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1.
Article | IMSEAR | ID: sea-231598

RÉSUMÉ

Oyster mushrooms (Pleurotus ostreatus), are included in the category of nutritious foods, due to the presence of vitamins, proteins and different kinds of chemicals which preserve good health. It exhibited several medicinal properties like, anti-tumor, immune modulatory, anti-inflammatory, anti-arthritic, hypo-cholesterolaemic, anti-diabetic, anti-oxidant, anti-hypertensive, antiviral and antimicrobial activities. The current study was aimed at the identification of phytochemicals by suitable methodology followed by molecular docking studies and the effect of test extract on different cell lines. Preliminary phytochemical testing was conducted; identification of different phytochemicals was carried out by GC-MS method. The protein 1DI8 (CDK-2) from the Protein Data Bank was used to analyse the molecular docking investigation of the identified phytochemicals. In the present study, the methanolic extract of Pleurotus ostreatus contained six compounds - Propanedioic acid, phenyl-, Cyclopropanecarboxylic acid, 1-amino-, 2-Undecene, 4,5-dimethyl-, [R*,R*-(E Heptanoic acid, 2-methyl-2-butyl ester, Acetic acid, 2-propyltetrahydropyran-3,3-Tetradecene. Amongst all of these phytochemicals, Propanedioic acid, and phenyl-was shown to possess the highest score with 1DI8 (CDK-2) in the molecular docking investigation. Anti-cancer effect was also evaluated; the test extract was found to possess the same activity which was evident by the IC50 values. It was concluded that Pleurotus ostreatus possessed six phytochemicals, out of which Propanedioic acid, phenyl was found to have therapeutic potential in the treatment of cancers and was proved by locking mechanism through molecular docking studies. As Pleurotus ostreatus is known for higher biomass availability, further research is of utmost importance in the treatment of cancers.

2.
Article | IMSEAR | ID: sea-231595

RÉSUMÉ

Noble bimetallic nanoparticles (BNPs) exhibit strong anticancer and antibacterial activities. They are known to be stable, less toxic, environmental friendly and biocompatible nature. Due to their enhanced biological properties, they are well suits for the biomedical applications such as cancer therapy, gene therapy and drug delivery. In the current study, we examine the anticancer and antibacterial potential of bio-mediated mono and bimetallic nanoparticles. Here, aqueous Capsicum annuum leaf extract was employed as a good reducing and capping agent for producing Ag, Au monometallic, and Ag-Au bimetallic nanoparticles. The formation of C.A- Ag, Au MPNs and Ag-Au BNPs was initially confirmed by visible color change of the reaction mixture and UV-Visible spectra show the Surface Plasmon Resonance (SPR) band observed at 543 nm. Furthermore, phytofabrication, crystallinities, structural alignments, particle size and elemental composition were studied by following standard physico-chemical techniques such as FT-IR (Fourier Transform Infrared), XRD (X-Ray diffraction), HR-TEM (High resolution-Transmission Electron Microscopy), SEM-EDX (Scanning Electron Microscopy and Energy- dispersive X-Ray Spectroscopy) respectively. The results were obtained from various characterization techniques confirmed that the C.A. mediated Ag, Au MNPs and Ag-Au BNPs were spherical in shape and FCC structure with nanoscale range (10-25 nm). The BNPs exhibit strong efficacy against bacterial strains. These nanoparticles were subjected to investigate the anticancer activity against human lung cancer cells (A549 cell line) through MTT assay. The cell viability was determined by this assay. The occurrence of cell apoptosis and necrotic were quantified by using dual fluorescent staining (AO/EB) and flow cytometry analysis. However, Ag-Au bimetallic nanoparticles showed highest cytotoxic potential with low IC50 - 57.35 ± 0.05 µM values. This IC50 value is comparatively lower than, Ag, Au MNPs and C.A. aqueous leaf extract. IC50 values of C.A- Ag-Au BNPs predominantly induced the cell apoptosis, necrotic and the death of A549 cells suggested the anticancer potential of C.A. mediated Ag-Au BNPs to treat the lung cancer cells.

3.
Article de Chinois | WPRIM | ID: wpr-1021966

RÉSUMÉ

BACKGROUND:Lung cancer is one of the most common malignant tumors with the worst prognosis worldwide.Its incidence rate and mortality rate have long been among the top of malignant tumors.The heterogeneity and drug resistance are among the reasons contributing to its poor prognosis.Lung cancer organoid,which is a 3D in vitro model cultured from patient-derived tumor cells recapitulating the biological characteristics of the primary tumor,can be used for various researches of lung cancer. OBJECTIVE:To review the application and research progress of lung cancer organoids in chemotherapy,targeted therapy,and immunotherapy drug sensitivity screening,analyze its limitations,aiming to provide new strategies for personalized and precision medicine of lung cancer. METHODS:The first author searched relevant articles published from 2013 to 2023 in CNKI and PubMed in July 2023.The search terms were"organoid,lung cancer organoid,lung cancer experimental model,precision medicine,drug sensitivity test,chemotherapy,targeted therapy,immunotherapy"in Chinese and English.Finally,a total of 84 articles were incorporated. RESULTS AND CONCLUSION:(1)Compared with traditional lung cancer research models,which can only demonstrate two-dimensional cell activities,lack cell-to-cell interactions,and suffer from species differences,lung cancer organoids offer a diverse cell source and continuously optimized culture conditions.They can simulate cellular interactions in a three-dimensional context while retaining the biological characteristics of the original tumor.These organoids represent a promising research model with significant potential,providing a solid foundation for their use in cancer drug screening.(2)Lung cancer organoids have shown preliminary significance in guiding anticancer drug selection.Their predictive outcomes align closely with actual clinical outcomes,marking a pivotal step towards precision in lung cancer treatment.By assessing the efficacy of common chemotherapy,targeted therapy,and immunotherapy drugs,these organoids enable the customization of individualized treatment strategies,reducing unnecessary drug trials and toxic and side reaction while exploring possible alternative drugs or combination regimens for drug resistance issues so as to guide the precision treatment of rare mutated lung cancer and fill the clinical gap.A more comprehensive drug evaluation is provided by comparing the activity of different drugs.Additionally,it is essential to consider the internal heterogeneity of organoids,emphasizing the importance of multiple sampling to enhance result accuracy.(3)Lung cancer organoids have limitations in practical applications such as inconsistent success rates and purity in cultivation and the lack of vascular tissue.To address these shortcomings,improvements are needed in cultivation conditions,expedited testing processes,and the development of multi-organ systems to simulate the overall effects of drugs in multiple organs.These enhancements will contribute to a more accurate assessment of drug efficacy and toxicity,thereby enhancing the precision of lung cancer treatment.

4.
Article de Chinois | WPRIM | ID: wpr-1030962

RÉSUMÉ

This article reviews relevant literature on the prevention and treatment of cancer with hesperidin published in the past 10 years by searching electronic databases such as China National Knowledge Infrastructure(CNKI), Wanfang, and PubMed, and summarizes the research progress on the anticancer mechanism of hesperidin. Hesperidin has a wide range of pharmacological effects, including anti-inflammatory, antioxidant, antibacterial, antiviral, anticancer, immune-regulatory, anti-radiation, neuroprotective and cardiovascular protective properties and so on. Its anticancer mechanisms mainly include inhibiting cancer cell proliferation, promoting apoptosis, reducing angiogenesis, inhibiting invasion and migration of cancer cells, regulating immunity and autophagy, and exerting antioxidant and anti-inflammatory effects. As a broad-spectrum anticancer drug, hesperidin manifests chemo-preventive and therapeutic effects across various cancers, contingent upon its multifaceted anticancer mechanisms. Furthermore, this article summarizes the synergistic effects of hesperidin in combination with cisplatin, doxorubicin, cyclophosphamide and paclitaxel. It elucidates that hesperidin can enhance the cytotoxicity of these anticancer drugs against cancer cells while mitigating drug resistance and adverse side effects. Nonetheless, the clinical use is somewhat constrained due to its poor water solubility and limited bioavailability. Therefore, this article also outlines the current strategies for enhancing hesperidin's bioavailability, including structural modification, combination with other chemical substances, and utilization of nano drug carriers.The discovery of derivatives of hesperidin not only preserves the anticancer efficacy of hesperidin, but also effectively overcomes the shortcomings of poor water solubility and low bioavailability of hesperidin, effectively predicting the good application prospects of hesperidin and its derivatives.

5.
Int J Pharm Pharm Sci ; 2023 Feb; 15(2): 8-17
Article | IMSEAR | ID: sea-231148

RÉSUMÉ

Objective: This study was aimed to access one of the hidden ANF in Indian bean and assessment of its antioxidant, immunomodulatory, antiangiogenic, and anti-cancer properties.Methods: Indian beans were processed and evaluated for the presence of ANF through HA activity. Bean-ANF was partially purified by ammonium sulfate precipitation (ASP) and dialysis. Obtained Partially Purified bean-ANF (PPb-ANF) resolved on 12% SDS-PAGE, analyzed protease digestibility. The immunogenicity of PPb-ANF was characterized by producing polyclonal antibodies and checked for the presence of natural antibodies in healthy human sera. Pharmacological studies of PPb-ANF were assessed through anti-oxidant, immunogenic, anti-angiogenic and anti-cancer assays.Results: Partially purified Bean-ANF (PPb-ANF) showed significant specific HA activity up to 150 Units/mg compared to crude extract 9.3 of Units/mg. The PPb-ANF was identified to have more than 90% homogeneity in purity with an observed M W of 30-32 kDa. PPb-ANF showed significant pepsin digestive stability up to 2 h at 37 ?C and appears digestive resistant. Rabbit produced anti-PPb-ANF IgG polyclonal antibody on immunization and exhibited immunogenic properties. Natural human IgG and IgE antibodies were found in the non-atopic human sera against PPb-ANF, indicative of its immunogenicity. Pharmacological studies of PPb-ANF confirmed its potent antioxidant activity. At 400 µg of PPb-ANF showed the highest around 90% DPPH activity and at 150 µg of PPb-ANF showed 89% inhibitory lipid peroxidation activity. The PPb-ANF showed 70% (3 ?g) and 40% (1.5 ?g) inhibitory in blood vessel density compared to control and exhibited significant anti-angiogenic activity. The PPb-ANF showed a significant (*p<0.05.) reduction in solid tumor weight upon dose-2 treatment (50 mg/kg body weight) and also increased lifespan up to 70 d compared with the control tumor model.Conclusion: PPb-ANF was identified as digestive-resistant, hemagglutinin with a molecular weight of 30-32 kDa. The protein is immunogenic and has potential antioxidant, antiangiogenic and anti-cancer properties. Further purification and mechanistic-based pharmacological characterization might explore this protein as a potential anti-cancer molecule.

6.
Chin. j. integr. med ; Chin. j. integr. med;(12): 268-279, 2023.
Article de Anglais | WPRIM | ID: wpr-971323

RÉSUMÉ

Cancers have high morbidity and mortality rates worldwide. Current anticancer therapies have demonstrated specific signaling pathways as a target in the involvement of carcinogenesis. Autophagy is a quality control system for proteins and plays a fundamental role in cancer carcinogenesis, exerting an anticarcinogenic role in normal cells and can inhibit the transformation of malignant cells. Therefore, drugs aimed at autophagy can function as antitumor agents. Flavonoids are a class of polyphenolic secondary metabolites commonly found in plants and, consequently, consumed in diets. In this review, the systematic search strategy was used, which included the search for descriptors "flavonoids" AND "mTOR pathway" AND "cancer" AND "autophagy", in the electronic databases of PubMed, Cochrane Library, Web of Science and Scopus, from January 2011 to January 2021. The current literature demonstrates that flavonoids have anticarcinogenic properties, including inhibition of cell proliferation, induction of apoptosis, autophagy, necrosis, cell cycle arrest, senescence, impaired cell migration, invasion, tumor angiogenesis and reduced resistance to multiple drugs in tumor cells. We demonstrate the available evidence on the roles of flavonoids and autophagy in cancer progression and inhibition. (Registration No. CRD42021243071 at PROSPERO).


Sujet(s)
Humains , Flavonoïdes/pharmacologie , Tumeurs , Antinéoplasiques/pharmacologie , Transduction du signal , Apoptose , Prolifération cellulaire , Carcinogenèse , Lignée cellulaire tumorale
7.
Acta Pharmaceutica Sinica B ; (6): 1303-1317, 2023.
Article de Anglais | WPRIM | ID: wpr-971759

RÉSUMÉ

In situ and real-time monitoring of responsive drug release is critical for the assessment of pharmacodynamics in chemotherapy. In this study, a novel pH-responsive nanosystem is proposed for real-time monitoring of drug release and chemo-phototherapy by surface-enhanced Raman spectroscopy (SERS). The Fe3O4@Au@Ag nanoparticles (NPs) deposited graphene oxide (GO) nanocomposites with a high SERS activity and stability are synthesized and labeled with a Raman reporter 4-mercaptophenylboronic acid (4-MPBA) to form SERS probes (GO-Fe3O4@Au@Ag-MPBA). Furthermore, doxorubicin (DOX) is attached to SERS probes through a pH-responsive linker boronic ester (GO-Fe3O4@Au@Ag-MPBA-DOX), accompanying the 4-MPBA signal change in SERS. After the entry into tumor, the breakage of boronic ester in the acidic environment gives rise to the release of DOX and the recovery of 4-MPBA SERS signal. Thus, the DOX dynamic release can be monitored by the real-time changes of 4-MPBA SERS spectra. Additionally, the strong T2 magnetic resonance (MR) signal and NIR photothermal transduction efficiency of the nanocomposites make it available for MR imaging and photothermal therapy (PTT). Altogether, this GO-Fe3O4@Au@Ag-MPBA-DOX can simultaneously fulfill the synergistic combination of cancer cell targeting, pH-sensitive drug release, SERS-traceable detection and MR imaging, endowing it great potential for SERS/MR imaging-guided efficient chemo-phototherapy on cancer treatment.

8.
China Pharmacy ; (12): 508-512, 2023.
Article de Chinois | WPRIM | ID: wpr-962501

RÉSUMÉ

With the advantage of high efficiency, low toxicity and targeting, liposomes have become the research hotspot of new drug preparations at home and abroad. In this paper, the research progress in recent years is reviewed from the aspects of preparation methods, classification and clinical application of liposomes. The results showed that in order to obtain more stable and controllable liposomes, scholars improved and optimized the traditional preparation methods and established novel preparation methods such as supercritical fluid methods, freeze-drying method and double-asymmetric centrifugation method. In order to enhance the efficacy and reduce toxicity, the conventional liposomes were optimized to get novel ones such as environmentally sensitive liposomes, long-circulating liposomes and multifunctional liposomes, which had greatly promoted the clinical application of liposomes. For now, liposomes have been used in many fields, such as anti-cancer agents, antimicrobial and vaccines, but most of the new liposomes are still in the early stage of development.

9.
China Pharmacy ; (12): 520-524, 2023.
Article de Chinois | WPRIM | ID: wpr-964758

RÉSUMÉ

OBJECTIVE To analyze the difference between the payment limitations of anti-cancer drugs and application scope of drug instructions, so as to better implement the payment policy of medical insurance drugs. METHODS The differences between the payment limitations of anti-cancer drugs and application scope of drug instructions in the National Catalogue of Drugs for Basic Medical Insurance, Industrial Injury Insurance and Maternity Insurance (2022) were compared and analyzed; the evidence-based basis of the difference was discussed, and the scope of limited payment was interpreted. RESULTS Totally 118 drugs had payment limitations; limitations scope mainly included limited evidence of gene detection results, limited indications, limited second-line and above treatment, limited payment duration, limited specialist prescription, limited medical institution grade, etc. Among them, 43 drugs had differences between the payment limitations and drug instructions, and the indications of 31 drugs were greater than payment limitations; for seven drugs, the drug indications beyond the payment limitations were recommended by the guidelines. The payment limitations of 75 drugs were consistent with drug instructions. The second-line and multi-line treatment was ineffective or intolerable with first-line drugs. There was a certain relationship between locally advanced, advanced or metastatic tumor and tumor stage, but different tumors had different criteria. Systemic treatment mainly referred to systemic treatment with drug. The results of limited genetic test required that the result was positive or negative. In addition, six kinds of TCM injections were limited to the level of medical institutions; the payment of two drugs did not exceed 12 months; when lenalidomide was combined with isazomide citrate, the medical insurance only paid for one of the drugs. CONCLUSIONS The payment limitations of some anti- cancer drugs are inconsistent with the drug indications. The drug payment limitations should be expanded according to the actual situation of clinical medication and the recommendations of guidelines. At the same time, the payment limitations should be formulated accurately and in detail, thus clinical and medical insurance staff can understand it and fully protect the interests of patients.

10.
Yao Xue Xue Bao ; (12): 413-422, 2023.
Article de Chinois | WPRIM | ID: wpr-965716

RÉSUMÉ

In this study, a series of 18 histone deacetylases inhibitors (HDACis), derived from our in-house anti-cancer trans-β-arylacryl 1,2,3,4-tetrahydroisoquinoline-based scaffold, were designed, synthesized, and antitumor evaluated. HDAC1 inhibitory activity assay showed that compounds 13d-13f and 13m-13o demonstrated attractive enzymatic activity with IC50 at single-digit nanomolar or subnanomolar level.In addition, 13o exerted superior anti-proliferative activity (A549, IC50 = 0.89 μmol·L-1; HCT116, IC50 = 0.49 μmol·L-1) to that of vorinostat (SAHA).Besides,13e, with the most potent HDAC1 enzymatic activity (IC50 = 3.8 nmol·L-1), also displayed attractive cellular activity (A549, IC50 = 1.74 μmol·L-1; HCT116, IC50 = 2.43 μmol·L-1). The Western blot analysis illustrated that 13e treatment increased the acetylation of H3 and α-tubulin in a dose-dependent manner in A549 cells. In summary, 13e and 13o deserve further functional investigation.

11.
Article de Chinois | WPRIM | ID: wpr-978469

RÉSUMÉ

Cervical cancer is a gynecological malignant tumor with a high incidence in the world. With the insidious onset and lack of obvious symptoms and signs in the early stage, 13% of cervical cancer patients are diagnosed in the advanced stage of the disease, and the 5-year survival rate of metastatic cervical cancer is only 16.5%. So far, surgery and radiotherapy/chemotherapy are still the basic means for the treatment of cervical cancer. However, with the emergence of toxicity, drug resistance, and other side effects, there are still some limitations in the clinical application of these therapies. In recent years, natural compounds represented by polysaccharides have been found to have a significant anti-cervical cancer effect, which has attracted extensive attention from researchers in China and abroad. Widely distributed in the roots, stems, leaves, flowers, and fruits of higher plants, plant-based polysaccharides are important components of natural polysaccharides, as well as multimers with a complex structure and biological response regulators, which have been widely studied in the fields of cancer, cardiovascular, endocrine, and other diseases. This study reviewed the research on the anti-cervical cancer effect and mechanism of natural plant-derived polysaccharides by consulting the literature in the past 20 years to bring breakthroughs in the research and development of anti-cervical cancer new drugs. Through the literature review, the results indicated that natural plant-derived polysaccharides could exert anti-tumor effects by inhibiting cell proliferation, promoting apoptosis, inhibiting invasion and migration, promoting autophagy, arresting cell cycle of cervical cancer cells, regulating epithelial-mesenchymal transition (EMT), resisting oxidative stress, inhibiting tumor angiogenesis, improving immunomodulatory activity, and regulating signaling pathways. It should be noted that in the current research on natural plant-derived polysaccharides against cervical cancer, the bioavailability of some natural polysaccharides is low and a considerable proportion of the research is limited to the in vitro experiment. Therefore, it is urgent to carry out more clinical experimental studies on the anti-cervical cancer of natural plant-based polysaccharides to obtain a more reliable theoretical and practical basis.

12.
Practical Oncology Journal ; (6): 485-490, 2023.
Article de Chinois | WPRIM | ID: wpr-1020885

RÉSUMÉ

γ-Tocotrienol(γ-T3)is a common phytochemical belonging to a major subclass of natural vitamin E,mainly de-rived from palm oil and rice bran.Compared to saturated tocopherol(TOC),the γ-T3 side chain contains unsaturated bonds and forms isoprene chains.γ-T3 has therapeutic activity for various chronic diseases with broad potential applications,especially in inhib-iting tumor proliferation and invasion.With deeply research,more and more evidence suggests that γ-T3 plays an important role in inhibiting cancer cell migration and metastasis,inducing tumor cell apoptosis,arresting cell cycle and regulating cancer-related sig-naling pathways.Therefore,this article will review the anti-cancer effects and mechanisms of γ-T3.

13.
Tumor ; (12): 534-540, 2023.
Article de Chinois | WPRIM | ID: wpr-1030311

RÉSUMÉ

Hepatocellular carcinoma(HCC)is a highly lethal cancer with significant incidence and mortality rates.The study of the biological features of liver cancer cells is critical for the development of novel treatment strategies for HCC.While traditional cell culture techniques fail to provide information on the growth and diffusion of cells in a threedim-ensional space(3D),3D bioprinting technology provides a new method to study the functional characteristics of HCC cells.With the development of 3D cell culture technology,researches are largely focused on exploring the function and behavior of cells in a three-dimensional environment,particularly in complex tumor models like liver tumors that comprise intricate cellular tissues and blood vessels.This article discussed about the cellular functions that need to be studied in the 3D bioprinting environment of HCC and other tumor cells by reviewing the research progress of 3D bioprinting in HCC and various other cancer cell lines,aiming to help researchers replicate the in vivo growth environment of tumor cells more accurately,expand application scenarios,and further explore cancer treatment methods.In addition,3D bioprinting technology is considered a promising tool for drug development,providing a more clinically relevant model for the pharmacological study of anti-cancer drugs,better revealing the drug sensitivity and resistance of tumors,reducing the need for animal experiments,and providing more possibilities for precision medicine.

14.
Chinese Pharmacological Bulletin ; (12): 2369-2377, 2023.
Article de Chinois | WPRIM | ID: wpr-1013664

RÉSUMÉ

Aim To investigate the mechanism of Qizhu anti-cancer prescription ( QZACP) inthe treatment of primary liver cancer using network pharmacology and molecular docking. Methods Drugs and primary liver cancer ( PLC) -related targets were found according to TCMSP database and disease databases such as GeneCard, the key chemical components and core targets were screened by Cytoscape 3. 9. 1 and String platform respectively, and a network relationship diagram of traditional Chinese medicine-active component-target was constructed by using Cytoscape 3.9. 1. GO functional analysis and KEGG pathway analysis were performed using DAVID platform, visualized by R 4. 1. 1 software, and finally the core clustered proteins were analyzed by CytoNCA plug-in to obtain the core action targets, and the core components and key targets were verified by using molecular docking technology and the pharmacodynamic mechanism of QZACP was further verified by animal experiments. Results The active ingredients of QZACP in the treatment of primary liver cancer may be quercetin, glycyrrhizin, Denudatin B, isoflavanone, sanguinarol, etc. ; the potential targets were STAT3, EGFR, AKT1 etc. ; the related pathways were mainly PI3K-Akt signaling pathway,MAPK signaling pathway,etc. ; molecular docking showed that the core compounds had better integrating conformation with the key targets. In addition, QZACP could inhibit the growth of tumor in nude mice and decrease the expression of STAT3, EGFR and AKT1. Conclusions Qizhu anti-cancer prescription may have some positive significance in the treatment of primary liver cancer, which may be related to the regulation of PI3K/Akt signaling pathway.

15.
Chinese Pharmacological Bulletin ; (12): 2288-2295, 2023.
Article de Chinois | WPRIM | ID: wpr-1013666

RÉSUMÉ

Aim To investigate the effect of AICAR on the expression of the proto-oncogene c-Myc and cell proliferation rates in specific cancer cell lines. Methods The mRNA levels of c-Myc were evaluated using fluorescence-based qRT-PCR to examine the effect of AICAR treatment on c-Myc mRNA expression levels. Western blot was used to evaluate the protein levels of c-Myc following AICAR treatment. RNA interference was employed to determine whether the regulatory effect of AICAR on c-Myc was dependent on AMPK and the downstream metabolic enzymes relating to AICAR. Actinomycin D and cycloheximide were used to assess the effect of AICAR on the stability of cMyc mR-NA and protein. Western blot was used to examine the regulatory effect of AICAR on c-Myc in various cancer cell lines. The MTT assay was used to determine the effect of AICAR on cell viability in these cell lines. Results AICAR significantly up-regulated c-Myc at both mRNA and protein levels. The protein level of c-Myc reached a plateau 12 h after the AICAR treatment. The up-regulatory effect of c-Myc induced by AICAR was not dependent on either the AMPK signaling pathway or the downstream metabolites of AICAR. AICAR could significantly enhance the mRNA stability of c-Myc but did not affect the protein stability. The up-regulation of c-Myc induced by AICAR was cell-type specific. AICAR up-regulated c-Myc in SW1990, 786-0, and A549, while down-regulated c-Myc in HepG2, MCF7, and U20S. In HepG2 cells, AICAR treatment decreased cell viability. However, in SW1990 and A549 cells, AICAR treatment did not lead to any significant difference in cell viability. AICAR decreased the cell viability only when c-Myc was knocked down in SW1990 and A549 cells. Conclusions AICAR directly up-regulates c-Myc expression in an AMPK-independent manner. The up-regulation effect is cell-type dependent. The regulation of c-Myc expression by AICAR is linked to the inhibitory effect of AICAR on tumor cell proliferation.

16.
Chinese Pharmacological Bulletin ; (12): 406-413, 2023.
Article de Chinois | WPRIM | ID: wpr-1013829

RÉSUMÉ

As an essential trace element, selenium plays a very important role in antioxidation and maintaining redox homeostasis in various metabolic processes. With the development of nano-technology, selenium nanoparticles ( SeNPs) have become potential biomedical drugs because of their low toxicity, degrad-ability and high bioavailability. With the ability to activate apop-tosis or autophagy by regulating the production of reactive oxygen species ( ROS) , SeNPs are widely used in anticancer therapy and pathogens killing/clearance. In addition, with excellent stability and drug encapsulation capacity, SeNPs are serving as a kind of effective nano-carriers for anti-cancer and anti-infection treatments. Interestingly, the important role of SeNPs in immune regulation ( such as the activation of macrophages and T effector cells) provides a new possibilities to achieve nano-immune syn-ergetic treatment strategy for anti-cancer and anti-infection thera¬pies. In this paper, we review the latest progress of the prepara¬tion methods and safety for SeNPs, followed by the advances of anti-infection, anti-cancer effects and its mechanisms, which would be helpful for promoting the pace of clinical research and application. In addition, we also summarize the functions of SeNPs in other aspects, so as to provide beneficial assistance for facilitating its scientific and clinical research.

17.
Acta Pharmaceutica Sinica B ; (6): 1498-1521, 2023.
Article de Anglais | WPRIM | ID: wpr-982800

RÉSUMÉ

Gas therapy has been proven to be a promising and advantageous treatment option for cancers. Studies have shown that nitric oxide (NO) is one of the smallest structurally significant gas molecules with great potential to suppress cancer. However, there is controversy and concern about its use as it exhibits the opposite physiological effects based on its levels in the tumor. Therefore, the anti-cancer mechanism of NO is the key to cancer treatment, and rationally designed NO delivery systems are crucial to the success of NO biomedical applications. This review summarizes the endogenous production of NO, its physiological mechanisms of action, the application of NO in cancer treatment, and nano-delivery systems for delivering NO donors. Moreover, it briefly reviews challenges in delivering NO from different nanoparticles and the issues associated with its combination treatment strategies. The advantages and challenges of various NO delivery platforms are recapitulated for possible transformation into clinical applications.

18.
Yao Xue Xue Bao ; (12): 2341-2352, 2023.
Article de Chinois | WPRIM | ID: wpr-999107

RÉSUMÉ

Cancer is still one of the major diseases threatening human life and health. At present, how to achieve precise diagnosis and treatment of tumors is the biggest challenge in cancer treatment. Prodrugs use the tumor specificity of targeting molecules to deliver anticancer drugs to tumor sites, which can effectively improve drug bioavailability, therapeutic efficacy and safety, and are currently a hot spot in the research and development of anticancer drugs. The targeting molecules of prodrugs mainly include nucleic acid aptamers, polymers, antibodies, polypeptides, etc. Among them, polypeptides have the advantages of good biocompatibility, controllable degradation performance, high in vivo responsiveness, and simple and easy preparation methods, and are widely used. It is used to construct peptide-drug conjugates (PDC) prodrugs to achieve targeted therapy of tumors. In recent years, with the development of phage peptide library technology and peptide standard solid-phase synthesis technology, more and more targeted peptides have been discovered and effectively synthesized and modified, providing strong support for the development of PDC. This review briefly introduces the types and functions of functional peptides and linkers in PDC, and discusses the application of PDC in chemotherapy, immunotherapy and photodynamic therapy in tumor targeted diagnosis and treatment, and finally summarizes the difficulties faced by PDC drug development.

19.
Acta Pharmaceutica Sinica B ; (6): 4621-4637, 2023.
Article de Anglais | WPRIM | ID: wpr-1011183

RÉSUMÉ

Hepatic stellate cells (HSCs) represent a significant component of hepatocellular carcinoma (HCC) microenvironments which play a critical role in tumor progression and drug resistance. Tumor-on-a-chip technology has provided a powerful in vitro platform to investigate the crosstalk between activated HSCs and HCC cells by mimicking physiological architecture with precise spatiotemporal control. Here we developed a tri-cell culture microfluidic chip to evaluate the impact of HSCs on HCC progression. On-chip analysis revealed activated HSCs contributed to endothelial invasion, HCC drug resistance and natural killer (NK) cell exhaustion. Cytokine array and RNA sequencing analysis were combined to indicate the iron-binding protein LIPOCALIN-2 (LCN-2) as a key factor in remodeling tumor microenvironments in the HCC-on-a-chip. LCN-2 targeted therapy demonstrated robust anti-tumor effects both in vitro 3D biomimetic chip and in vivo mouse model, including angiogenesis inhibition, sorafenib sensitivity promotion and NK-cell cytotoxicity enhancement. Taken together, the microfluidic platform exhibited obvious advantages in mimicking functional characteristics of tumor microenvironments and developing targeted therapies.

20.
Article de Chinois | WPRIM | ID: wpr-931263

RÉSUMÉ

GB7 acetate is a galbulimima alkaloid obtained from Galbulimima belgraveana.However,information regarding its structure,biological activities,and related mechanisms is not entirely available.A series of spectroscopic analyses,structural degradation,interconversion,and crystallography were performed to identify the structure of GB7 acetate.The MTT assay was applied to measure cell proliferation on human colorectal cancer HCT 116 cells.The expressions of the related proteins were measured by Western blotting.Transmission electron microscopy(TEM),acridine orange(AO)and monodansylcadaverine(MDC)staining were used to detect the presence of autophagic vesicles and autolysosomes.A transwell assay was performed to demonstrate metastatic capabilities.Oxygen consumption rate(OCR)and extracellular acidification rate(ECAR)assays were performed to determine the mitochondrial oxidative phosphorylation(OXPHOS)and glycolysis activity of HCT 116 cells.The data showed that GB7 acetate suppressed the proliferation and colony-forming ability of HCT 116 cells.Pretreatment with GB7 acetate significantly induced the formation of autophagic vesicles and autolysosomes.GB7 acetate upregulated the expressions of LC3 and Thr172 phosphorylated adenosine 5'-monophosphate(AMP)-activated pro-tein kinase α(p-AMPKα),which are key elements of autophagy.In addition,GB7 acetate suppressed the metastatic capabilities of HCT 116 cells.Additionally,the production of matrix metallo-proteinase-2(MMP-2)and MMP-9 was reduced,whereas the expression of E-cadherin(E-cad)was upregulated.Furthermore,GB7 acetate significantly reduced mitochondrial OXPHOS and glycolysis.In conclusion,the structure of the novel Galbulimima alkaloid GB7 acetate was identified.GB7 acetate was shown to have anti-proliferative,pro-autophagic,anti-metastatic,and anti-metabolite capabilities in HCT 116 cells.This study might provide new insights into cancer treatment efficacy and cancer chemoprevention.

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