ABSTRACT Introduction It has a long history to employ Macleaya cordata (Willd.) R. Br. (Papaveraceae) for the treatment of a variety of diseases in China. Chelerythrine, one of the major of M. cordata with detoxifying and anti-inflammatory effect, is reported to combat bacteria and fungus. This work aims to explore the effect of chelerythrine against fluconazole-resistant C. albicans and also illustrate its potential mechanism. Methods The microdilution method, following CLSI-M27-A3 was used to evaluate the effect of chelerythrine against fluconazole-resistant C. albicans. Meanwhile, biofilm viability was assessed by XTT assay and cell morphology was observed by inverted microscope. RT-qPCR and confocal laser scanning microscope were employed to detect the mRNA expression and DCFH-DA staining, respectively. Fluorescence intensity was quantified by flow cytometry. Results The total alkaloids extract of M. cordata significantly inhibited the viability of C. albicans, concentration of which in 64 μg/mL presented to 40% inhibitory effect . In addition, the MIC 80 for chelerythrine was 8 μM, whereas chelerythrine in 4 μM inhibited biofilm formation by 47.7%. Further studies revealed that chelerythrine reduced the hydrophobicity of cellular surface, inhibited hyphal growth, downregulated the expression of genes related to cAMP pathway, increased cellular permeability and promoted the production of reactive oxygen species (ROS). Conclusion Chelerythrine inhibited biofilm formation by decreasing CSH and inhibiting the cAMP pathway. Chelerythrine increased cellular permeability and promoted the production of reactive oxygen species, which leads to the cell death of fluconazole-resistant C. albicans .
The protopine alkaloids are widely distributed within the opium poppy family and have a wide range of pharmacological effects. MPTA is a product of the protopine total alkaloids extracted from the Macleaya cordata (Willd.) R. Br. Previously, we reported good anti-inflammatory activity of MPTA as well as oral acute and sub-chronic toxicity studies in rats. In order to perform a systematic toxicological safety assessment of MPTA, oral acute toxicity, genotoxicity (bone marrow cell chromosome aberration test, sperm abnormality test, bone marrow cell micronucleus test, and rat teratogenicity test), and chronic toxicity in mice were performed in this study. In the oral acute toxicity test, the LD50 in ICR mice was 481.99 mg/kg, with 95% confidence limits ranging from 404.27 to 574.70 mg/kg. All three mutagenicity tests tested negative in the range of 60.25–241.00 mg/kg. The results of the teratogenicity test in rats showed no reproductive or embryonic developmental toxicity at only 7.53 mg/kg, which can be considered as a no observed effect level (NOEL) for the teratogenicity test. Therefore, MPTA is safe for use at the doses tested, but attention should be paid to the potential risk to pregnant animals and the safety evaluation and toxicity mechanisms in target animals should be further investigated.
A novel type of magnetic molecularly imprinted polymers (MMIP) as the solid-phase extraction sorbent was prepared, which can extract effectively the allocryptopine from the waster of Macleaya cordata (Willd) R . Br . In this study, MMIP was synthesized by using Fe 3 O 4 @SiO 2 , 4-vinyl-pyridine, ethylene glycol dimethacrylate, and allocryptopine, and these ingredients worked as magnetic core, functional monomer, cross-linker, and template, respectively. Concluded by the calculation of Gaussian 09 software, different ratio models of 4-vinyl-pyridine and allocryptopine were simulated, and the optimal ratio was 1:5 and the energy was −2205.34 kJ/mol. Transmission electron microscopy, vibration sample magnetometry, X-ray diffraction, Fourier transform infrared spectroscopy, and thermogravimetric analysis were used to determine the morphology and structure of MMIP. Furthermore, the results of adsorption experiments indicated that MMIP had high selectivity, excellent recyclability, and good adsorption performance (9.86 mg/g, 298 K). The adsorption process was consistent with the Langmuir adsorption isotherm ( R 2 > 0.98, 298 K) and pseudo-second-order kinetics model ( R 2 > 0.99, 298 K). After six times adsorption-desorption experiments, the adsorption amount of MMIP only reduced to 8.5%. In the experiments of selective adsorption, MMIP has better adsorption properties for allocryptopine (ALL, C 21 H 23 NO 5 ) than those having the same functional group. The limit of detection (LOD) was 0.4 μg/mL. The relative standard deviation ranged from 0.09% to 0.72%. The recovery of allocryptopine in samples ranged from 93.60% to 106.19%. In addition, the synthesized complex had a certain adsorption effect on allocryptopine separating from the wastewater of Macleaya cordata (Willd) R . Br .
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