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Objective:To investigate the effect of coix seed oil on chemosensitivity of colon cancer cells.Methods:HT29 cell line was cultured in vitro. Different concentrations of coix seed oil (1, 2, 4, 8 mg/ml) and 30 μg/ml 5-fluorouracil (5-FU) were incubated with HT29 cells for 24 hours to simulate chemotherapy. The cell proliferation inhibition rate, apoptosis rate and cell cycle ratio were measured by methyl thiazolyl tetrazolium (MTT) method and flow cytometry, and the protein expression of cleaved caspase-3 was measured by Western blot. Results:The inhibition rate of cell proliferation in 1, 2, 4, 8 mg/ml coix oil + 5-FU group was significantly higher than that in 5-FU group and coix oil group, and the inhibition rate in 2, 4, 8 mg/ml coix oil + 5-FU group was significantly higher than that in 1 mg/ml coix oil + 5-FU group ( P<0.05). The apoptosis rate in 5-FU group, coix oil group and 1, 2, 4, 8 mg/ml coix oil + 5-FU group was higher than that in the blank control group ( P<0.05). The apoptosis rate in 1, 2, 4, 8 mg/ml coix oil + 5-FU group was significantly higher than that in 5-FU group and coix oil group ( P<0.05). The apoptosis rate of 2, 4, 8 mg/ml coix oil + 5-FU group was significantly higher than that of 1 mg/ml coix oil + 5-FU group ( P<0.05). The expression of cleaved caspase-3 in each group was basically in line with the apoptosis rate of flow cytometry. The percentage of G1/M phase cells in 5-FU group, coix oil group and 1, 2, 4, 8 mg/ml coix oil + 5-FU group was significantly higher than that in the blank control, and the percentage of S phase cells was lower comparing with blank control ( P<0.05). Besides, the percentage of G1/M phase cells in 1, 2, 4, 8 mg/ml coix oil + 5-FU group was significantly higher than that in 5-FU group and coix oil group, and the percentage of S phase cells was significantly lower than that in 5-FU group and coix oil group ( P<0.05). The percentage of G1/M phase cells in 2, 4, 8 mg/ml coix oil + 5-FU group was significantly higher than that in 1 mg/ml coix oil + 5-FU group, and the percentage of S phase cells was significantly lower than that in 1 mg/ml coix oil + 5-FU group ( P<0.05). Conclusions:Coix seed oil may enhance the chemosensitivity of colon cancer cells by inducing cell cycle arrest and apoptosis.
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To optimize the formulation and preparation process of icaritin-coix seed oil microemulsion(IC-MEs) based on quality by design(QbD) concept. IC-MEs were prepared by water titration. Firstly, the risk factors that may affect the quality of IC-MEs were evaluated. Then Plackett-Burman design was used to screen out prescription factors and process parameters that had a significant effect on the indicators. Finally, Box-Behnken design was used to optimize the prescription ratio of IC-MEs. Through the risk assessment and Plackett-Burman design, three formulation factors [drug loading efficiency, the ratio of mixed-oil(coix seed oil-Glycerol tributyrate) to mixed-surfactant(HS15-RH40) and water addition] were determined as the key factors affecting IC-MEs. The regression model established by Box-Behnken design had a good predictability. The optimal formula was as following: the drug loading efficiency of 0.92%, the ratio of mixed-oil(coix seed oil-glycerol tributyrate) to mixed-surfactant(HS15-RH40) of 4∶6, and the water addition of 5.7 mL. According to this prescription, IC-MEs were prepared, and its encapsulation efficiency after 1 week was 92.45%±1.00%. Therefore, the stability of IC-MEs could be improved by optimizing prescription and process parameters of IC-MEs based on the QbD concept, which can provide certain reference value for the future development of IC-MEs.
Subject(s)
Coix , Emulsions , Flavonoids , Plant OilsABSTRACT
This study was designed to explore the mechanism of Coix seed oil (Coix) impact on the drug resistance, bioluminescence imaging (BLI) and the efflux of D-luciferin potassium salt, the substrate of ABC transporters, in doxorubicin-resistant breast cancer cells. Multidrug resistance (MDR) gene and protein expression were analyzed in the cells by q-PCR and Western blot. First, in order to investigate the effect of the efflux function by ABC protein, a cell line with overexpressed luciferase was established in MCF-7 cell line. BLI was used to monitor the efflux kinetics of D-luciferin potassium salt before and after Coix treament. The results showed that the efflux of D-fluorescein potassium from MCF-7/DOXFluc was lessened when pretreated with Coix, which means that Coix may decrease the efflux of other chemotherapies using ABC transporters. Both of the results of q-PCR and Western blot showed that gene and protein expression of ABC transporters such as ABCG2, ABCC1 and ABCB1 were down-regulated by Coix treatment. The efficacy of Coix reversing MDR was verified with the chemotherapy medication doxorubicin (DOX). MTT assay showed that Coix increased the inhibitory effect of DOX on proliferation of MCF-7/DOX, and the optimal combination of ratio was 25 times that of DOX. The results suggest that Coix may reverse MDR of the substrate of ABC transporters from two aspects, one is to cut down the ABC protein efflux function, and the other is to decrease the quantity of ABC gene and protein expression.
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This study was aimed to prepare tripterine-coix seed component microemulsions (TCC-MEs) with coix seed oil and coix seed polysaccharide as bimodal excipients and evaluate its activity on anti-lung cancer in vivo.Coix seed oil was extracted by supercritical extraction methods and coix seed polysaccharide was obtained through hot water extraction and alcohol precipitation from coix seed.Then,coix seed oil was used as the oil phase,and coix seed polysaccharide aqueous solution was used as the aqueous phase.RH40 was used as the surfactant.PEG400 was used as cosurfactant to prepare microemulsion.TCC-MEs were made by water titration method and characterized by size,polymer dispersity index (PDI),zeta potential,encapsulation efficiency and drug loading capacity.And then,anti-tumor activity of TCC-MEs was evaluated on the xenograft Lewis tumor mouse models.The liver and kidney toxicity was evaluated by HE staining and biochemical indicators.The results showed that the optimized prescription for TCC-MEs was coix seed oil 400 mg,RH40 300 mg,PEG 400 100 mg,coix seed polysaccharide 50 mg,tripterine 10 mg;and the tripterine encapsulation efficiency was (90.72 ± 0.28)％;the drug loading capacity was (1.08 ± 0.17)％;the mean diameter of microemulsion was (43.86 ± 0.22) nm;PDI was 0.10 ± 0.01;the zeta potential was (-13.14 ± 1.35) mV.The activity of anti-lung cancer in TCC-MEs was significantly better than that of the control group,with no significant liver and kidney toxicity after treatment with TCC-MEs.It was concluded that the prepared TCC-MEs had advantages of small amount of conventional auxiliary materials,small particle size and high stability.This study showed that the combination of triptolide and coix seed to microemulsion system has synergistic and attenuated effect.
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OBJECTIVE: To delevop a UPLC-MS method for determining the content of olein in rat plasma, and investigate the pharmacokinetics and bioavailability of nanoparticles of coix seed oil in rats. METHODS: The rats were divided into three groups randomly. They were administered orally suspension of the raw material of the coix seed oil, Kang lai te soft capsules and nanoparticles of coix seed oil, respectively. Blood samples were collected at 0.083, 0.167, 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, and 120 h and the concentrations of olein in rat plasma were determined by UPLC-MS. The pharmacokinetic parameters were calculated by 3P97 pharmacokinetic program. RESULTS: The pharmacokinetic parameters of olein in the the raw material of coix seed oil, KLT soft capsules and nanoparticles of coix seed oil in rat plasma were as follows: ρmax were (5.43±0.45), (7.54±0.44) and (7.30±1.13) mg·L-1, respectively, with significant difference between the nanoparticles and raw material (P0.05); AUC0-∞ were (68.71±5.12), (46.61±3.86), and (178.91±6.26) mg·h·L-1, respectively, which was the highest for the nanoparticles. The relative bioavailability of olein in the nanoparticles of coix seed oil was 260.38% to the raw material and 383.84% to the common oral prepatation. CONCLUSION : The nanoparticles system can increase the bioavailability of coix seed oil and improve its biopharmaceutical property.
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AlM: To study the effects of different concentrations of Coix seed oil on human retinal capillary endothelial cells ( HRCECs ) proliferation and vascular endothelial growth factor ( VEGF) expression in high glucose environment. METHODS: HRCECs extracted from human fresher eyeball and cultured in vitro, and ultimately used in the experiment were the growth of 3rd ~ 4th cells, the experimental were divided into blank control group, low glucose control group, high glucose control group, high glucose + ( 50ü L/mL, 100ü L/mL, 200ü L/mL ) different concentrations Coix seed oil group. Detecting the multiplication of HRCECs by MTT, the immunocytochemical method was employed to detect the each group HRCECs of VEGF expression. RESULTS:MTT assay results showed that: different concentrations of coix seed oil acted at HRCECs for 48h, inhibition of cell proliferation was significant difference compared with high glucose control group (P0. 05). lmmunocytochemical assay showed that:50ü L/mL, 100ü L/mL, 200ü L/mL Coix seed oil acted at HRCECs 48h, the expression of VEGF decreased significantly compared with the high glucose control group ( P CONCLUSlON:Coix seed oil can inhibit the HRCECs proliferation and suppress the VEGF expression in high glucose environment.
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Objective: To prepare Lingyi Formula multicomponent microemulsion and evaluate its anti-lung cancer activity. Methods: Lingyi Formula multicomponent microemulsion was prepared by aqueous titration method using polysaccharides solution of Ganoderma lucidum and Coix lachryma-jobi var. ma-yuen as aqueous phase and coix seed oil as oil phase, loading ganoderma triterpenes. The average particle size, Zeta potential, and stability were detected. The results of antitumor efficacy including tumor inhibitory rate, body weight change, immune organ index, and concentration of TNF-α and IL-6 were investigated. Besides, pathological section of tumor tissue and TUNEL labeling were conducted subsequently. Results: The prepared microemulsion displayed spherical surface with mean droplet size of (69.92 ± 8.43) nm, polydispersity (PDI) of 0.060 ± 0.008, and Zeta potential of (-11.30 ± 1.34) mV. Tumor inhibitory rate of microemulsion (57.25%) was significantly higher than that of suspension (45.89%), immune tissue index as well as the concentration of TNF-α and IL-6 were increased significantly. TUNEL labeling and pathological section of tumor tissue showed that the antitumor activity of microemulsion was significantly effective compared with that of suspensions. Conclusion: Lingyi Formula multicomponent microemulsion has a good anti-lung cancer activity.