Total Saponins in Paridis Rhizoma： A Review / 中国实验方剂学杂志

Paridis Rhizoma possesses the functions of clearing heat and detoxifying， alleviating swelling and relieving pain， cooling the liver and calming the convulsion. Saponins are the main active components of Paridis Rhizoma. Studies have shown that total saponins in Paridis Rhizoma have obvious inhibitory effect on solid tumors such as breast cancer， lung cancer， gastric cancer， and liver cancer and non-solid tumors such as leukemia. The saponins may exert the anti-tumor effects by inhibiting the proliferation， migration， and invasion of tumor cells， regulating cell cycle， inducing apoptotic and non-apoptotic death pathways， and regulating metabolism and tumor microenvironment. Furthermore， total saponins in Paridis Rhizoma showed anti-inflammatory， antioxidant， antimicrobial， hemostatic， and uterus-contracting activities. At the same time， they may induce apoptosis of normal cells， inflammation and oxidative stress， and metabolic disorders. In recent years， the reports of liver injury， reproductive injury， gastrointestinal injury， hemolysis， and other adverse reactions caused by total saponins in Paridis Rhizoma have been increasing. Pharmacokinetic studies have shown that there are significant differences in the metabolism of total saponins in Paridis Rhizoma administrated in different ways. Injection has a fast clearance rate， while oral administration may have hepatoenteric circulation. Meanwhile， due to the low solubility and activation of P-glycoprotein （P-gp） molecular pump， the prototype absorption， intestinal permeability， and recovery rate of total saponins in Paridis Rhizoma are poor， which affects the bioavailability. The bioavailability can be improved to some extent by preparing new dosage forms or new drug delivery systems with advanced technology. This paper reviews the pharmacological effect， pharmacokinetics， and adverse reactions of Rhizoma Paridis total saponins by searching the China National Knowledge Infrastructure （CNKI）， VIP， and Web of Science with ''Rhizoma Paridis total saponins'' as the keywords， hoping to provide references for the research， development， and clinical application of such components.

Research progress on metabolism and efficacy of small molecular prodrug nanosystems responsive to tumor redox microenvironment / 药学学报

Compared with normal tissues and cells, the tumor microenvironment has significant differences. For example, glutathione-related metabolic enzymes and reactive oxygen species are highly expressed in different subcellular structures, resulting in an unbalanced redox state. Aiming at the specific redox state in tumor tissues and cells, a series of small molecule prodrug self-assembled nanoparticles can be designed and connected by intelligent response linkers including disulfide bonds, sulfide bonds, and selenium bonds, thioketal bonds, etc. The in vitro and in vivo efficiency and metabolic mode of these nanoparticles are related to the type of linker. This review will summarize the tumor redox microenvironment, the design of intelligent responsive small molecule prodrug nanoparticles, and the metabolic pathways of small molecule prodrug nanoparticles with different connecting linkers and their relationship with drug efficacy.

New possible silver lining for pancreatic cancer therapy: Hydrogen sulfide and its donors

As one of the most lethal diseases, pancreatic cancer shows a dismal overall prognosis and high resistance to most treatment modalities. Furthermore, pancreatic cancer escapes early detection during the curable period because early symptoms rarely emerge and specific markers for this disease have not been found. Although combinations of new drugs, multimodal therapies, and adjuvants prolong survival, most patients still relapse after surgery and eventually die. Consequently, the search for more effective treatments for pancreatic cancer is highly relevant and justified. As a newly re-discovered mediator of gasotransmission, hydrogen sulfide (H

Antitumor Effects of Ethanol Extract from Ventilago leiocarpa Benth on Sarcoma 180 Tumor-Bearing Mice and Possible Immune Mechanism / 中国结合医学杂志

OBJECTIVE@#To explore the antitumor effects of ethanol extract from Ventilago leiocarpa Benth (EEVLB) on sarcoma 180 (S180) tumor-bearing mice and the potential mechanism.@*METHODS@#Sixty mice were randomly assigned to 6 groups according to a random number table: normal group, model group, 5-fluorouracil (5-FU) group (0.02 g·kg@*RESULTS@#EEVLB with different concentrations achieved inhibition of tumor growth in vivo, wherein the high-dose group showed the most significant reduction in tumor weight and increased apoptosis of tumor cells (P<0.05). In addition, both net weight gain and spleen index of mice showed uptrend in EEVLB treatment groups (P<0.05). Besides, serum levels of IL-2 and IL-6, percentages of CD3@*CONCLUSIONS@#EEVLB exhibits promising antitumor activity in vivo. This effect might be due to activation of apoptotic signaling pathway, increase of cytokine levels and enhancement of immune function in tumor-bearing mice.

In vitro antitumor effect of cucurbitacin E on human lung cancer cell line and its molecular mechanism / 中国天然药物

Cucurbitacin E (CuE) is previously reported to exhibit antitumor effect by several means. In this study, CuE acted as a tyrosine kinase inhibitor interfering with the epidermal growth factor receptor/mitogen-activated protein kinase (EGFR/MAPK) signaling pathway and subsequently induced apoptosis and cell cycle arrest in non-small-cell lung cancer (NSCLC) cell line A549. The apoptosis regulators, cleaved Caspases-3 and Caspases-9, were observed to be increased with the treatment of CuE. The activated transcription factor STAT3 and the apoptosis inhibitor protein survivin were also observed to be reduced. The cell cycle regulators, CyclinA2, cylinB1, CyclinD1 and CyclinE, were also investigated and the results suggested that the cell cycle was arrested at G1/G0 phase. Treatment of CuE also altered the existence status of most of the participants in the EGFR/MAPK signaling. Phosphorylation of EGFR enhanced significantly, leading to the alteration of members downstream, either total amount or phosphorylation level, notably, MEK1/2 and ERK1/2. Moreover, the results of molecular simulation brought an insight on the interaction mechanism between CuE and EGFR. In summary, CuE exhibited anti-proliferative effect against A549 cells by targeting the EGFR/MAPK signaling pathway.

Metformin inhibits proliferation and functions of regulatory T cells in acidic environment / 南方医科大学学报

OBJECTIVE@#To investigate the regulatory effect of metformin on regulatory T cells (Treg) in acidic environment.@*METHODS@#CD4 CD25 Treg cells were obtained by magnetic bead sorting. Treg and conventional T cells (Tcon) cells were cultured for 24-72 h in pH 7.4 or pH 6.7 medium, and the cell proliferation, apoptosis and Foxp3 expression were detected by flow cytometry. Real-time PCR was used to detect the expression levels of the genes related with glucose metabolism. Thirty-two C57BL/6 male mouse models bearing subcutaneous prostate cancer xenograft derived from RM-1 cells were randomized into 4 equal groups for treatment with PBS, metformin, tumor vaccine, or both metformin and the vaccine. The treatment started on the 4th day following tumor cell injection, and metformin (100 mg/kg) or PBS was administered by intraperitoneal injection on a daily basis; the vaccine was intramuscularly injected every 4 days. The tumor size was continuously monitored, and the mice were euthanized on day 25 after tumor implantation to obtain tumor and blood samples. Flow cytometry was used to detect the changes in CD4, CD8, CD4Foxp3 cell subsets in the tumor tissue and peripheral blood.@*RESULTS@#Treg cells showed significantly enhanced proliferation ( < 0.05) while the proliferation of Tcon cells was suppressed in acidic medium ( < 0.001). Treg cells cultured in acidic medium showed significantly increased expressions of OXPHOS-related genes pgc1a ( < 0.001) and cox5b ( < 0.01), which did not vary significantly in Tcon cells in acidic medium. Treg cells exhibited significantly decreased apoptosis in acidic medium ( < 0.01) with increased Foxp3 cells ( < 0.001) and intracellular alkaline levels ( < 0.01). Metformin obviously reversed the acid tolerance of Treg cells without producing significant effect on Tcon cells. In the animal experiment, both metformin ( < 0.05) and vaccine ( < 0.01) alone reduced the tumor volume, but their combined treatment more potently reduced the tumor volume ( < 0.001). Metformin alone did not obviously affect CD4 cells or CD8 cells but significantly decreased the percentage of CD4Foxp3 ( < 0.05); the vaccine alone significantly increased CD4 cells and CD8 cells ( < 0.001) and also the percentage of CD4Foxp3 cells ( < 0.05). The combined treatment, while reducing the percentage of CD4Foxp3cells to a level lower than that in the vaccine group ( < 0.01), produced the strongest effect to increase CD4 cells and CD8 cells ( < 0.01).@*CONCLUSIONS@#Metformin can inhibit the proliferation and function of regulatory T cells in an acidic environment and enhance the effect of tumor vaccine by reducing the proportion of Treg cells to achieve the anti-tumor effect.

Preparation of Magnetic Solid Lipid Nanoparticles Co-loaded Quercetin and Resveratrol and Evaluation of Its Antitumor Effect / 中国实验方剂学杂志

Objective:To prepare magnetic solid lipid nanoparticles co-loaded quercetin and resveratrol(QR-MSLN),develop the reasonable characterization method,and investigate its inhibitory effect on transplanted hepatocarcinoma H22 tumor in mice. Method:Magnetic Fe3O4 particles coated with oleic acid(OA-Fe3O4) were synthesized and its structure was confirmed by Fourier transform infrared spectrometer(FT-IR).QR-MSLN was prepared by emulsion ultrasonic dispersion method,its morphology was examined by transmission electron microscopy,its particle size was determined by laser particle sizer.Concentration of Fe in the preparation was determined by phenanthroline spectrophotometry.The entrapment efficiency,saturation magnetization,in vitro release behavior were investigated by ultrafiltration centrifugation,vibrating sample magnetometer(VSM) and dialysis method,respectively.Mouse tumor model transplanted with hepatoma H22 ascites tumor was established and antitumor effect of QR-MSLN on H22 bearing mice were observed in the presence of an applied magnetic field. Result:Morphology of QR-MSLN was round,and black magnetic particles could be observed inside it,its particle size was (171.9±2.2) nm,the concentration of Fe was (1.40±0.46) g·L-1.The preparation exhibited apparent superparamagnetism and the saturation magnetization was 7.75 A·m2·kg-1.The entrapment efficiencies of quercetin and resveratrol in QR-MSLN were 99.10% and 80.83%,respectively.QR-MSLN had a significantly higher effect of tumor inhibition than SLN(containing quercetin and resveratrol) and free drug(PConclusion:QR-MSLN has uniform particle size and good magnetic response,and shows remarkable antitumor effect on H22 bearing mice.

Research progress on pharmacological effect of Artemisiae Scopariae Herba / 中草药

The main chemical components of Artemisiae Scopariae Herba (ASH) include coumarins, flavonoids, organic acids, essential oils, and so on. Except for the traditional actions of clearing and draining dampness-heat, and disinhibiting gallbladder and anti-icteric, ASH has multiple pharmacological activities, such as antipyretic, analgesic, anti-inflammatory, antiviral, antitumor, hypotensive, hypolipidemic, anti-osteoporotic, neuroprotective, metabolic regulation effects, as well as prevention of Alzheimer’s disease, whose mechanism of actions are complex. This article reviews pharmacological actions and the corresponding mechanism of ASH, which can provide reference for the research, development and clinical application of ASH and its preparations.

In Vitro and In Vivo Evaluation of Antitumor Activity of Ligustrum robustum, A Chinese Herbal Tea / 中国结合医学杂志

OBJECTIVE@#To examine the effect of the aqueous extract of Ligustrum robustum on tumor growth in vitro and in vivo and explore the possible molecular mechanisms.@*METHODS@#In in vitro study, cell viabilities of human cervical carcinoma cells (HeLa), human breast cancer cells (MCF-7), human prostate cancer cells (PC-3), human hepatoma cells (7721) and human colon carcinoma cells (SW480) were evaluated with cell counting kit-8. For L. robustum-treated Hela cells, early or late apoptosis were evaluated by annexin V/PI staining. Mitochondrial membrane potential was measured by staining cells with JC-1. Apoptosis was monitored by nuclear morphology based on chromatin condensation and fragmentation by 4',6-diamidino-2-phenylinole (DAPI) staining. Caspase-3 and -8 activity levels were measured by a colorimetric assay. In vivo, to evaluate the possible mechanism of L. robustum-mediated antitumor effect, nude mouse xenograft study was also conducted.@*RESULTS@#In in vitro study, L. robustum was found to be toxic to HeLa, MCF-7, PC-3, 7721, SW480, with an half maximal inhibitory concentration value of 2-5 mg/mL (P<0.05). Moreover, externalization of phosphatidylserine, loss of mitochondrial membrane potential, DNA fragmentation and activation of caspase-3 and -8 were detected in L. robustum-treated Hela cells. Using a nude mouse model bearing Hela xenografts, we found that L. robustum reduced tumor volume and tumor weight (P<0.05), but had no effect on body weight and histological damage of important organs. Intraperitoneal injection of L. robustum caused a significant reduction in serum aspartate transaminase and alanine transaminase levels (P<0.05). Furthermore, cleaved caspase-3-positive and terminal nucleotidyl transferase-mediated nick end labeling (TUNEL)-positive cells were observed in L. robustum-treated tumor tissues.@*CONCLUSIONS@#L. robustum inhibits tumor cell growth both in vitro and in vivo by inducing apoptosis in a caspase-dependent way without apparent hepatic toxicity and histological damage, which may offer partial scientific support for the ethnopharmacological claims of L. robustum as a herbal tea for its antitumor activity.

Antitumor effect and mechanism of tropolones / 国际药学研究杂志

Tropolones,non-benzenoid aromatic compounds with a seven-numbered-ring structure,are mainly found in the secondary metabolites of fungi.Tropolones are characterized by the antibacterial,antifungal,antiviral,anti-inflammatory,insecticidal, and antitumor activities.Antitumor effect has been extensively explored in recent years,but so far there is still no ideal antitumor drug-candidates obtained from these compounds.The research progress of antitumor effect and mechanism of tropolones are reviewed in this paper for a reference for the future.

Preparation and anti-tumor effect of quercetin nano-liposome / 中国基层医药

Objective To prepare quercetin liposome and to explore the antitumor effect of quercetin liposome.Methods The cholesterol and lecithin were used as membrane materials,quercetin nano liposome was prepared by thin film ultrasound method.The zeta potential and particle size distribution of quercetin liposome were tested by Malvern laser particle size analyzer and transmission electron microscope respectively.In order to explore the anti-tumor effect of quercetin nano-liposome,the mouse model of cervical cancer was established.After tail vein injection of quercetin and quercetin nano-liposome for 15 days,the tumor inhibitory rate,the thymus (spleen) index were analyzed,and the pathology of tumor tissues was further observed.Results Under the condition of lecithin∶cholesterol ∶ quercetin =8 ∶ 2 ∶ 1,the hydration time of 15 min and the ultrasonic time of 15 min,the quercetin nano-liposome was prepared,and the particle size distribution was uniform and the potential was-10.8.The tumor inhibitory rate of quercetin nano-liposome treatment group was 54.16％,which was significantly higher than that of the quercetin treatment group (x2 =6.477,P ＜ 0.05).The pathology results of the tumor tissues showed that nanocrystallization of quercetin could increase the anti-cancer effect of quercetin.Conclusion Both quercetin and quercetin nano-liposome exhibit significant effect on the tumor growth,and the inhibitory rate is increased after quercetin was nanocrystallization.Our study will provide theoretical basis for the application of quercetin nano-liposome in the treatment of cervical cancer.

Antitumor Effect of Phellinus Linteus Polysaccharide on Sarcoma S180 Cells in vivo and in vitro / 中国药房

OBJECTIVE:To study the antitumor effect of phellinus linteus polysaccharide on sarcoma S180 cells in vivo and in vitro. METHODS:Sarcoma S180 cells in logarithmic growth period were selected,adding into 0(blank control),2,4,8 mg/mL phellinus linteus polysaccharide solution and respectively culturing for 12,24,36,48 h. The in vitro proliferation inhibition rate of cells was determined by MTT method;its apoptotic morphology was observed by fluorescence staining and cell apoptosis rate was detected by flow cytometry. S180 tumor-bearing mice models were established and randomly divided into control group,phellinus linteus polysaccharide high-dose,medium-dose,low-dose groups(400,200,100 mg/kg),10 in each group. Model mice were in-tragastrically administrated related medicined,once a day,for 12 d. Mice were executed after 24 h of last administration,tumor weight was determined,tumor inhibition rate was calculated. Immunohistochemistry was conducted to detect the tumor suppressor gene PTEN and oncogene C-myc protein expressions in tumor tissue. RESULTS:Compared with blank control group,phellinus linteus polysaccharide can increase the proliferation inhibition rate of S180 cells and induce the increase of apoptosis rate(P<0.05 or P<0.01),showing a concentration-time manner. Compared with control group,the tumor inhibition rates in phellinus linteus polysaccharide groups were obviously increased (P<0.01),PTEN protein expressions were strengthened (P<0.05 or P<0.01) and C-myc protein expressions were weakened (P<0.05). CONCLUSIONS:Phellinus linteus polysaccharide shows antitumor ef-fect in vivo and in vitro,which can up-regulate the PTEN,down-regulate C-myc protein expressions.

Research progress on chemical constituents and pharmacological activities of Bufonis Venenum / 中草药

Bufonis Venenum, as an important Chinese traditional natural medicine, has complex chemical composition and has been widely used in clinical treatment with significant effects. The chemical constituents in Bufonis Venenum mainly included bufadienolides, indole alkaloids, steriods, etc. With the further research on Bufonis Venenum both at home and abroad, its chemical composition and mechanism of pharmacological activities have been more and more clearly, especially in the aspects of narcotic analgesic, cardiac, and antitumor therapy. This paper reviewed the chemical composition and pharmacology advances of Bufonis Venenum in order to provide reference to clinical use.

Preparation of Hispidulin Liposomes and Its Antitumor Effect in Vitro / 中国药学杂志

OBJECTIVE: To study the preparing METHODS of hispidulin liposomes and evaluate their antitumor effects in vitro. METHODS: Hispidulin liposomes were prepared by thin film dispersion method, and the formulation was further optimized. At the same time, the liposomes particle size and Zeta potential were characterized separately. The antiproliferative effect of the liposomes on A549 cells was investigated by sulforhodamine B(SRB) method. RESULTS: According to the optimal prescription, the encapsulation efficiency of hispidulin liposomes was (87.06±0.67)%. Additionally, the average particle size was (104.83±1.40) nm and the Zeta potential was (-4.61±0.32) mV. Furthermore, the hispidulin liposomes exhibited the strongest inhibiting effect on A549 cells in vitro with comparison with control groups. CONCLUSION: The preparation method builtin our research is easy. And the liposomes are well distributed with high encapsulation efficiency. Meanwhile, the hispidulin liposomes exhibit the most significant antitumor effects in vitro.

Inhibition of Yuyihe Powder on Tumor Growth in Mice Models of Sarcoma 180 / 中草药·英文版

Objective To explore the antitumor effect of Yuyihe Powder (Yu Yi He San, YYHS) and its antitumor mechanism. Methods After treatment, tumor weight, immune apparatus weight, the life span of transplanted animals, spleen lymphocyte proliferation assays, and IL-2 concentration in mouse serum were recorded or detected. Results YYHS showed strong antitumor ability. Compared with control group, mid-dose YYHS (1.0 g/kg) could inhibit the tumor growth, prolong the life span of S180-bearing mice to some extent, significantly increase the thymic and splenic indices of S180 mice, and strongly promote the secretion of IL-2 in blood; The inhibitory rate on tumor growth and life prolongation rate were 37.1% and 38.37%, respectively. Conclusion YYHS could not only significantly inhibit the growth of S180 cells, but also markedly prolong the survival time of S180 bearing mice. The mechanism of antitumor effect could obviously enhance immunologic function of the S180 bearing mice to inhibit the growth of S180 cells.

Preparation of Vinorelbine-tetrandrine Liposomes Modified with RGD and Study on the in vitro Antitumor Effect / 中国药房

OBJECTIVE:To prepare the vinorelbine-tetrandrine liposomes modified with RGD,and study the inhibitory effect on glioma C6 cells. METHODS:Film dispersion method and ammonium sulfate gradient method were used to prepare the vinorel-bine-tetrandrine liposomes modified with RGD,and the morphology and particle size distribution were observed. The vinorelbine content was determined,and sulforhodamine B method was used to respectively determine the inhibitory effects of blank targeting liposomes,normal vinorelbine liposomes and vinorelbine-tetrandrine liposomes modified with RGD on C6 cells. RESULTS:The prepared vinorelbine-tetrandrine liposomes modified with RGD were spherical or almost spherical with smooth surface,and particle size was about 120 nm. The average content of vinorelbine was 28.27 μg/mL(RSD=0.38％,n=3). Blank targeting liposomes had no significant effect on the growth of C6 cells;vinorelbine-tetrandrine liposomes modified with RGD can obviously inhibit the growth of C6 cells,and cell viability after its effect was significantly lower than normal vinorelbine liposomes (P<0.05). CON-CLUSIONS:Vinorelbine-tetrandrine liposomes modified with RGD are successfully prepared,and they show obvious inhibitory ef-fects on the growth of C6 cells.

Preparation of Norcantharidin Nano-micelle and Study on Its Antitumor Effect / 中国药房

OBJECTIVE:To prepare the norcantharidin (NCTD) nano-micelle and study its antitumor effect. METHODS:NCTD nano-micelle was self-formed in water using Triblock copolymers distearyl phosphatidylethanolamine-polyethylene glycol-ma-leimide;its shape was observed,the drug-loading rate,entrapment efficiency,particle size,Zeta potential were investigated. MTT was used to investigate the cell survival rate of human lung cancer A549 cells in negative control group (Phosphate buffer solu-tion),carrier group (blank nano-micelle),positive control group (NCTD APIs,5-320 μg/mL) and NCTD nano-micelle group (NCTD,5-320 μg/mL) after acting different time (24,48,72 h). Tumor nude mice were randomly divided into blank control group,NCTD injection group(1 mg/kg),NCTD low-dose,high-dose groups(0.5,1 mg/kg),6 in each group. All mice were in-travenously injected relevant medicines in tail,once a day,for 8 weeks. Tumor size was measured every week,and tumor quality was detected after the second day of finishing administration. RESULTS:NCTD nano-micelle was round,drug-loading rate was (2.82±0.05)%,entrapment efficiency was(83.67±1.78)%,particle size was(138.6±45.8)nm,Zeta potential was -(12.75± 0.34)mV(n=6). Cell survival rate of A549 cells in carrier group had no obvious changes,and was obviously decreased in posi-tive control group and NCTD nano-micelle group,which was positively correlated with concentration and time. And the decrease degree of cell survival rate in NCTD nano-micelle group was stronger than positive control group(P<0.01). Compared with blank control group,the tumor quality of mice in 3 administration groups was reduced (P<0.05),the reduction degree in NCTD na-no-micelle high-dose group was stronger than NCTD nano-micelle injection group (P<0.05). CONCLUSIONS:NCTD nano-mi-celle is successfully prepared,which has good in vitro and in vitro anti-tumor effect on A549 cells.

Metformin displays in vitro and in vivo antitumor effect against osteosarcoma / 소아과

PURPOSE: Patients with unresectable, relapsed, or refractory osteosarcoma need a novel therapeutic agent. Metformin is a biguanide derivative used in the treatment of type II diabetes, and is recently gaining attention in cancer research. METHODS: We evaluated the effect of metformin against human osteosarcoma. Four osteosarcoma cell lines (KHOS/NP, HOS, MG-63, U-2 OS) were treated with metformin and cell proliferation was evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Cell cycle progression and apoptosis were evaluated using flow cytometric analysis, and migration and wound healing assay were performed. Fourteen female Balb/c-nude mice received KHOS/NP cell grafts in their thigh, and were allowed access to metformin containing water (2 mg/mL) ad libitum. Tumor volume was measured every 3–4 days for a period of 4 weeks. RESULTS: Metformin had a significant antiproliferative effect on human osteosarcoma cells. In particular, metformin inhibited the proliferation and migration of KHOS/NP cells by activation of AMP-activated protein kinase and consequent inhibition of the mammalian target of rapamycin pathway. It also inhibited the proliferation of cisplatin-resistant KHOS/NP clone cells. Analysis of KHOS/NP xenograft Balb/c-nude models indicated that metformin displayed potent in vivo antitumor effects. CONCLUSION: Further studies are necessary to explore metformin's therapeutic potential and the possibilities for its use as an adjuvant agent for osteosarcoma.

Antitumor effect of 16-dehydropregnenoione liposomes / 中国药学杂志

OBJECTIVE: To investigate the antitumor effect of 16-dehydropregnenolone (16-DHP) liposomes. METHODS: Twelve kinds of tumor cells were used to determine the cytotoxic effect of 16-DHP liposome by MTT assay. The established tumor xenograft in nude mouse model was used to evaluate anti-tumor effect of 16-DHP liposomes after tail vein injection. RESULTS: IC50 value of 16-DHP liposomes to the human hepatoma cell HepG2, human oral carcinoma KB cell, human breast cancer T47D, human gastric cancer cell SGC7901, human fibrosarcoma cell HT1080, human ovarian cancer cell SKOV3, human prostate cancer cell PC3, human prostrate cancer cell DU145, human lung cancer cell A549, human rhabdomyosarcoma A204 cell and human cervical carcinoma cell HeLa were 44.69, 9.17, 26.22, 19.58, 28.01, 37.18, 24.58, 21.38, 54.69, 4.18 and 8.96 μg · mL-1, respectively. The relative tumor increment rate and inhibition rates of tumor weight were 93.7%, 60.52%, 37.84% and 23.05%, 48.84%, 69.70% respectively after treated with 16-DHP liposomes (7.5, 15 and 30 mg · kg-1 · d-1, 28 d). CONCLUSION: 16-DHP liposomes possess in vitro and in vivo anti-tumor activities.

Antitumor mechanism of mouse colon cancer cells transfected with IL-17 gene in vivo / 中国免疫学杂志

Objective:To investigate the effects of interleukin-17 on tumor,we transfected interleukin-17 gene into mouse colon cancer cells(C26)and set up an animal model in tumor.Methods:By plasmid vector,IL-17 gene was transfected into C26.Meanwhile, empty plasmid vector(pcDNA3.1)and C26 cells were transfected as control groups.C26/pcDNA3.1-IL-17,C26/pcDNA3.1,and C26 cells were subcutaneously inoculated into mice respectively and the tumor volume and the survival time were observed.Proliferation of splenocyte and NK activity were detected.Detect the characteristic cytokines and transcriptional factors of Th1,Th2,Th17 and Treg cells in splenic lymphocyte.Proliferation of TIL was detected.The characteristic cytokines IL-10 of M1 and the characteristic cytokines IL-12 of M2 in tumor infiltrating macrophages were detected.Results: The growth of tumor in mice inoculated with C26/pcDNA3.1-IL-17 cells was significantly retarded ( P0.05).The proliferation of the splenocytes from C26/pcDNA3.1-IL-17 inoculated mice was higher than those of C26/pcDNA3.1,C26 groups(P0.05),the proliferation of the splenocytes from C26/pcDNA3.1 and C26 inoculated mice was slow than those of normal groups(P0.05 ).The splenocytes from the mice inoculated with C26/pcDNA3.1-IL-17 cells secreted more IFN-γ( the characteristic cytokines of Th1 ) , IL-4 ( the characteristic cytokines of Th2),GATA-3,ROR-γt,IL-10(the characteristic cytokines of Treg)mRNA(P<0.05).The proliferation of TIL from C26/pcDNA3.1-IL-17 inoculated mice was higher than those of C26/pcDNA3.1,C26 groups(P<0.05),the proliferation of TIL from C26/pcDNA3.1-IL-17,C26/pcDNA3.1 and C26 inoculated mice was lower than those of normal groups( P<0.05).And there′s no differences among every groups of the express of cytokines IL-10 and IL-12 mRNA in tumor infiltrating macrophages(P<0.05).Conclusion: The transfection of IL-17 gene inhibited tumor growth in the mice,inoculated with enhancing the immune function.