1.Atractylodin-loaded PLGA nanoparticles:formulation and characterization
MUHAMAD NADDA ; PLENGSURIYAKARN TULLAYAKORN ; CHITTASUPHO CHUDA ; NA-BANGCHANG KESARA
Chinese Journal of Pharmacology and Toxicology 2018;32(4):244-244
OBJECTIVE To formulate atractylodin-loaded poly (lactic- co- glycolic acid) (PLGA) nanoparticles and characterize the prepared nanoparticle formulation.METHODS The nanoparticle formu-lation was developed using solvent displacement method. The encapsulation and loading efficiency were characterized and particle size, and zeta potential were determined by dynamic light scattering technique.Drug release was assessed in vitro.RESULTS The size(mean±SD of diameter)of the prepared atractylodin-loaded PLGA nanoparticles were (161.27 ± 1.87)nm with narrow size distribution (mean PDI: 0.068±0.015)and zeta potential(28.83±0.35)mV.The encapsulation and loading efficiency were (48.31±0.83)% and(2.15±0.04)%,respectively.Drug release from atractylodin-loaded PLGA nanoparticles was observed up to (87.70 ± 0.47)% in 72 h with biphasic manner. Moreover, the nanoparticles were found to be freely dispersible in water without aggregation. CONCLUSION Results suggest that PLGA nanoparticles may be used as an effective drug delivery system for atractylodin.The anti-cholangiocar-cinoma activity of this nanoparticle formulation is required.
2. Inhibitory activities of plumbagin on cell migration and invasion and inducing activity on cholangiocarcinoma cell apoptosis
Luxsana PANRIT ; Luxsana PANRIT ; Tullayakorn PLENGSURIYAKARN ; Pongsakorn MARTVISET ; Kesara NA-BANGCHANG ; Tullayakorn PLENGSURIYAKARN ; Kesara NA-BANGCHANG ; Pongsakorn MARTVISET
Asian Pacific Journal of Tropical Medicine 2018;11(7):430-435
Objective: To investigate the cytotoxic, apoptotic and inhibitory activities on cell migration and invasion of plumbagin in the human cholangiocarcinoma (CCA) cell line (CL-6) in comparison with human embryonic fibroblast cell line (OUMS). Methods: Cytotoxicity activity was evaluated using MTT assay. Inhibitory effect on cell migration and invasion were investigated using label-free real-time cell analysis and QCM ECMatrix cell invasion chamber, respectively. Apoptotic activity was evaluated using flow cytometry and CellEvent™ Caspase 3/7 assay. Results: Based on results of the cytotoxicity test in CL-6 cells, 50% inhibitory concentration (IC
3.In vitro cytotoxic and toxicological activities of ethanolic extract of Kaempferia galanga Linn. and its active component, ethyl-p-methoxycinnamate, against cholangiocarcinoma.
Porwornwisit TRITRIPMONGKOL ; Tullayakorn PLENGSURIYAKARN ; Mayuri TARASUK ; Kesara NA-BANGCHANG
Journal of Integrative Medicine 2020;18(4):326-333
OBJECTIVE:
To evaluate the cytotoxic, apoptotic, mutagenic and immunomodulatory activities of Kaempferia galanga Linn. (KG) extract and ethyl-p-methoxycinnamate (EPMC) in vitro.
METHODS:
The present study investigated the cytotoxic [using the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide test], apoptotic (using a mitochondrial membrane potential assay), mutagenic (using a micronucleus test) and immunomodulatory (using flow cytometry) activities of the ethanolic extract of KG and its bioactive component, EPMC, against two cholangiocarcinoma (CCA) cell lines, CL-6 and HuCCT1, and one normal human cell line, OUMS-36T-1F.
RESULTS:
Both KG extract and EPMC exhibited moderate cytotoxic activity against both CCA cells. The cytotoxic activity was supported by their concentration-dependent induction of apoptosis. CL-6 was most sensitive (3-4 fold) and selective to 5-fluorouracil (5-FU), compared with KG extract and EPMC [median half inhibiting concentration (IC) and selectivity index (SI) were 23.01 μg/mL and 17.32; 78.41 μg/mL and 4.44; 100.76 μg/mL and 2.20, respectively for 5-FU vs. KG extract vs. EPMC]. HuCCT1 was relatively more sensitive and selective to 5-FU and EPMC than KG extract [median IC and SI were 66.03 μg/mL and 6.04; 60.90 μg/mL and 3.65; 156.60 μg/mL and 2.23, respectively for 5-FU vs. EPMC vs. KG extract]. EPMC produced relatively potent cytotoxic activity against polymorphonuclear cells (IC = 92.20 μg/mL). KG extract and EPMC exhibited concentration-dependent mutagenic activity, as well as inhibition of tumor necrosis factor-α and interleukin-6.
CONCLUSION
Considering cytotoxic, apoptotic, immunomodulatory and mutagenic activities, further development of KG as a drug candidate is likely to focus on the oral pharmaceutical formulation of a standardized KG extract rather than isolated compounds.