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1.
China Pharmacy ; (12): 58-63, 2022.
Article in Chinese | WPRIM | ID: wpr-907013

ABSTRACT

OBJECTIVE To prepare apigenin silk fibroin(API@SF)nanoparticles and to evaluate their safety and anti-tumor activity. METHODS API@SF nanoparticles were prepared by nanoprecipitation method ,and their morphology ,particle size ,Zeta potential,drug loading amount and in vitro release were characterized. The safety of nanoparticles was evaluated by hemolysis test and HE staining. MTT assay was adopted to evaluate inhibitory effects of API@SF nanoparticles on breast cancer 4T1 cells in mice. RESULTS The prepared API@SF nanoparticles were spherical with uniform distribution. The average particle size was 406.61 nm, the polydispersity index was 0.154,the Zeta potential was -18.4 mV,and the average drug-loading amount was 5.20%. The in vitro release results showed that the release rate of the nanoparticles was relatively fast in the release medium of pH 5.0 and relatively slow in the release medium of pH 7.4. Results of hemolysis test and HE staining showed that the nanoparticles had good biocompatibility. Results of MTT assay showed that the inhibitory effect of API@SF nanoparticles on 4T1 cells was significantly higher than that of API raw materials (P<0.05),and its mechanism may be related to increasing the level of reactive oxygen species in cells. CONCLUSIONS API@SF nanoparticles are prepared successfully ,which possess good safety and anti-tumor activity.

2.
Acta Pharmaceutica Sinica ; (12): 707-715, 2022.
Article in Chinese | WPRIM | ID: wpr-922888

ABSTRACT

We analyzed the anticancer effect and mechanism of the novel indoleamine 2,‍3-dioxygenase 1 (IDO1) inhibitor NLG-919 combined with temozolomide (TMZ) on human glioma cell lines. The anti-tumor activity of NLG-919 and temozolomide after single and combined treatments was detected by MTT assay. Colony formation assay, invasion assay and migration assays were used to detect the effects of NLG-919 and temozolomide alone or in combination on proliferation, invasion and migration of human glioma cells. A flow cytometry assay was used to detect cell apoptosis, cell cycle arrest, reactive oxygen species (ROS) production and mitochondrial membrane potential damage (JC-1). An immunofluorescence assay was used to detect the expression level of IDO1 and HPLC was used to detect the expression level of L-kynurenine (Kyn) to explore the anti-tumor mechanism of NLG-919 and temozolomide. The results show that NLG-919 had a weak in vitro inhibitory effect compared to that of temozolomide. The IC50 of NLG-919 on U251 cells and U87 after 72 h was 26.9 and 30.7 μmol·L-1, respectively. However, when NLG-919 was used in combination with temozolomide, its anti-glioma activity was significantly increased. Compared with the single treatment, the combination treatment had a potent ability to inhibit proliferation, invasion and migration of glioma cells. Combination treatment improved the capacity of temozolomide to induce cell cycle arrest and inhibit the growth of glioma cells. NLG-919 significantly down-regulated the expression and activity of IDO1 in glioma cells, and the inhibitory effect was improved after combination with temozolomide, and effectively blocked the production of Kyn through the metabolism of L-tryptophan (Trp). In conclusion, the IDO1 inhibitor NLG-919 and temozolomide showed synergistic effects in the anticancer therapy of human glioma cell lines.

3.
Acta Pharmaceutica Sinica ; (12): 547-556, 2022.
Article in Chinese | WPRIM | ID: wpr-922884

ABSTRACT

The abnormality of ubiquitin proteasome pathway is an important factor leading to the imbalance of protein homeostasis. In this process, the deubiquitinase responsible for removing the ubiquitin chain of protein substrate is very important. Its abnormal activity or expression can cause the functional changes of key oncogenic/tumor suppressor proteins, which directly or indirectly lead to the occurrence, development and malignant evolution of tumors. Based on this, the discovery and research of small molecule inhibitors targeting deubiquitinases have become a hot field of anti-tumor candidate drugs. This review will focus on the regulatory effect and mechanism of ubiquitin proteasome pathway, especially deubiquitinase on tumor, introduce the application of deubiquitinase small molecule inhibitors in tumor treatment, and discuss the research status and latest progress of small molecule inhibitors, so as to provide ideas for the research of new anti-tumor strategies based on deubiquitinase.

4.
Article in Chinese | WPRIM | ID: wpr-920647

ABSTRACT

@#Ten novel podophyllotoxin derivatives (IIIa-IIIi and IV) were synthesized by three-step reactions using podophyllotoxin and N-benzyloxycarbonyl glycine-L-proline as raw material. The structures of the target compounds were confirmed by 1H NMR, 13C NMR and MS. MTT method was used to test anti-tumor activity of the target compounds on HepG2, THP-1, HeLa and MCF-7 cells. The results showed that all the target compounds had inhibitory activity against HepG2, THP-1, HeLa and MCF-7 cells, and the inhibitory activity of IIIa on HepG2 cells was the most prominent with an IC50 value of 0.58 nmol/L. The binding mode of compound IIIa and FAPα was studied by molecular docking. Compound IIIa could bind to multiple sites of FAPα enzyme.

5.
Acta Pharmaceutica Sinica ; (12): 222-232, 2022.
Article in Chinese | WPRIM | ID: wpr-913174

ABSTRACT

The dense extracellular matrix (ECM) of the tumor severely limits the deep penetration of nanomedicine and weakens its anti-tumor effect. Based on this, the yeast vesicle biomimetic nanomedicine with active deep penetration ability of tumor tissue was designed and developed for enhanced tumor therapy. Results of characterization showed that the yeast cell vesicles (YCV) displayed a spherical morphology with diameter of around 100 nm and was well dispersed. Then the chemotherapeutic drug doxorubicin (DOX) was selected as a model drug, and DOX was loaded into YCV to obtain YCV/DOX through electrostatic interaction, the encapsulation efficiencies of DOX were calculated as 82.5%. The drug release profile of YCV/DOX implied that DOX release showed a manner of pH-dependent, it may be that pH has affected the electrostatic effect of YCV and DOX. Compared with liposomes (Lipo), in vitro cell experiments showed that YCV from natural sources had stronger permeability in three-dimensional multicellular spheres. It is speculated that the mechanism may be good deformation capacity of YCV. A 4T1 xenograft tumor model was established to evaluate the therapeutic efficacy of YCV/DOX. The results suggested that YCV/DOX has stronger tumor tissue penetration ability and could effectively inhibit the tumor growth. All animal experiments were performed in line with national regulations and approved by the Animal Experiments Ethical Committee of Zhengzhou University. This study brings new ideas for the development of biomimetic nanomedicine to overcome the ECM of solid tumors.

6.
Article in Chinese | WPRIM | ID: wpr-913016

ABSTRACT

@#Metformin is currently the first-line drug for the treatment of diabetes. In addition to its hypoglycemic effect, it has also been found to have other potential effects, such as anti-inflammatory, odontogenic differentiation-promoting, osteogenic differentiation-promoting, and antitumor effects. Previous studies have shown that metformin can promote the healing of periapical lesions, and its mechanism may be related to the promotion of osteogenic differentiation and the induction of dental pulp cell differentiation by activation of adenylate-activated protein kinase by dimethyldiphosphate. Clinical indexes, such as the probing depth, attachment loss level and probing bleeding index, were significantly improved in patients with periodontitis treated with metformin, which may play a role in the prevention and treatment of periodontal disease by promoting the proliferation, migration and osteogenic differentiation of periodontal ligament stem cells. Metformin has been proven to inhibit the growth and proliferation of tumor cells and plays an important role in the prevention and treatment of oral tumors such as oral squamous cell carcinoma. At present, research remains in the in vitro and animal experimental stage, and the related mechanism needs to be further explored. Clinical trials remain in the evaluation of clinical indicators, so large-scale, long-term, multicenter, randomized controlled clinical trials need to be further developed

7.
Acta Pharmaceutica Sinica ; (12): 3252-3260, 2021.
Article in Chinese | WPRIM | ID: wpr-906843

ABSTRACT

Drug combination can effectively enhance the anti-tumor effect, reduce the drug dose, and improve medication safety. The use of nano-carrier for drug co-delivery can effectively avoid the differences in drug delivery behavior in vivo. Triptolide and celastrol are the main anti-tumor active components of Tripterygium wilfordii Hook f. Modern studies have shown that the combination of triptolide and celastrol can significantly enhance the antitumor effect, but they are limited by poor water solubility and low tumor tissue delivery rate. In this study, a biomimetic erythrocyte membrane liposome co-loaded with triptolide and celastrol was prepared to characterize the morphology, particle size, potential, drug release, serum stability, and other properties. The immunogenicity, uptake behavior, and anti-cell proliferation ability of the biomimetic liposome was compared. All the animal experiments were carried out in accordance with protocol evaluated and approved by the Ethics Committee of Chengdu University of Traditional Chinese Medicine (Chengdu, China). The results showed that the biomimetic erythrocyte membrane liposome co-loaded with triptolide and celastrol (C+T/RBCm@Lip) in this study had an average particle size of 119.12 ± 2.78 nm and a spherical "core-shell" structure. The zeta potential value was -16.9 ± 1.2 mV, and the drug release behavior in vitro was slow. In addition, the process of coating the cell membrane maintained the characteristics of erythrocyte membrane protein, had good stability in serum, and could effectively avoid the recognition and clearance of macrophages, without causing immunogenicity in vivo. The uptake effect of co-loaded biomimetic liposomes on HepG2 hepatocellular carcinoma cells was enhanced compared with that of uncoated cell membrane liposomes, and the inhibitory effect on proliferation of HepG2 cells was enhanced. In conclusion, the biomimetic liposomes coated with erythrocyte membrane prepared in this study is beneficial to the anti-tumor delivery of triptolide and celastrol, and could enhance the inhibitory effect on the growth of HepG2 liver cancer cells, providing a new idea for the anti-tumor application of Tripterygium wilfordii Hook f.

8.
Acta Pharmaceutica Sinica ; (12): 3212-3223, 2021.
Article in Chinese | WPRIM | ID: wpr-906817

ABSTRACT

Natural polysaccharides with good biocompatibility and unique tumor immunomodulatory activity are becoming an important adjuvant anticancer therapy in clinic. In the field of pharmaceutics, natural polysaccharides can be used as not only bioactive components but also drug delivery carriers, as well as tumor-targeted ligands. Besides, various novel drug delivery systems based on natural polysaccharides exhibit unique advantages in regulating tumor immune microenvironment. In this review, we summarize the progress on natural polysaccharides in tumor microenvironment (TME) regulation and the designs of nano-sized drug delivery system, and point out challenges of polysaccharide-based drug delivery systems in the future application, and also give the potential solutions for these issues.

9.
China Pharmacy ; (12): 2980-2986, 2021.
Article in Chinese | WPRIM | ID: wpr-906778

ABSTRACT

OBJECTIVE:To prepare chelerythrine nanoparticles(CHE-NPs),optimize their formulation ,and evaluate its drug release behavior in vitro and its inhibitory effect on melanoma. METHODS :Using methoxy polyethylene glycol-poly (lactic-co- glycolic acid )(mPEG-PLGA)as carrier ,CHE-NPs were prepared by the nano-precipitation method. HPLC method and dialysis bag method were used to determine entrapment efficiency and drug loading. The formulation of CHE-NPs was optimized by Box-Behnken response surface design using overall desirability (OD)of them as dependent variables ,CHE dosage ,mPEG-PLGA concentration and poloxamer 188(F68)concentration as independent variables. The particle size and Zeta potential of CHE-NPs prepared by the optimal formulation were detected ;the characteristics of drug release in vitro were investigated ;the effects of CHE and CHE-NPs on survival rate of mice B 16 melanoma cells were compared ,and median inhibition concentrations (IC50)of them were calculated. RESULTS :The optimal formulation included CHE of 2 mg,mPEG-PLGA of 13 mg/mL,F68 of 1.8%. Average entrapment efficiency rate of CHE-NPs prepared by the optimal formulation was (80.18±1.11)%,average drug loading was (11.36±0.28)%,average OD value was 0.96±0.04 [the relative deviation from predicted value (0.90)of OD was 6.67%]; particle size was (113.1±1.40)nm,and Zeta potential was (-21.6±0.29)mV;polydispersity index was 0.07±0.01(n=3); accumulative release rates of CHE control and CHE-NPs were 90.87% and 68.68% within 8 h,and drug release behavior in vitro of the latter was in accordance with Weibull kinetic model. Inhibitory effect of CHE-NPs on B 16 melanoma cells was significantly stronger than that of CHE ;the 24 h IC 50 of CHE-NPs and CHEwere 69.35 and 107.36 μg/mL,respectively. CONCLUSIONS :The prepared CHE-NPs show good sustained-effect and high capacity of drug loading ,and strengthen the inhibitory effect of CHE on melanoma.

10.
Article in Chinese | WPRIM | ID: wpr-906771

ABSTRACT

@#Sphingosine kinase 1 (SphK1) is an important protein that regulates the lipid microenvironment of cell membranes, and plays an important role in the dynamic equilibrium of ceramide, sphingosine and sphingosine-1-phosphate.The overexpression of SphK1 is closely related to the occurrence, development and migration of tumors as well as the generation of drug resistance.SphK1 inhibitors can induce apoptosis of various tumor cells and reverse drug resistance, which has a good prospect for drug development.In this article, the structural biology of SphK1, the structural types and structure-activity relationships of SphK1 inhibitors are reviewed.

11.
Article in Chinese | WPRIM | ID: wpr-906537

ABSTRACT

The root of Tripterygium wilfordii has the effect in dispelling wind and eliminating dampness. Now it is mostly used in the treatment of systemic lupus erythematosus and other diseases. Triptonide is a diterpene small molecule compound extracted from T. wilfordii. In the early years, it was studied as a potential drug with anti-inflammatory and anti-reproductive effects. Recently, researchers found that its anti-tumor effect was particularly prominent because triptonide could inhibit the growth of a variety of tumors with different mechanisms at the nanomole dose, with a potential to be used as a broad-spectrum anti-cancer drug. In addition, due to the low yield from T. wilfordii, low bioavailability due to poor water solubility and anti-reproductive side effect as an antitumor drug, it will become study hotspots to exploring its synthesis and preparation and modifying its structure to reduce cost, improve bioavailability and reduce side effect, while maintaining its pharmacological activity. The authors reviewed domestic and foreign studies and patents on triptonide, and summarized its pharmacological activity and mechanism. It is found that although current studies on triptonide are still in the preliminary stage, there have been increasingly more studies on its anti-tumor mechanism year by year since 2014. This paper mainly introduces the antitumor pharmacological activity and mechanism of triptonide. In addition, it reviews anti-inflammatory, immunosuppression and anti-reproductive pharmacological effect of triptonide, as well as the existing studies on its toxicity, synthesis and structural modification. The authors put forward some personal ideas on its future study direction, in the hope to provide thinking and inspirations for other researchers and provide references for further development and research.

12.
Article in Chinese | WPRIM | ID: wpr-906535

ABSTRACT

Xihuangwan is composed of four Chinese medicines: Bovis Calculus, Olibanum, Myrrha, and Moschus. Modern pharmacology studies have shown that Xihuangwan has anti-inflammatory, antibacterial, anti-tumor, anti-mammary gland hyperplasia effect, and can enhance the body's immune function. Cancer seriously endangers public health and safety-of-life, and is a major cause of mortality of Chinese citizens. It is a disease with intricate etiopathogenesis caused by the joint action of circumstances and hereditary factors. At present, anti-tumor chemotherapy drugs in clinical application not only have toxic and side effect, but also affect clinical efficacy and prognosis of patients. Long-term use will also lead to drug resistance of tumors. As a traditional classic anti-cancer prescription, Xihuangwan has been used more and more in tumor research with the rise of Chinese medicine culture. It is provided with remarkable inhibitory effect on liver cancer, gastric cancer, carcinoma of the lungs, mammary gland, colorectal carcinoma and other malignant tumors. In clinical practice, Xihuangwan , mostly used as adjuvant drugs in combined use with chemotherapy drugs for anti-tumor effect, can reduce the side effect of chemotherapy drugs and the untoward reaction of sufferers, improve the survivability of patients to chemotherapy, reduce or delay postoperative tumor recurrence, enhance the body's immune function, and reverse the tolerance of tumor cells. Based on the anti-tumor research of Xihuangwan, we summarized its mechanisms in inducing cell apoptosis, regulating amino acid metabolism, reversing drug resistance, interfering with cell cycle, resisting tumor metastasis and invasion, regulating immune function, improving tumor microenvironment, and regulating signal pathways, as well as its clinical combination with chemotherapeutic anti-tumor drugs, analyzed the current anti-tumor research status of Xihuangwan's research, and put forward the shortcomings and unresolved problems in order to provide theoretical basis for further research and clinical application of Xihuangwan.

13.
Article in Chinese | WPRIM | ID: wpr-906506

ABSTRACT

Prostate cancer is an epithelial malignant tumor that occurs in the prostate. It is the most common cancer among men in the world. Its mortality rate is second only to lung cancer, which has seriously affected men's healthy life. Prostate cancer is not easy to be detected in the early stage. Most patients are already in the advanced stage and metastasized when they are diagnosed. At this time, radical surgery is not suitable for treatment. Advanced prostate cancer is mainly treated with endocrine therapy, but after a median time of 14-30 months, the patient will develop hormone-resistant prostate cancer and enter the advanced stage. Advanced hormone-resistant prostate cancer is treated with radiotherapy and chemotherapy, which, however, are not ideal for treating advanced prostate cancer. They can also cause serious side effects such as frequent urination, dysuria, urinary incontinence, rectal bleeding, loss of libido, hot flashes, and impotence, as well as generate multi-drug resistance. Therefore, it′s urgent to find a safe, effective and low-toxic anti-tumor drug. With the deepening of the research on the pharmacological effects of peptides, it has been proved that peptides have important application value in anti-fatigue, anti-aging, anti-inflammatory, antibacterial and anti-tumor. The anti-tumor peptides have attracted extensive attention in the field of anti-tumor research due to their high specificity, high bioavailability, good stability, low toxicity, low molecular weight, and easy synthesis. Pharmacological experiments have shown that polypeptides exert their anti-tumor effect mainly by inducing cell apoptosis, causing cell cycle arrest, inhibiting angiogenesis, and regulating immune function. This article summarized the related literature of peptides in recent years, the sources of peptides, the mechanisms and applications of peptides against prostate cancer for experimental research and clinical reference.

14.
Article in Chinese | WPRIM | ID: wpr-906503

ABSTRACT

Formononetin is a kind of plant isoflavones extracted from medicinal herbs such as Trifolium pratense,Astragalus membranaceus and Spatholobi Caulis have shown that formononetin has strong anti-tumor biological activity,and can be used as an anti-tumor drug in the treatment of various malignant tumors. Many studies so far have shown that formononetin can inhibit cell proliferation,induce cell apoptosis,inhibit cell migration and invasion,and induce cell cycle arrest on tumors through a variety of molecular mechanisms and pathways. These antitumor activities can be observed in cells of various tumors such as breast cancer,colorectal cancer,prostate cancer,bladder cancer and lung cancer in trials and animal models. Examples of these effects include triggering the generation of reactive oxygen species (ROS),regulating phosphatidylinositol-3-kinase/protein kinase B/mammalian target of rapamycin(PI3K/Akt/mTOR) and Mitogen-activated protein kinases(MAPK) signaling pathways,inhibiting the activation of tyrosine kinase(JAK1 and JAK2 )and nonreceptor tyrosine kinase(c-Src),and regulating cytokeratin 19(CK19),matrix metalloproteinases(MMP),microRNA-21(miR-21),lamin A/C antibody(Lamin A/C),expression of Cyclin D1 and Cyclin E1. In addition, the anti-tumor effects of formononetin derivatives were reviewed in this paper. By modifying the chemical structure of formononetin,many related derivatives have been obtained. Experimental results have shown that some derivatives of formononetin have stronger anti-tumor activity and lower cytotoxicity,but the related molecular mechanism of action still needs to be explored further in-depth. In conclusion,formononetin and its derivatives may become potential anti-tumor drugs.

15.
Article in Chinese | WPRIM | ID: wpr-906385

ABSTRACT

Curcumae Longae Rhizoma is a traditional Chinese medicine with the efficacy of activating blood and moving Qi. Curcumin, a polyphenolic substance extracted from the rhizome of plant Curcuma longa, possesses multiple pharmacological activities like anti-tumor, anti-oxidation, anti-bacteria, and anti-inflammation. Laryngeal carcinoma (LC) is a common malignant tumor, whose incidence in recent years has been on the rise, and the 5-year survival rate has continuously decreased. Considering the specific location of larynx, researchers are actively exploring diverse treatment modalities for laryngeal organ preservation. Many studies have shown that curcumin has an inhibitory effect on the development of LC. By virtue of multiple pharmacological effects, curcumin deserves to be thoroughly explored. However, most of the current research is limited to in vitro exploration, and the partial mechanism of curcumin remains unclear, indicating that there is still a long way to go before curcumin becomes a Chinese medicinal preparation for the clinical treatment of LC. This paper reviewed the physicochemical properties of curcumin and the methods for its extraction from plants, the efficacy of curcumin in inducing cell apoptosis and protective autophagy, reversing cell drug resistance, inhibiting cell proliferation, migration, and invasion and tumor angiogenesis, the action mechanism of curcumin in combination with resveratrol, platinum drugs, 3-methyladenine, taxols, and 5-fluorouracil against LC, as well as the bioinformatics analysis concerning curcumin and LC. This paper is expected to provide reference for relevant researchers to clarify the mechanism and important targets of curcumin against LC and promote its clinical application.

16.
Article in Chinese | WPRIM | ID: wpr-906308

ABSTRACT

Objective:To investigate bonding ability between 4-sulfonylcalix [6] arene (SCA6) and 15 alkaloids (matrine, allomatrine, dauricine, daurisoline, quinidine, quinine, crotaline, vincristine, gelsemine, koumine, tetrandrine, aloperine, oxymatrine, sophocarpine and sinomenine), and to evaluate viability<italic> in vitro</italic> of HepG2 and H9c2 cells with 12 alkaloids/SCA6 bonding systems (except allomatrine, oxymatrine, sinomenine). Method:Fluorescence competitive titration was used to determine the binding constants of alkaloids and SCA6, the inhibitory effect of alkaloid/SCA6 complex on proliferation of HepG2 and H9c2 cells was investigated by cell counting kit-8 (CCK-8). Result:All the 15 alkaloids had good bonding with SCA6 at the ratio of 1∶1 (the binding constants >1×10<sup>5</sup> mol·L<sup>-1</sup>, <italic>R</italic><sup>2</sup>>0.98), the aloperine (quinolizidine alkaloids) and SCA6 had the biggest binding constant (20.55×10<sup>6</sup> mol·L<sup>-1</sup>). In addition to gelsemine, crotaline, matrine and sophocarpine, 8 alkaloids (including aloperine, tetrandrine, dauricine, daurisoline, quinidine, quinine, vincristine and koumine) exhibited significant anti-tumor effects on HepG2 cells. Except for daurisoline, the anti-proliferation effect of the other 11 alkaloids before and after binding with SCA6 had no difference in HepG2 cells. In addition to gelsemine, crotaline, matrine and sophocarpine, the anti-proliferation effect of the other 8 alkaloids before and after binding with SCA6 had no difference in H9c2 cells. Conclusion:SCA6 shows intense binding ability with bisbenzylisoquinoline, quinolizidine and indole alkaloids. It can improve the solubility of alkaloids without affecting their anti-tumor activity, which provides a reference for subsequent related applications of SCA6 as a drug delivery carrier.

17.
Article in Chinese | WPRIM | ID: wpr-906269

ABSTRACT

Objective:To investigate the effect and mechanism of PAE<sub>2</sub>, a polypeptide of <italic>Periplaneta americana, </italic>in reversing multidrug resistance (MDR) for liver cancer <italic>in vivo</italic>. Method:Balb/c-nude mice were inoculated with HepG2 and HepG2/ADM cells under the armpits to establish animal models of liver cancer sensitive strains and animal models of MDR respectively. After successful modeling, the nude mice were randomly divided into normal group, HepG2 model group, HepG2/ADM model group, sorafenib group (positive drug control group, <italic>ig</italic> 30 mg·kg<sup>-1</sup>), HepG2/ADM+PAE<sub>2</sub> (<italic>iv</italic>) low, medium and high dose groups (50, 100, 200 mg·kg<sup>-1</sup>), HepG2/ADM+PAE<sub>2</sub> (<italic>ig</italic>) low, medium, and high dose groups (50, 100, 200 mg·kg<sup>-1</sup>), skim cream group (<italic>ig</italic> 200 mg·kg<sup>-1</sup>), and CⅡ-3 group (<italic>ig</italic> 200 mg·kg<sup>-1</sup>), all of which received corresponding drug treatment. The body weight and tumor volume of nude mice were measured and recorded every 2 days. The next day after the last administration, tumor tissues of nude mice were taken to record the tumor weight. The effect of <italic>P. americana </italic>polypeptide PAE<sub>2</sub> on permeability-glycoprotein(P-gp), lung resistance protein(LRP) , breast cancer resistance protein(BCRP), protein kinase C(PKC), glutathione S-transferase-π(GST-π), topo-isomerase typeⅡ(ToPoⅡ), multidurg resistance gene 1(MDR1)<sub> </sub>and Multidrug resistance-associated proteins(MRP1) of the protein level and gene level expression in tumor tissues were determined by immunohistochemistry (IHC) and real-time quantitative polymerase chain reaction (Real-time PCR). In addition, both oral and intravenous administration groups were set up at the same time for preliminary study on the basic pharmacokinetic characteristics of <italic>P. americana </italic>polypeptide PAE<sub>2</sub>. Result:After the successful modeling, the body weight of the nude mice was significantly lower than that in the normal mice(<italic>P</italic><0.05). After treatment with corresponding drugs, the body weight increased to a certain extent, but it was still not as good as the normal nude mice. In <italic>iv</italic> administration, the medium-dose <italic>P. americana </italic>polypeptide PAE<sub>2</sub> showed the best anti-tumor effect as compared with the model group (<italic>P</italic><0.05), while in oral administration, the anti-effect increased with the increase of the dose, so the high-dose group showed the best effect (<italic>P</italic><0.05). Preliminary crude extract CII-3 had no obvious anti-tumor effect, and skim cream showed a certain anti-tumor effect (<italic>P</italic><0.05). <italic>P. americana </italic>polypeptide PAE<sub>2</sub> had certain effects on MDR related proteins and enzymes<italic> in vivo</italic>, mainly by inhibiting the expression of LRP and BCRP in tumor tissues and affecting the expression of these related proteins and genes to different degrees to inhibit intracellular drugs outflow, thereby promoting tumor apoptosis, and the effect was superior to that of the <italic>P. americana</italic> crude extract CⅡ-3 and skim cream. Conclusion:<italic>P. americana</italic> polypeptide PAE<sub>2</sub> may reduce the drug efflux, promote intracellular drug accumulation and apoptosis by affecting the expression of related proteins and enzymes that mediate multidrug resistance, thereby exerting a reverse effect on HepG2/ADM cells Balb/c MDR in nude mice.

18.
Article in Chinese | WPRIM | ID: wpr-906135

ABSTRACT

Presently, tumor has become an important factor threatening human health, and how to cure tumor effectively is still one of the most important problems in the modern medical field. Mongolian medicine has a long history, and is an important component of traditional Chinese medicine (TCM), with distinctive national characteristics. It has been gradually formed and developed by absorbing Tibetan medicine,Indian medical theory and TCM. It has the advantages of a low toxicity,diverse structures and effect in modulating immune responses,with a important value and application perspectives. This paper focused on literatures from China National Knowledge Infrastructure,WanFang and Pubmed databases in recent years,with Mongolian medicine,anti-tumor and mechanism of action as the key words. The relevant literatures were collected, and the anti-tumor mechanisms of Mongolian medicinal in inhibiting cell proliferation, affecting cell cycle,inducing apoptosis,suppressing tumor invasion and metastasis,controlling angiogenesis and regulating immune status were summarized, in the hope to provide a reference for prevention and treatment of tumors with Mongolian medicine. The survey results showed that the study methods for Mongolian medicine at this stage were mostly simple, with a low overall level and based on in vitro cell level. However,the antitumor mechanism of Mongolian medicine compounds was not deeply studied. The material basis and mechanism of Mongolian medicine shall be further studied by modern medicine and bioscience techniques. Long-term goals and plans shall be established to form their own characteristics and advantages.

19.
Article in Chinese | WPRIM | ID: wpr-906101

ABSTRACT

Cancer is a threat to human health. New treatments for cancer can significantly prolong the survival time of patients, but fail to improve the adverse reactions induced by chemoradiotherapy. Improving patient outcomes still requires the effort of cancer researchers. In recent years, the anti-tumor effects of active components from Chinese herbs have received wide attention. Kaempferol, a flavonoid mainly found in the medicinal plant Kaempferia galanga, can be used to treat obesity, cardiovascular diseases, diabetes and other diseases. It has also exhibited good efficacy in inhibiting the occurrence and development of liver cancer, colon cancer, lung cancer, ovarian cancer, and other malignant tumors. Kaempferol mainly exerts the anti-cancer effect by inducing apoptosis. Specifically, it promotes the production of intracellular reactive oxygen species (ROS) and triggers cell apoptosis through the mitochondrial pathway. Besides, it is capable of interfering with the cancer cell cycle, causing most cancer cells to arrest in the G2/M phase, and inducing cell autophagy, a programmed cell death, thus inhibiting cell migration and invasion and angiogenesis, synergistically improving chemotherapeutic drug efficacy, and reducing adverse effects. Kaempferol acts on a series of intracellular and extracellular targets to participate in the regulation of tumor cell signaling pathways, involving phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt), epidermal growth factor receptor (EGFR), mitogen activated protein kinase (MAPK), and Wnt signaling pathways, with the PI3K/Akt signaling pathway being most significant. In addition, kaempferol also plays an important regulatory role in tumor epigenetics. This paper reviewed the anti-tumor effect and mechanism of kaempferol, aiming to provide reference for in-depth study on its prevention and treatment of tumor and the development of new anti-tumor drugs.

20.
Article in Chinese | WPRIM | ID: wpr-905848

ABSTRACT

Tumors are new organisms formed by uncontrollable cell proliferation of local tissues driven by various oncogenic factors. The cause of tumors is unknown with life-threating outcome. Tumors can be classified into benign tumors, borderline tumors, and malignant tumors according to their pathological properties. Among them, malignant tumor is commonly known as cancer, with no specific medicines or reliable cure means, so this is a hot spot and difficult point in current medical research. In ancient literatures, there are many records about the efficacy of Chinese herbal medicine in treating tumor, and modern pharmacological researches have shown that more and more active ingredients of traditional Chinese medicine(TCM) have gradually highlighted their inhibitory effect on various types of tumor. Caulis sinomenii has been used for treatment of rheumatic diseases in TCM for a long history. Sinomenine is a major bioactive alkaloid presented in C. sinomenii, which has demonstrated a wide range of pharmacological activities such as anti-inflammation, immunosuppression, analgesia and sedation, and due to its slightly soluble in water, it is commonly used in clinic in the form of hydrochloride, with its commercial name of Zhengqing Fengtongning. Recent studies show that sinomenine alone or combined with chemoradiotherapy can inhibit growth of several tumors significantly or in a synergistic way, so it is termed as an inhibitor of tumors. Anti-tumor effect of sinomenine involve inhibition of tumor cell proliferation, induction of tumor cell apoptosis, blockade of tumor cell cycle, suppression of tumor invasion and metastasis, induction of autophagy of tumor cells, and reversal of multidrug resistance of tumor cells. Upon combination with nanomaterials, it can enhance efficiency and reduce toxicity. Here we summarized and reviewed recent advances on basic anti-tumor research of sinomenine, and then made a classification and description according to its in vivo and in vitro pharmacological action and mechanism of action, so as to elucidate the great potential of sinomenine as a promising anti-tumor drug, and provide reference for further research on its anti-tumor mechanism.

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