FROM AUTHOR]

Aspirin is a well-known nonsteroidal anti-inflammatory drug (NSAID) that has a recognized role in cancer prevention as well as evidence to support its use as an adjuvant for cancer treatment. Importantly there has been an increasing number of studies contributing to the mechanistic understanding of aspirins’ anti-tumour effects and these studies continue to inform the potential clinical use of aspirin for both the prevention and treatment of cancer. This review focuses on the emerging role of aspirin as a regulator of metabolic reprogramming, an essential “hallmark of cancer” required to support the increased demand for biosynthetic intermediates needed for sustained proliferation. Cancer cells frequently undergo metabolic rewiring driven by oncogenic pathways such as hypoxia-inducible factor (HIF), wingless-related integration site (Wnt), mammalian target of rapamycin (mTOR), and nuclear factor kappa light chain enhancer of activated B cells (NF-κB), which supports the increased proliferative rate as tumours develop and progress. Reviewed here, cellular metabolic reprogramming has been identified as a key mechanism of action of aspirin and include the regulation of key metabolic drivers, the regulation of enzymes involved in glycolysis and glutaminolysis, and altered nutrient utilisation upon aspirin exposure. Importantly, as aspirin treatment exposes metabolic vulnerabilities in tumour cells, there is an opportunity for the use of aspirin in combination with specific metabolic inhibitors in particular, glutaminase (GLS) inhibitors currently in clinical trials such as telaglenastat (CB-839) and IACS-6274 for the treatment of colorectal and potentially other cancers. The increasing evidence that aspirin impacts metabolism in cancer cells suggests that aspirin could provide a simple, relatively safe, and cost-effective way to target this important hallmark of cancer. Excitingly, this review highlights a potential new role for aspirin in improving the efficacy of a new generation of metabolic inhibitors currently undergoing clinical investigation.

Emilia sonchifolia (L.) DC, it belongs to the family Asteraceae or Compositae, is conventionally used in ethnomedicine, and acquires various medicinal properties. This plant has been regarded as one of the widespread traditional vegetable salads in Malaysia, Bangladesh, and India. In addendum to its avail as a vegetable, the plant has been documented with several medicinal benefits in the extravagance of night blindness, epilepsy, malaria, asthma, burns, breast abscesses, and inflammatory diseases. On scrutinization of their pharmacological properties, it has been revealed that they possess numerous notable biological properties such as antimicrobial, analgesic, anti-inflammatory, antioxidant, hepatoprotective, antianxiety, and anticataract, as well as anticonvulsant activities. Concrete evidence suggests the presence of potential phytochemicals in this plant with a wide range of unknown applications. In this current review, we discuss the phytochemicals present in the plant Emilia sonchifolia and emphasize the therapeutic and pharmacological activities reported so far concerning this plant. [ABSTRACT FROM AUTHOR]

Background: Photodynamic therapy (PDT) plays an immunoregulatory role in tumours. Here, we conducted a retrospective patient analysis to evaluate the effectiveness of PDT plus immune checkpoint inhibitors (ICIs) in gastric cancer. Further, we performed a dynamic analysis of gastric cancer patients receiving PDT to clarify its effects on anti-tumour immunity. Methods: Forty ICI-treated patients that received PDT or not were retrospectively analysed. Five patients with gastric adenocarcinoma were enrolled for sample collection before and after PDT. Single-cell RNA/T cell receptor (TCR) sequencing, flow cytometry and histological exanimation were used to analyse the collected specimens. Results: Patients in PDT group had a significantly better OS after ICI treatment than those in No PDT group. Single-cell analysis identified ten cell types in gastric cancer tissues and four sub-populations of T cells. Immune cell infiltration increased in the tumours after PDT and the circular immune cells showed consistent alterations. TCR analysis revealed a specific clonal expansion after PDT in cytotoxic T lymphocytes (CTL), but a constriction in Tregs. The B2M gene is upregulated in tumour cells after PDT and is associated with immune cell infiltration. Several pathways involving the positive regulation of immunity were enriched in tumour cells in the post-PDT group. The interactions following PDT were increased between tumour cells and effector cells but decreased between Tregs and other immune cells. Some co-stimulatory signaling emerged, whereas co-inhibitory signaling disappeared in intercellular communication after PDT. Conclusions: PDT elicits an anti-tumour response through various mechanisms and is promising as an adjuvant to enhance ICI benefit. [ABSTRACT FROM AUTHOR]

Zhiru Xiu,1 Yiquan Li,1 Jinbo Fang,1 Jicheng Han,1 Shanzhi Li,1 Yaru Li,1,2 Xia Yang,1 Gaojie Song,3 Yue Li,1 Ningyi Jin,1,4,5 Yilong Zhu,1 Guangze Zhu,1 Lili Sun,6 Xiao Li1,4,7 1Academician Workstation of Jilin Province, Changchun University of Chinese Medicine, Changchun, People’s Republic of China; 2Medical College, Yanbian University, Yanji, People’s Republic of China; 3Medical College, Jiujiang· University, Jiujiang, People’s Republic of China; 4Changchun Veterinary Research Institute, Chinese Academy of Agricultural Sciences, Changchun, People’s Republic of China; 5Jiangsu Co-Innovation Center for Prevention and Control of Important Animal Infectious Diseases and Zoonoses, Yangzhou, People’s Republic of China; 6Department of Head and Neck Surgery, Tumor Hospital of Jilin Province, Changchun, People’s Republic of China; 7College of Life Sciences, Shandong Normal University, Jinan, People’s Republic of ChinaCorrespondence: Lili Sun; Xiao Li, Boshuo Road, 1035, Jingyue Economic & Technological Development Zone, Changchun, Jilin, 130122, People’s Republic of China, Tel +86-431-86985923, Fax +86-431-87985861, Email skylee6226@163.com; linjiaxiaoya@163.comObjective: To explore the effects of Esculetin on liver cancer and explore potential mechanisms of Esculetin-inducing cells death.Methods: Esculetin’s effects on the proliferation, migration and apoptosis of HUH7 and HCCLM3 cells were detected by using CCK8, crystal violet staining, wound healing, TranswellTM and Annexin V-FITC/PI. Flow cytometry, fluorescence staining, Western blot, T-AOC, DPPH radical scavenging assay, hydroxyl radical’s inhibitory capability and GSH test were used to examine the esculetin’s effects on the ROS level, the oxidation-related substances and proteins’ expression in hepatoma cells. In vivo experiment was performed by xenograft model. Ferrostatin-1 was used to determine the death way of hepatoma cells induced by esculetin. Live cell probe, Western blot, Fe2+ content, MDA, HE staining, Prussian blue staining and immunohistochemistry were used to examine the ferritinophagy-related phenomenon induced by esculetin in hepatoma cells. The relationship between esculetin and NCOA4-mediated ferritinophagy was confirmed through gene silence and overexpression, immunofluorescence staining and Western blot.Results: Esculetin suppressed the proliferation, migration and apoptosis of HUH7 and HCCLM3 cells significantly, influenced the oxidative stress level, altered the autophagy and iron metabolism levels in cells, and produced a ferritinophagy-related phenomena. Esculetin increased the levels of cellular lipid peroxidation and reactive oxygen species. In vivo, esculetin could decrease tumour volume, promote LC3 and NCOA4 expressions, suppresse hydroxyl radical‘s inhibiting capacity and GSH, increase Fe2+ and MDA levels, decrease antioxidant proteins expression in tumour tissue. In addition, Esculetin could also increase the iron deposition of tumour tissues, promote ferritinophagy, and induce tumours’ ferroptosis.Conclusion: Esculetin has an inhibitory effect on liver cancer in vivo and in vitro through triggering NCOA4 pathway-mediation ferritinophagy.Keywords: esculetin, ferritinophagy, liver cancer, anti-tumour, NCOA4

Berberine (BBR) is a potential plant metabolite and has remarkable anticancer properties. Many kinds of research are being focused on the cytotoxic activity of berberine in in vitro and in vivo studies. A variety of molecular targets which lead to the anticancer effect of berberine ranges from p‐53 activation, Cyclin B expression for arresting cell cycles; protein kinase B (AKT), MAP kinase and IKB kinase for antiproliferative activity; effect on beclin‐1 involved in autophagy; reduced expression of MMP‐9 and MMP‐2 for the inhibition of invasion and metastasis etc. Berberine also interferes with transcription factor‐1 (AP‐1) activity responsible for the expression of oncogenes and neoplastic transformation of the cell. It also leads to the inhibition of various enzymes which are directly or indirectly involved in carcinogenesis like N acetyl transferase, Cyclo‐oxygenase‐2, Telomerase and Topoisomerase. In addition to these actions, Berberine plays a role in, the regulation of reactive oxygen species and inflammatory cytokines in preventing cancer formation. Berberine anticancer properties are demonstrated due to the interaction of berberine with micro‐RNA. The summarized information presented in this review article may help and lead the researchers, scientists/industry persons to use berberine as a promising candidate against cancer. [ABSTRACT FROM AUTHOR]

Abstract Background The plant Kingiodendron pinnatum (DC.) Harms, belonging to the family Fabaceae is endemic to the Western Ghats of India and is commonly used for various ailments, especially by the tribes. K. pinnatum is occasionally used as a substitute for Saraca asoca in Asokarishta, a well-known uterine tonic in Ayurveda. Recent studies revealed a pharmacological similarity between the plants. S. asoca is reported to have anti-cancer properties, but there are no reports on K. pinnatum except for antioxidant and antimicrobial activities. Therefore, the study is aimed to investigate the anticancer potential of the plant. Methods Cytotoxicity of methanolic bark extract of the plant was analysed on different cancer cell lines by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. Dalton's lymphoma ascites (DLA) cell-induced solid and Ehrlich ascites carcinoma (EAC) cell-induced ascites tumour models in mice were used to study the antitumor potential. Phytochemical screening of the extract was also performed. Results The extract was found cytotoxic to DLA, EAC, HCT15, MDA-MB-231, T47D and PC3 with inhibitory concentration (IC50) values of 50.09, 74.74, 67.02, 119.22, 149.04 and 194.5 μg/mL, respectively. In the solid tumour model, a significant (P

Elemene is a second-line broad-spectrum anti-tumour drug that has been used in China for more than two decades. However, its main anti-tumour ingredient, β-elemene, has disadvantages, including excessive lipophilicity and relatively weak anti-tumour efficacy. To improve the anti-tumour activity of β-elemene, based on its minor molecular weight character, we introduced furoxan nitric oxide (NO) donors into the β-elemene structure and designed six series of new generation β-elemene NO donor hybrids. The synthesised compounds could effectively release NO in vitro, displayed significant anti-proliferative effects on U87MG, NCI-H520, and SW620 cell lines. In the orthotopic glioma model, compound Id significantly and continuously suppressed the growth of gliomas in nude mice, and the brain glioma of the treatment group was markedly inhibited (>90%). In short, the structural fusion design of NO donor and β-elemene is a feasible strategy to improve the in vivo anti-tumour activity of β-elemene.

Background: Previous studies have proven that Purinostat Mesylate (PM) is a new HDAC inhibitor and exhibits significant antitumor efficacy. However, the clinical application of PM was greatly limited by its poor solubility in water and low bioavailability.Objective:To increase the solubility of PM through pharmaceutical research, and prepare it into an injection that meets the needs of intravenous use to promote its clinical application.MethodsThe prepared PM/HP-β-CD inclusion complex was studied by computer simulation, fourier transform infrared spectroscopy (FT-IR), nuclear magnetic resonance (1H-NMR spectroscopy), and scanning electron microscopy (SEM). Then, the antitumor effects of PM/HP-β-CD inclusion complex were studied by in vitro cytotoxicity assay, apoptosis assay, pharmacokinetic study and in vivo antitumor assay.Results:Phase Solubility Analysis revealed that PM and HP-β-CD were compatible and the solubility of PM increased almost 220 times, to 2.02 mg/mL. The interaction mechanism studies revealed that PM could be embedded into the cavity of HP-β-CD through the side of the aminobenzene ring. Cell viability and apoptosis assays showed that PM/HP-β-CD complex maintained the good anti-cancer activity of PM, and PM/HP-β-CD complex has a better anti-tumor effect and lower toxicity than LBH589 and Hyper-CVAD/RTX in vivo. All the results suggest that HP-β-CD can solve the problem of PM administration and provide a way for clinical application of PM.Conclusions: In this study, an injectable formulation of PM in HP-β-CD (10% w/v) was prepared to improve its water solubility. Our research provides a way for clinical administration of PM, which has been under phase I clinical trial for the treatment of relapsed or refractory B-cell-related hematologic malignancies in China and the USA.KEY MESSAGESWe developed a preparation of Purinostat Mesylate that can be administered intravenously, reducing the toxicity associated with oral administration.This preparation has an outstanding therapeutic effect on SU-DHL-6 xenograft tumour, indicating its clinical value, which has been under phase I clinical trial for the treatment of relapsed or refractory B-cell-related haematologic malignancies in China and the USA.

A novel series of aminotrimethylpyridinol and aminodimethylpyrimidinol derivatives were designed and synthesised for FGFR4 inhibitors. Structure-activity relationship on the FGFR4 inhibitory activity of the new compounds was clearly elucidated by an intensive molecular docking study. Anti-cancer activity of the compounds was evaluated using hepatocellular carcinoma (HCC) cell lines and a chick chorioallantoic membrane (CAM) tumour model. Compound 6O showed FGFR4 inhibitory activity over FGFR1 − 3. Compared to the positive control BLU9931, compound 6O exhibited at least 8 times higher FGFR4 selectivity. Strong anti-proliferative activity of compound 6O was observed against Hep3B, an HCC cell line which was a much more sensitive cell line to BLU9931. In vivo anti-tumour activity of compound 6O against Hep3B-xenografted CAM tumour model was almost similar to BLU9931. Overall, compound 6O, a novel derivative of aminodimethylpyrimidinol, was a selective FGFR4 kinase inhibitor blocking HCC tumour growth.

Abstract Background As a kind of flavonoid, baicalin (C21H18O11) is extracted from Scutellaria baicalensis Georgi, the extract of which can be added to animal feed in China. Objectives The present review will describe the current understanding of the pharmacological effects of baicalin in the regulation of inflammation, oxidative stress anti‐virus and anti‐tumour responses. Methods We highlight emerging literature that the application in livestock health and performance, the biological activities, the molecular mechanisms and the dosage forms of baicalin by analysing and summarising the main points of the cited literatures. Results It is found that baicalin can improve the functions of multiple physiological systems. Baicalin has a strong anti‐inflammatory effect by regulating TLR4‐NFκB‐MAPK signalling pathway; it also can reduce oxidative stress by regulating Nrf2–Keap1 pathway; it can inhabit many kinds of virus such as influenza virus, respiratory virus, hepacivirus and others; it can also inhibit the growth of tumour cells by blocking the cell cycle or inducing apoptosis; and new dosage forms such as cationic solid lipid nanoparticles, cyclodextrin inclusion complexes or nanocrystalline can be applied to improve the deficiency of baicalin. Conclusions In summary, these studies have elucidated a comprehensive report on the anti‐inflammatory, anti‐oxidant, anti‐virus and anti‐tumour of baicalin, these findings thus indicated that baicalin can be used effectively to the field of animal production in future when the appropriate dosage form is determined.

Background: The plant Kingiodendron pinnatum (DC.) Harms, belonging to the family Fabaceae is endemic to the Western Ghats of India and is commonly used for various ailments, especially by the tribes. K. pinnatum is occasionally used as a substitute for Saraca asoca in Asokarishta, a well-known uterine tonic in Ayurveda. Recent studies revealed a pharmacological similarity between the plants. S. asoca is reported to have anti-cancer properties, but there are no reports on K. pinnatum except for antioxidant and antimicrobial activities. Therefore, the study is aimed to investigate the anticancer potential of the plant. Methods: Cytotoxicity of methanolic bark extract of the plant was analysed on different cancer cell lines by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. Dalton's lymphoma ascites (DLA) cell-induced solid and Ehrlich ascites carcinoma (EAC) cell-induced ascites tumour models in mice were used to study the antitumor potential. Phytochemical screening of the extract was also performed. Results: The extract was found cytotoxic to DLA, EAC, HCT15, MDA-MB-231, T47D and PC3 with inhibitory concentration (IC50) values of 50.09, 74.74, 67.02, 119.22, 149.04 and 194.5 μg/mL, respectively. In the solid tumour model, a significant (P < 0.001) reduction in tumour weight of 0.7 ± 0.15 g was observed in 500 mg/kg b.wt. extract treated group compared to the control group (3.6 ± 0.24 g) by oral administration for 30 days. In the ascites tumour model, a high survival rate of 28.2 ± 8.72 days (P < 0.01) was found by the extract treatment compared to the control animals. Phytochemicals like alkaloids, flavonoids, phenols, phytosterols, saponins, tannins, steroids and terpenoids were detected in the extract. Conclusion: Results obtained by the cytotoxic and anti-tumour studies revealed the anticancer potential of K. pinnatum. The plant exhibits more cytotoxicity towards cancer cell lines of the reproductive system such as the breast and prostate. [ABSTRACT FROM AUTHOR]

Using STAT3 inhibitors as a potential strategy in cancer therapy have attracted much attention. Recently, celastrol has been reported that it could directly bind to and suppress the activity of STAT3 in the cardiac dysfunction model. To explore more effective STAT3 inhibiting anti-tumour drug candidates, we synthesised a series of celastrol derivatives and biologically evaluated them with several human cancer cell lines. The western blotting analysis showed that compound 4m, the most active derivative, could suppress the STAT3's phosphorylation as well as its downstream genes. SPR analysis, molecular docking and dynamics simulations' results indicated that the 4m could bind with STAT3 protein more tightly than celastrol. Then we found that the 4m could block cell-cycle and induce apoptosis on HCT-116 cells. Furthermore, the anti-tumour effect of 4m was verified on colorectal cancer organoid. This is the first research that discovered effective STAT3 inhibitors as potent anti-tumour agents from celastrol derivatives. [ABSTRACT FROM AUTHOR]

A novel series of aminotrimethylpyridinol and aminodimethylpyrimidinol derivatives were designed and synthesised for FGFR4 inhibitors. Structure-activity relationship on the FGFR4 inhibitory activity of the new compounds was clearly elucidated by an intensive molecular docking study. Anti-cancer activity of the compounds was evaluated using hepatocellular carcinoma (HCC) cell lines and a chick chorioallantoic membrane (CAM) tumour model. Compound 6O showed FGFR4 inhibitory activity over FGFR1 -- 3. Compared to the positive control BLU9931, compound 6O exhibited at least 8 times higher FGFR4 selectivity. Strong anti-proliferative activity of compound 6O was observed against Hep3B, an HCC cell line which was a much more sensitive cell line to BLU9931. In vivo anti-tumour activity of compound 6O against Hep3B-xenografted CAM tumour model was almost similar to BLU9931. Overall, compound 6O, a novel derivative of aminodimethyl-pyrimidinol, was a selective FGFR4 kinase inhibitor blocking HCC tumour growth. [ABSTRACT FROM AUTHOR]

Background: Previous studies have proven that Purinostat Mesylate (PM) is a new HDAC inhibitor and exhibits significant antitumor efficacy. However, the clinical application of PM was greatly limited by its poor solubility in water and low bioavailability. Objective:To increase the solubility of PM through pharmaceutical research, and prepare it into an injection that meets the needs of intravenous use to promote its clinical application. MethodsThe prepared PM/HP-β-CD inclusion complex was studied by computer simulation, fourier transform infrared spectroscopy (FT-IR), nuclear magnetic resonance (1H-NMR spectroscopy), and scanning electron microscopy (SEM). Then, the antitumor effects of PM/HP-β-CD inclusion complex were studied by in vitro cytotoxicity assay, apoptosis assay, pharmacokinetic study and in vivo antitumor assay. Results:Phase Solubility Analysis revealed that PM and HP-β-CD were compatible and the solubility of PM increased almost 220 times, to 2.02 mg/mL. The interaction mechanism studies revealed that PM could be embedded into the cavity of HP-β-CD through the side of the aminobenzene ring. Cell viability and apoptosis assays showed that PM/HP-β-CD complex maintained the good anti-cancer activity of PM, and PM/HP-β-CD complex has a better anti-tumor effect and lower toxicity than LBH589 and Hyper-CVAD/RTX in vivo. All the results suggest that HP-β-CD can solve the problem of PM administration and provide a way for clinical application of PM. Conclusions: In this study, an injectable formulation of PM in HP-β-CD (10% w/v) was prepared to improve its water solubility. Our research provides a way for clinical administration of PM, which has been under phase I clinical trial for the treatment of relapsed or refractory B-cell-related hematologic malignancies in China and the USA. We developed a preparation of Purinostat Mesylate that can be administered intravenously, reducing the toxicity associated with oral administration. This preparation has an outstanding therapeutic effect on SU-DHL-6 xenograft tumour, indicating its clinical value, which has been under phase I clinical trial for the treatment of relapsed or refractory B-cell-related haematologic malignancies in China and the USA. [ABSTRACT FROM AUTHOR]

The sclerotium of Lignosus rhinocerus (Cooke) Ryvarden is used by the local communities in Southeast Asia and China to treat cancer, asthma, fever, and other ailments based on traditional knowledge. The sclerotial water extracts were previously reported to exhibit cytotoxic, apoptotic, and immunomodulatory activities – providing a scientific basis for its use in treating cancer; however, there is still a lack of evidence on its potential anti-angiogenic activity. This study aimed to investigate the toxicity, anti-angiogenic, and anti-tumour activities of the hot-water and cold-water extracts of L. rhinocerus using HCT116 human colorectal carcinoma cells implanted in the chick chorioallantoic membrane (CAM) model. The toxicity of L. rhinocerus extracts towards the chick embryos was determined 24 h post-treatment. The anti-angiogenic activity of the extracts was then investigated at 0.1–10 μg/embryo (6.7–670 μg/mL) at targeted blood vessels. The anti-tumour effect of selected extracts against the HCT116 human colorectal carcinoma cells xenografted onto the chick embryos was also studied. The cold-water extracts of L. rhinocerus displayed strong in ovo toxicity (LC 50 : 1.2–37.7 μg/mL) while the hot-water extracts are non-toxic up to 670 μg/mL. Among the extracts, the hot-water extracts demonstrated the highest anti-angiogenic activity with 44.0 ± 17.7% reduction of capillary diameter (relative to the saline-treated control). Moreover, treatment of the HCT116 cells xenografted onto the chick embryos with the hot-water extracts resulted in smaller tumour size and lower number of blood vessels compared to the saline-treated control. The hot-water extracts of L. rhinocerus sclerotium demonstrated anti-angiogenic and anti-tumour activities but most of the cold-water extracts at similar concentrations were devoid of that. Our findings provide further scientific validation of the medicinal use of the sclerotium in treating cancer and thus, expanding our knowledge on the possible mechanism of its anti-cancer effect apart from direct cytotoxicity, induction of apoptosis and immunomodulation that have been studied thus far. [Display omitted] • Lignosus rhinocerus cold water extracts exhibited strong in ovo toxicity in CAM model. • Lignosus rhinocerus hot water extracts displayed high antiangiogenic activity in CAM model. • Lignosus rhinocerus hot water extracts suppressed the growth of HCT116 cells xenografted on chick embryos. [ABSTRACT FROM AUTHOR]

Cancer is a condition in which cells grow uncontrollably and may metastasis to other parts of the body. Despite the recent advances in synthesising new anticancer agents, plant-derived compounds are traditionally considered as the primary health care approaches in some parts of the world. Eucalyptus-derived essential oils are the rich resources of active phytochemicals, which have been used for treating or preventing different ailments. However, there is less literature addressing the bioactivity of Eucalyptus-derived phytochemicals in the treatment of cancers. In this review paper, we summarised the existing evidence on the wide-spectrum activity of Eucalyptus-derived essential oil against malignancies. Our review highlighted that Eucalyptus-derived essential oil contains a wide variety of secondary metabolites, and thus capable of slowing or inhibiting the cancerous cell lines in vitro and in vivo conditions. We also summarized the achievement in the anti-tumour activity of nanoparticles, the application of plant-based essential oils in food safety, and the application of green extraction technologies. It can be concluded that Eucalyptus has immense potential to cure malignancies, and such information can be used in further studies. Notwithstanding the advantages, Eucalyptus-derived essential oils can be poisonous; therefore, more evidence is still required to confirm the efficacy of Eucalyptus-derived essential oil. [ABSTRACT FROM AUTHOR]

Background: As a kind of flavonoid, baicalin (C21H18O11) is extracted from Scutellaria baicalensis Georgi, the extract of which can be added to animal feed in China. Objectives: The present review will describe the current understanding of the pharmacological effects of baicalin in the regulation of inflammation, oxidative stress anti‐virus and anti‐tumour responses. Methods: We highlight emerging literature that the application in livestock health and performance, the biological activities, the molecular mechanisms and the dosage forms of baicalin by analysing and summarising the main points of the cited literatures. Results: It is found that baicalin can improve the functions of multiple physiological systems. Baicalin has a strong anti‐inflammatory effect by regulating TLR4‐NFκB‐MAPK signalling pathway; it also can reduce oxidative stress by regulating Nrf2–Keap1 pathway; it can inhabit many kinds of virus such as influenza virus, respiratory virus, hepacivirus and others; it can also inhibit the growth of tumour cells by blocking the cell cycle or inducing apoptosis; and new dosage forms such as cationic solid lipid nanoparticles, cyclodextrin inclusion complexes or nanocrystalline can be applied to improve the deficiency of baicalin. Conclusions: In summary, these studies have elucidated a comprehensive report on the anti‐inflammatory, anti‐oxidant, anti‐virus and anti‐tumour of baicalin, these findings thus indicated that baicalin can be used effectively to the field of animal production in future when the appropriate dosage form is determined. [ABSTRACT FROM AUTHOR]

Despite its low prevalence, pancreatic cancer (PC) is one of the deadliest, typically characterised as silent in early stages and with a dramatically poor prognosis when in its advanced stages, commonly associated with a high degree of metastasis. Many efforts have been made in pursuing innovative therapeutical approaches, from the search for new cytotoxic drugs and other bioactive compounds, to the development of more targeted approaches, including improved drug delivery devices. Marine biotechnology has been contributing to this quest by providing new chemical leads and materials originating from different organisms. In this review, marine biodiscovery for PC is addressed, particularly regarding marine invertebrates (namely sponges, molluscs, and bryozoans), seaweeds, fungi, and bacteria. In addition, the development of biomaterials based on marine-originating compounds, particularly chitosan, fucoidan, and alginate, for the production of advanced cancer therapies, is also discussed. The key role that drug delivery can play in new cancer treatments is highlighted, as therapeutical outcomes need to be improved to give further hope to patients. [ABSTRACT FROM AUTHOR]

Objectives Cervical cancer (CC) is the common female malignant tumour with non-negligible morbidity and mortality. Eleutheroside E (EE) has anti-oxidative stress, anti-inflammatory and anti-proliferation effects in diverse disease models. However, its anti-tumour role remains unclear. Methods The cell viability, apoptosis rate and protein expressions were detected by CCK-8, flow cytometry and western blot assays, respectively. The metabolic profile was performed by GC/MS analysis. Furthermore, the effect of EE on CC was verified in nude mice. Key findings EE notably decreased the viability and increased the cell apoptosis, which could be reversed with 740Y-P treatment. EE treatment changed the metabolic categories of SiHa cells. The fatty acids signalling pathway was the most outstanding differential pathway. Myo-inositol prominently enhanced the level of phosphorylated Akt in a dose-dependent way. Moreover, EE declined the tumour volume and weight and the proliferation, but promoted the apoptosis in vivo. EE reduced the relative expression of phosphorylated PI3K and Akt. However, all these in-vivo results were observably antagonized with myo-inositol treatment. Conclusions EE plays an anti-tumour role in CC via inhibiting the PI3K pathway and reprogramming the metabolic responses. [ABSTRACT FROM AUTHOR]

Glucose-6-phosphate dehydrogenase (G6PD) is a pentose phosphate pathway (PPP) enzyme that generates NADPH, which is required for cellular redox equilibrium and reductive biosynthesis. It has been demonstrated that abnormal G6PD activation promotes cancer cell proliferation and metastasis. To date, no G6PD inhibitor has passed clinical testing successfully enough to be launched as a medicine. As a result, in this investigation, cannabinoids were chosen to evaluate their anticancer potential by targeting G6PD. Molecular docking indicated that three molecules, Tetrahydrocannabinolic acid (THCA), Cannabichromenic acid (CBCA), and tetrahydrocannabivarin (THCV), have the highest binding affinities for G6PD of -8.61, -8.39, and 8.01 Kcal mol. ADMET analysis found that all of them were safe prospective drug candidates. Molecular dynamics (MD) simulation and MM-PBSA analysis confirm the structural compactness and lower conformational variation of protein-ligand complexes, thereby maintaining structural stability and rigidity. Thus, our in silico investigation exhibited all three cannabinoids as potential competitive inhibitors of G6PD., (© 2024 Wiley-VHCA AG, Zurich, Switzerland.)

Reproductive toxicity from food and environmental contaminants has greatly affected human life. Plants are a fundamental source of bioactive components for relieving the harmful effects of pollutants. Hydrazine metabolites pose health threats when they enter the food chain. Croton tiglium ( C. tiglium ) exhibits anti-inflammatory and anti-tumor properties. Silver nanoparticles enhance the chemical stability of C. tiglium . Reproductive toxicity of Azoxymethane (AOM) and anticancer effects of silver C. tiglium were evaluated. Thirty-six adult female rats were divided into six groups ( n = 6 ) and treated with AOM with or without silver C. tiglium nano-extract as pre- and post-treatment. Sexual hormones and proteins were assessed under silver C. tiglium nano-extract and AOM. Histopathologically, AOM caused metaplastic myometrial endometriotic cysts and endometrial metaplasia. Silver C. tiglium in pre- and post-treated rats mitigated the carcinogenic effects of AOM. Immunohistochemically, AOM carcinogenicity was evident through moderate detection of the CK-7 tumor marker in the ovaries and uterus of the AOM-, simultaneous-, and post-treated groups. C. tiglium ameliorated this, with CK-7 slightly expressed in the pre-treated group. Furthermore, C. tiglium alleviated the negative impact on FSH, LH, and 17-β estradiol hormones. In conclusion, Silver C. tiglium nano-extract successfully prevented tumors in the ovaries and uterus of AOM-treated rats., Competing Interests: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (© 2024 The Authors.)

Epimedium Folium has been extensively utilized for medicinal purposes in China for a significant period. This review undertakes a comprehensive examination of literature pertaining to Epimedium and its metabolites over the past decade, drawing from databases such as PubMed. Through meticulous organization and synthesis of pertinent research findings, including disease models, pharmacological effects, and related aspects, this narrative review sheds light on the principal pharmacological activities and associated mechanisms of Epimedium in safeguarding the reproductive system, promoting bone health, mitigating inflammation, and combating tumors and viral infections. Consequently, this review contributes to a more profound comprehension of the recent advances in Epimedium research., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (Copyright © 2024 Cui, Lin, Hao, Shi, Gao, Yang, Yang, Wu, Gao, Ru, Li, Xiao, Gao and Wang.)

Background: Epidemiological studies suggest that metformin reduces the risk of developing several types of cancer, including gliomas, and improves the overall survival in cancer patients. Nevertheless, while the effect of metformin on cancer cells has been extensively studied, its impact on other components of the tumour microenvironment, such as macrophages, is less understood., Results: Metformin-treated mouse bone marrow cells differentiate into spindle-shaped macrophages exhibiting increased phagocytic activity and tumour cell cytotoxicity coupled with modulated expression of co-stimulatory molecules displaying reduced sensitivity to inflammatory cues compared with untreated cells. Transcriptional analyses of metformin-treated mouse bone marrow-derived macrophages show decreased expression levels of pro-tumour genes, including Tgfbi and Il1β , related to enhanced mTOR/HIF1α signalling and metabolic rewiring towards glycolysis., Significance: Our study provides novel insights into the immunomodulatory properties of metformin in macrophages and its potential application in preventing tumour onset and in cancer immunotherapy., Competing Interests: The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest., (© 2024 The Authors.)

The objective of this work is to provide an overview of the numerous pharmacological features that are associated with the pteridine molecule. Pteridines are nitrogen-containing heterocyclic compounds that are well-known and noteworthy. Their chemical formula is C6H4N4. In recent years, pteridine's various potential uses in the field of medicinal chemistry research have garnered significant attention. In the expanding field of intensive study, Pteridine is regarded as a privileged scaffold, and the alteration created with diverse substituents around the centroid opened the way for researchers to deal with it at ease. The heterocycle, which is a fused ring, has a high pharmacological quality. A pteridine is one of the heterocycles that has attracted a lot of interest in terms of biological uses. The pteridine nucleus serves as the quintessential framework in a range of physiologically energetic chemicals and pharmacological molecules. This evaluation is necessary in order to bring to light the remarkable potential that this ring device possesses as a result of the wide variety of pharmacological effects it may perform. This research might unquestionably hasten the graph and synthesis procedures, which would ultimately yield in a wide array of therapeutically feasible medicinal options. [ABSTRACT FROM AUTHOR]

Daratumumab (DAR) is novel human anti-CD38 IgG1, high-affinity human monoclonal antibody having broad-spectrum killing activity. The antibody is recommended to treat multiple myeloma. Recently Antibody-dependent cellular phagocytosis (ADCP) have been identified as the potential mechanism of DAR in addition to complement-dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC). In the present study we evaluated the effect of Daratumumab on other effector cells of multiple myeloma. Luciferase+ MM.1R GFP cells were selected for the study. For immune-compromised multiple myeloma tumour xenograft mouse model we used severe combined immunodeficient beige (SCID-beige), NOD SCID gamma (NSG) and C57Bl/6j mice. Bioluminescence imaging was carried by injecting luciferin, and in vivo confocal microscopy was done for tracing bone marrow niches. Spleen and tumours were submitted to immunophenotypic analysis. MTT assay was done for cell proliferation studies. We established tumour xenograft mouse model. It was found that DAR showed significant anti-tumour effect in tumour xenograft multiple myeloma mice. We found that DAR showed anti-tumour activity via Fc–FcγR interaction with macrophages. DAR induced phenotypic activation of macrophages in mice and resulted in ADCP of cancerous cells via interacting Fc-FcγR in vitro. The study suggested that DAR exerted anti-tumour activity in multiple myeloma by interacting with Fc-FcγR. [ABSTRACT FROM AUTHOR]

Background: Tumours are among the most lethal diseases that heavily endanger human health globally. Xuefu Zhuyu Decoction (XFZYD) is a prescription used to treat bloodactivating stasis. Although XFZYD has been shown to suppress migration and invasion of tumour cells, the active ingredients, potential targets, and underlying mechanism remain largely elusive. Purpose: To identify the prospective ingredients and major targets of XFZYD against tumours, and evaluate the efficacy and potential molecular mechanisms of XFZYD extract on tumour growth and invasion. Methods: We predicted that XFZYD might act on 80 targets through 128 active components using the network pharmacology analysis method. In addition, we prepared an XFZYD aqueous extract and employed the RasV12/lgl-/--induced Drosophila tumour model to carry out experimental verification. Results: XFZYD did not exhibit any side effects on development, viability, and fertility. Furthermore, XFZYD significantly impeded tumour size and invasion at moderate concentrations and suppressed the increased phosphorylation of JNK but strongly enhanced the expression of Caspase 3 in the RasV12/lgl-/- model. Finally, the mRNA level of the transcription complex AP-1 component c-FOS was remarkably reduced. In contrast, the transcription of three pro-apoptotic genes was significantly increased when XFZYD was used to treat the tumour model. Conclusion: The study findings suggest that XFZYD may promote tumour cell apoptosis by activating caspase signalling to control primary growth and hinder tumour cell invasion by suppressing JNK/AP-1 signalling activity, thus providing a potential therapeutic strategy for XFZYD in the clinical treatment of cancer and other related diseases. [ABSTRACT FROM AUTHOR]

Background: Inappropriate repair of DNA damage drives carcinogenesis. Lymphoid-specific helicase (HELLS) is an important component of the chromatin remodeling complex that helps repair DNA through various mechanisms such as DNA methylation, histone posttranslational modification, and nucleosome remodeling. Its role in human cancer initiation and progression has garnered recent attention. Our study aims to provide a more systematic and comprehensive understanding of the role of HELLS in the development and progression of multiple malignancies through analysis of HELLS in cancers. Methods: We explored the role of HELLS in cancers using The Cancer Genome Atlas (TCGA) and Genotype-Tissue Expression (GTEx) database. Multiple web platforms and software were used for data analysis, including R, Cytoscape, HPA, Archs4, TISIDB, cBioPortal, STRING, GSCALite, and CancerSEA. Results: High HELLS expression was found in a variety of cancers and differentially expressed across molecular and immune subtypes. HELLS was involved in many cancer pathways. Its expression positively correlated with Th2 and Tcm cells in most cancers. It also correlated with genetic markers of immunomodulators in various cancers. Conclusions: Our study elucidates the role HELLS plays in promotion, inhibition, and treatment of different cancers. HELLS is a potential cancer diagnostic and prognostic biomarker with immune, targeted, or cytotoxic therapeutic value. This work is a prerequisite to clinical validation and treatment of HELLS in cancers. [ABSTRACT FROM AUTHOR]

BackgroundInappropriate repair of DNA damage drives carcinogenesis. Lymphoid-specific helicase (HELLS) is an important component of the chromatin remodeling complex that helps repair DNA through various mechanisms such as DNA methylation, histone posttranslational modification, and nucleosome remodeling. Its role in human cancer initiation and progression has garnered recent attention. Our study aims to provide a more systematic and comprehensive understanding of the role of HELLS in the development and progression of multiple malignancies through analysis of HELLS in cancers.MethodsWe explored the role of HELLS in cancers using The Cancer Genome Atlas (TCGA) and Genotype-Tissue Expression (GTEx) database. Multiple web platforms and software were used for data analysis, including R, Cytoscape, HPA, Archs4, TISIDB, cBioPortal, STRING, GSCALite, and CancerSEA.ResultsHigh HELLS expression was found in a variety of cancers and differentially expressed across molecular and immune subtypes. HELLS was involved in many cancer pathways. Its expression positively correlated with Th2 and Tcm cells in most cancers. It also correlated with genetic markers of immunomodulators in various cancers.ConclusionsOur study elucidates the role HELLS plays in promotion, inhibition, and treatment of different cancers. HELLS is a potential cancer diagnostic and prognostic biomarker with immune, targeted, or cytotoxic therapeutic value. This work is a prerequisite to clinical validation and treatment of HELLS in cancers.

Objectives: Plant-derived flavonolignans had been demonstrated to have various biological functions. They are an important class of natural products combined by a flavonoid unit and a phenylpropanoid unit. Key findings: From the literature survey, 88 constituents from natural resources were identified. Different derivatives of flavonolignans were listed, fused phenylpropanoid unit with dioxane ring, or cyclic ether, or simple ether side chain, or lactone, and so on. Besides, the pharmacological effects of flavonolignans were summarized as well. It has a wide range of anti-tumour, antioxidant, anti-microorganic and anti-inflammatory effects. Summary: This review had provided a full-scale profile of flavonolignans on its plant sources, phytochemistry and pharmacology, and also proposed some issues and perspectives which may be of concern in the future. It was greatly anticipated that the commercialization of the flavonolignans would lead to uplift the financial abilities of communities attending the growing of the flavonolignans and the relevant and potential production becoming an international herbal and pharmaceutical commodity. [ABSTRACT FROM AUTHOR]

Introduction: To conduct a retrospective data collection on prevalence of functional food lentinan as its role in anti-cancer therapies and management of carcinomas. Methods: The methodical review was carried out on various indexed databases Scopus, Web of sciences and Pubmed, in addition to the Google Scholar database. The work focuses on observational studies like anti-tumour, cytotoxic and immunomodulating of functional food lentinan. Results: World Health Organisation (WHO) classifies cancer as the second leading cause of death worldwide, approximately 1 in 6 deaths occurring are because of cancer, and WHO estimates ∼14.1 million new cancer cases and ∼10 million deaths per year. In recent years’ natural products like mushrooms have emerged as an anti-cancer and immunomodulating agent and have overcome the drawbacks of conventional chemotherapeutic strategies. Similarly, Lentinan (LNT) a bioactive molecule obtained from Lentinus edodes with a chemical backbone of β -1, 3-glucan with two β -1, 6-glucose chains. The literature has suggested lentinan as a chemotherapeutic has improved quality of life and has promoted the efficacy of chemotherapy and radiation therapy during cancer treatment. The anti-tumour and biological response modifier and the ability of immunoregulation of lentinan have drawn the attraction to oncologists and pharmacologists Conclusion: Hence this review describes the possible mechanism of Lentinan as anti-tumour, cytotoxic and immunomodulating moiety in treating various cancers.

Background & objectives: Gastric mucosa-associated lymphoid tissue (MALT) lymphoma is a common marginal zone lymphoma. The stomach is the relatively common origin of the MALT lymphoma, now termed as extranodal marginal zone B-cell lymphoma. Gastric MALT lymphoma has good prognosis due to clinical response to treatment and favourable overall survival. In this study, clinical characteristics and treatment of patients of early gastric MALT lymphoma were retrospectively analysed. Methods: Seventy patients with stages I–II MALT-lymphoma treated from April 2003 to August 2015 were included. The most common symptoms were abdominal discomfort, nausea, vomiting and other digestive symptoms. Helicobacter pylori eradication was done in patients with proven H. pylori infection. Patients in whom H. pylori eradication therapy was not effective, alternative treatments options including chemotherapy, radiotherapy and surgery, were given. Results: Fifty two patients with H. pylori infection underwent anti-H. pylori therapy, the total effective rate of anti-H. pylori treatment was 92.3 per cent (48/52). Thirty two patients were given anti-tumour treatment, including chemotherapy, radiotherapy and surgery. The total effective rate was 90.6 per cent (29/32). The five-year overall survival rate and five-year progression-free survival rate were 93.4 and 84.2 per cent, respectively. Interpretation & conclusions: For patients with early gastric MALT lymphoma, anti-H. pylori treatment may be effective. Patients with poor results of anti-H. pylori treatment need to be treated with anti-tumour therapy. [ABSTRACT FROM AUTHOR]

Despite its low prevalence, pancreatic cancer (PC) is one of the deadliest, typically characterised as silent in early stages and with a dramatically poor prognosis when in its advanced stages, commonly associated with a high degree of metastasis. Many efforts have been made in pursuing innovative therapeutical approaches, from the search for new cytotoxic drugs and other bioactive compounds, to the development of more targeted approaches, including improved drug delivery devices. Marine biotechnology has been contributing to this quest by providing new chemical leads and materials originating from different organisms. In this review, marine biodiscovery for PC is addressed, particularly regarding marine invertebrates (namely sponges, molluscs, and bryozoans), seaweeds, fungi, and bacteria. In addition, the development of biomaterials based on marine-originating compounds, particularly chitosan, fucoidan, and alginate, for the production of advanced cancer therapies, is also discussed. The key role that drug delivery can play in new cancer treatments is highlighted, as therapeutical outcomes need to be improved to give further hope to patients.

Background: Bacopaside II is one of the four triterpenoid saponin components of bacoside A, the major bioactive constituent in the medicinal herb, Bacopa monnieri. Purpose: The present study is aimed to investigate the effect of PLGA-PEG encapsulated bacopaside II nanoparticles (BM1NPs) on C6 glioma cells. Methods: Bacopaside II was isolated from B. monnieri using sequential extraction followed by fractionation, column chromatography and characterized by FTIR and NMR. BM1NPs were prepared by nanoprecipitation and their physicochemical characterization was carried out by DLS, XRD, TEM and zeta potential analyses. Results: The spherical nanoparticles showed optimum size range, negative zeta potential and slow but significant in vitro release profile. BM1NPs (100–300 µg/mL) on MTT assay displayed 30–90% cell cytotoxicity against C6 glioma cells. In 2′,7′-dichlorodihydrofluorescein diacetate (H2DCFDA) assay, BM1NP-treated cells showed more intracellular reactive oxygen species (ROS). The apoptosis-inducing property was evaluated by annexin V Alexa fluor 488 staining. EdU (5-ethynyl-2’-deoxyuridine) assay on C6 glioma cells confirmed the antiproliferative potential of BM1NPs. Cell cycle analysis by quantitation of DNA content showed the appearance of sub-G1 peak and confirmed the occurrence of apoptosis. Conclusion: Our results indicate that BM1NPs significantly inhibited C6 glioma cell proliferation and promoted cell apoptosis.

Lung cancer is one of the most common types of cancer in the world, and it represents a significant percentage of all diagnosed cancers. Despite better clinical outcomes associated with current drugs, lung cancer has a worse survival rate than any of the other commonly occurring malignancies. Evidence suggests that natural products offer promising potential for improving the current treatment approaches and/or developing novel treatment strategies. Bee products such as honey, propolis, and venom have been reported to exert anti-cancer effects on a variety of human cancer cell lines, thereby paving the way for a wide range of treatment possibilities. The current review focuses on the cytotoxic effects of bee bioactive compounds on all types of cancer, and the molecular pathways by which they might reduce tumor cell growth or trigger apoptosis of cancer cells, with particular reference to lung cancer. This strategy could potentially improve the efficacy of current remedies, reduce the doses of chemotherapy drugs, and decrease adverse effects of chemotherapy drugs. Furthermore, in vitro studies on anti-cancer properties of bee products are carefully reviewed. The results reveal that bee products have the potential to become effective treatment agents against many forms of cancer in the future. [ABSTRACT FROM AUTHOR]

Chemotherapy, the most common class of anticancer drugs, is considerably limited owing to its adverse side effects. In this study, we aimed to evaluate the protective effect and mechanism of action of large-leaf yellow tea polysaccharides (ULYTP-1, 1.29 × 104 Da) against chemotherapeutic 5-fluorouracil (5-Fu). Structural characterisation revealed that ULYTP-1 was a β-galactopyranouronic acid. Furthermore, ULYTP-1 promoted autolysosome formation, activating autophagy and reducing the oxidative stress and inflammation caused by 5-Fu. Our in vivo study of 4 T1 tumour-bearing mice revealed that ULYTP-1 also attenuated 5-Fu toxicity through modulation of the gut microbiota. Moreover, ULYTP-1 effectively protected immune organs and the liver from 5-Fu toxicity, while promoting its tumour-inhibitory properties. The current findings provide a new strategy for optimising chemotherapy regimens in the clinic. [Display omitted] • Polysaccharide ULYTP-1 was extracted from large-leaf yellow tea. • ULYTP-1 is a β-galactopyranouronic acid with a spongy steric configuration. • ULYTP-1 activates autophagy to alleviate 5-fluorouracil-induced liver injury. • ULYTP-1 alleviated gut dysbiosis in 4 T1 tumour-bearing mice. [ABSTRACT FROM AUTHOR]

Tongue cancer has a very high incidence in China, and there is a need to develop new anti-tumour drugs against it. We synthesised 31 novel quinoline derivatives to test their anti-tumour activity. A compound referred to as " f25 " was identified through screening for its high in vitro toxicity against an oral squamous carcinoma cell line (CAL-27). f25 exhibited significant cytotoxicity against CAL-27 cells (IC 50 = 7.70 ± 0.58 μΜ). f25 also inhibited the migration and invasion of CAL-27 cells to a level comparable with that of the chemotherapy agent cisplatin. Moreover, f25 promoted the apoptosis of CAL-27 cells. Transcriptome sequencing and western blotting showed that the mechanism of action of f25 against CAL-27 cells involved the peroxisome proliferator-activated receptor (PPAR) signalling pathway. Specifically, f25 could bind to PPAR-α, PPAR-β, and PPAR-γ and increase their expression. In vivo experiments showed that treatment with f25 led to a reduction in tumour volume in nude mice without significant toxicity. Overall, this study highlights the potential of quinoline compounds (particularly f25) for the design and synthesis of anti-tumour drugs. It also underscores the importance of the PPAR signalling pathway as a target for potential cancer therapies. [Display omitted] • f25 exhibits high cytotoxicity against tongue squamous cell carcinoma cell line CAL-27 cells. • f25 significantly inhibited the migration and invasion of CAL-27 cells and promoted apoptosis. • f25 acts on CAL-27 cells by activating the PPAR signalling pathway thereby exerting an anti-tumour effect. • f25 inhibits tumour growth in a nude mouse model and has a high biosafety profile. [ABSTRACT FROM AUTHOR]

Pancreatic ductal adenocarcinoma (PDAC) is the fourth leading cause of cancer-associated death in the United States and has a 5-year survival rate of