Anticancer effect of the extracts from Polyalthia evecta against human hepatoma cell line(HepG2)

Objective:To investigate the anticancer activity of Polyalthia evecta(P.evecta)(Pierre) Finet & Gagnep against human hepatoma cell line(HepG2).Methods:The anticancer activity was based on(a) the cytotoxicity against human hepatoma cells(HepG2) assessed using a neutral red assay and(b) apoptosis induction determined by evaluation of nuclei morphological changes after DAP1 staining.Preliminary phytochemical analysis of the crude extract was assessed by HPLC analysis.Results:The 50% ethanol-water crude leaf extract of P.evecta(EW-L) showed greater potential anticancer activity with high cytotoxicity[IC_(50)=(62.8±7.3)μg/mL]and higher selectivity in HepG2 cells than normal Vero cells[selective index(SI)=7.9].The SI of EW-L was higher than the positive control,melphalan(SI=1.6) and the apoptotic cells(46.4±2.6)%induced by EW-L was higher than the melphalan(41.6±2.1)%(P<0.05).The HPLC chromatogram of the EW-L revealed the presence of various kinds of polyphenolics and flavonoids in it.Conclusions: P.evecta is a potential plant with anticancer activity.The isolation of pure compounds and determination of the bioactivity of individual compounds will be further performed.

Synergistic anticancer effect of the extracts from Polyalthia evecta caused apoptosis in human hepatoma(HepG2)cells

Objective:To evaluate the anticancer activity of the extract fraction of Polyalthia evecta(P. evecta)(Pierre) Finet & Gagnep and the synergistic anticancer effect of the extracts from P.evecta by using the ATR/FT-IR spectroscopy.Methods:The 50%ethanol-water crude leaf extract of P.evecta(EW-L) was prepared and was further fractionated to isolate various fractions.The anticancer activity was investigated from cytotoxicity against HepG2 using a neutral red assay and apoptosis induction by evaluation of nuclei morphological changes after DAPI staining. Synergistic anticancer effects of the extracts from P.evecta were performed using the ATR/FTIR spectroscopy.Results:The result showed that the EW-L showed higher cytotoxicity and apoptosis induction in HepG2 cells than its fractionated extracts.The hexane extract exhibited higher cytotoxicity and apoptosis induction than the water extracts,but less than the EW-L. The combined water and hexane extracts apparently increased cytotoxicity and apoptosis induction.The%apoptotic cells induced by the extract mixture were increased about 2-fold compared to the single hexane extract Conclusions:The polar extract fraction is necessary for the anticancer activity of the non-polar extract fraction.The ATR/FT-IR spectra illustrates the physical interaction among the constituents in the extract mixture and reveals the presence of polyphenolic constituents in the EW-L,which might play a role for the synergistic anticancer effect.

Effect of ABCB1 3435C>T transporter gene polymorphism on plasma efavirenz concentration in HIV-1 infected Thai adults

Objective:To investigate the influence of ABCB1 polymorphisms on the plasma level of efavirenz in Thai adult cases infected with HIV-1.Methods:A single nucleotide polymorphism of ABCB13435 C>T(rs1045642)in the gene encoding ABCB1 was genotyped using real-time PCR-based alleles in 149 HIV-infected Thai adults receiving efavirenz treatment.Plasma concentrations of efavirenz were measured by high-performance liquid chromatography 12 hr after administration.The relationship between plasma efavirenz concentrations and ABCB13435 C>T polymorphisms was analyzed.Results:Logistic regression analysis showed no significant predictors of high plasma efavirenz concentration in relation to age,gender,body weight,CD4 count and plasma HIV-1 RNA,blood biochemical parameters,antiretroviral duration or ABCB13435 C>T polymorphisms,except for height(OR=0.902,95%CI:0.835-0.973)(P<0.05).The minor allele frequency of ABCB13435 C>T was0.446.The frequency of the heterozygous mutant ABCB13435 C/T was 53.02%(n=79),ABCB13435 T/T homozygous mutant was 18.12%(n=21)and the wild type ABCB13435 C/C genotype was 28.86%(n=43).The overall median plasma concentration of efavirenz in 149 HIV-infected Thai cases was 2.41 mg/L[IQR:(1.46-4.12)mg/L].The plasma concentration of efavirenz was higher in cases with ABCB13435 T/T homozygous mutant[2.73 mg/L,IQR:(2.02-4.19)mg/L]and ABCB13435 C/T heterozygous mutant[2.29 mg/L,IQR:(1.41-4.28)mg/L]genotypes compared to the wild type ABCB13435 C/C homozygous[2.1 mg/L,IQR:(1.37-3.53)mg/L].However,there was no statistically significant difference in the efavirenz concentration between the different genotypes(P>0.05).Objective:To investigate the influence of ABCB1 polymorphisms on the plasma level of efavirenz in Thai adult cases infected with HIV-1.Methods:A single nucleotide polymorphism of ABCB13435 C>T(rs1045642)in the gene encoding ABCB1 was genotyped using real-time PCR-based alleles in 149 HIV-infected Thai adults receiving efavirenz treatment.Plasma concentrations of efavirenz were measured by high-performance liquid chromatography 12 hr after administration.The relationship between plasma efavirenz concentrations and ABCB13435 C>T polymorphisms was analyzed.Results:Logistic regression analysis showed no significant predictors of high plasma efavirenz concentration in relation to age,gender,body weight,CD4 count and plasma HIV-1 RNA,blood biochemical parameters,antiretroviral duration or ABCB13435 C>T polymorphisms,except for height(OR=0.902,95%CI:0.835-0.973)(P<0.05).The minor allele frequency of ABCB13435 C>T was 0.446.The frequency of the heterozygous mutant ABCB13435 C/T was 53.02%(n=79),ABCB13435 T/T homozygous mutant was 18.12%(n=27)and the wild type ABCB13435 C/C genotype was 28.86%(n=43).The overall median plasma concentration of efavirenz in 149 HIV-infected Thai cases was 2.41 mg/L[IQR:(1.46-4.12)mg/L].The plasma concentration of efavirenz was higher in cases with ABCB13435 T/T homozygous mutant[2.73 mg/L,IQR:(2.02-4.19)mg/L]and ABCB13435 C/T heterozygous mutant[2.29 mg/L,IQR:(1.41-4.28)mg/L]genotypes compared to the wild type ABCB13435 C/C homozygous[2.1 mg/L,IQR:(1.37-3.53)mg/L].However,there was no statistically significant difference in the efavirenz concentration between the different genotypes(P>0.05).Conclusions:There is no statistical significance for a tendency toward higher plasma efavirenz concentration in the ABCB13435 T/T and ABCB13435 C/T genotypes.No parameters of physiological characteristics in this study except for height were found to be predictors of high plasma efavirenz concentration in Thai HIV-1 infected cases.