Inhibitory Effects of Various Ratios of Polysaccharides/Alkaloids from Rhizome of Coptis chinensis Franch on α-Glucosidase

Purpose: To investigate the inhibitory effects of various ratios of polysaccharides/ alkaloids from the rhizome of Coptis chinensis Franch (RCC) on α-glucosidase.Methods: The polysaccharides (PSD) and alkaloids (ALK) from RCC were prepared using the water extraction and alcohol precipitation method and Reinecke’s salt precipitation method, respectively. Subsequently, the α glucosidase inhibitory effects of PSD, ALK, and PSD/ALK at various ratios were evaluated spectrophotometrically in vitro.Results: With a half maximal inhibitory concentration (IC50) value of 171.67 μg/mL, ALK showed higher α-glucosidase inhibitory activity than PSD (IC50 = 296.89 μg/mL). In addition, the polysaccharides/alkaloids (PSD/ALK) at the ratio of 3:1 exhibited stronger α-glucosidase inhibitory activity (IC50 = 160.9 μg/mL) than PSD, ALK and PSD/ALK at ratios of 1:3 (IC50 = 394.78 μg/mL), 1:2 (IC50 = 185.18 μg/mL), 1:1 (IC50 = 350.51 μg/mL), and 2:1 (IC50 = 229.16 μg/mL).Conclusion: The results obtained suggest that PSD/ALK (3:1) possesses the strongest α-glucosidase inhibitory effect and may be considered as a candidate agent in future anti-diabetes drug development.Keywords: Coptis chinensis, Polysaccharides, Alkaloids, α-Glucosidase, Antidiabeti

Quality evaluation of cortex berberidis from different geographical origins by simultaneous high performance liquid chromatography combined with statistical methods

Purpose: To develop an effective method for evaluating the quality of Cortex berberidis from different geographical origins.Methods: A simple, precise and accurate high performance liquid chromatography (HPLC) method was first developed for simultaneous quantification of four active alkaloids (magnoflorine, jatrorrhizine, palmatine, and berberine) in Cortex berberidis obtained from Qinghai, Tibet and Sichuan Provinces of China. Method validation was performed in terms of precision, repeatability, stability, accuracy, and linearity. Besides, partial least squares discriminant analysis (PLS-DA) and one-way analysis of variance (ANOVA) were applied to study the quality variations of Cortex berberidis from various geographical origins.Results: The proposed HPLC method showed good linearity, precision, repeatability, and accuracy. The four alkaloids were detected in all samples of Cortex berberidis. Among them, magnoflorine (36.46 - 87.30 mg/g) consistently showed the highest amounts in all the samples, followed by berberine (16.00 - 37.50 mg/g). The content varied in the range of 0.66 - 4.57 mg/g for palmatine and 1.53 - 16.26 mg/g for jatrorrhizine, respectively. The total content of the four alkaloids ranged from 67.62 to 114.79 mg/g. Moreover, the results obtained by the PLS-DA and ANOVA showed that magnoflorine level and the total content of these four alkaloids in Qinghai and Tibet samples were significantly higher (p < 0.01) than those in Sichuan samples.Conclusion: Quantification of multi-ingredients by HPLC combined with statistical methods provide an effective approach for achieving origin discrimination and quality evaluation of Cortex berberidis. The quality of Cortex berberidis closely correlates to the geographical origin of the samples, with Cortex berberidis samples from Qinghai and Tibet exhibiting superior qualities to those from Sichuan.Keywords: Tibetan medicine, Cortex berberidis, Origin discrimination, Quality evaluation, Magnoflorine, Palmatine, Berberine, Jatrorrhizin

Biofilm development in time on a silicone voice prosthesis:A case study

Voice prostheses from silicone elastomers become rapidly colonised by a mixed biofilm of bacteria and yeasts. In this study, microorganisms were isolated from biofilms on explanted prostheses after having been in place for various time intervals ranging from 1 to 67 d. The isolates were examined for their identity, adhesion to hexadecane and electrophoretic mobility. Bacteria from early (shorter than 8 d) and late (longer than 8 d) explants could not be classified according to their taxonomy, hydrophobicity or electrophoretic mobility. However, the yeasts clearly revealed a dominance of only hydrophilic Candida albicans isolates from early explants and only hydrophobic C. tropicalis isolates from late explants. These findings may be of significance for the development of strategies to control mixed biofilms on biomaterials.</p

Network pharmacology and UPLC-Q-TOF/MS studies on the anti-arthritic mechanism of Pterocephalus hookeri

Purpose: To investigate the mechanism underlying the anti-arthritic properties of Pterocephalus hookeri used for treatment of rheumatoid arthritis (RA).Methods: Aqueous methanol extract of P. hookeri was analyzed using UPLC-Q-TOF/MS, a Waters Acquity UPLCR BEH C18 column (2.1 × 100 mm, 1.7 μm) and gradient elution with acetonitrile-formic acid-water. Targets and related pathways were predicted by PharmMapper database and Molecule Annotation System, respectively. The network was built with Cytoscape software.Results: Forty compounds were identified, comprising 17 iridoid glycosides, 7 phenolic acids, 13 triterpenes, and 3 other compounds. A total of 38 targets and 44 pathways associated with RA were obtained. These involved mainly MAPK signaling pathway, adherens junction, and colorectal cancer.Conclusion: These results from network pharmacology suggest that P. hookeri exerts therapeutic effect on RA via multiple components, multiple targets and multiple pathways.Keywords: Pterocephalus hookeri, Rheumatoid arthritis, UPLC-Q-TOF/MS, Chemical composition, Network pharmacolog

Lead Exposure Is Associated with Decreased Serum Paraoxonase 1 (PON1) Activity and Genotypes

Lead exposure causes cardiac and vascular damage in experimental animals. However, there is considerable debate regarding the causal relationship between lead exposure and cardiovascular dysfunction in humans. Paraoxonase 1 (PON1), a high-density lipoprotein-associated antioxidant enzyme, is capable of hydrolyzing oxidized lipids and thus protects against atherosclerosis. Previous studies have shown that lead and several other metal ions are able to inhibit PON1 activity in vitro. To investigate whether lead exposure has influence on serum PON1 activity, we conducted a cross-sectional study of workers from a lead battery manufactory and lead recycling plant. Blood samples were analyzed for whole-blood lead levels, serum PON1 activity, and three common PON1 polymorphisms (Q192R, L55M, −108C/T). The mean blood lead level (± SD) of this cohort was 27.1 ± 15 μg/dL. Multiple linear regression analysis showed that blood lead levels were significantly associated with decreased serum PON1 activity (p < 0.001) in lead workers. This negative correlation was more evident for workers who carry the R192 allele, which has been suggested to be a risk factor for coronary heart disease. Taken together, our results suggest that the decrease in serum PON1 activity due to lead exposure may render individuals more susceptible to atherosclerosis, particularly subjects who are homozygous for the R192 allele

A study on the mutagenic effect of dichloromethane extract of pickled vegetables from high risk area for nasopharyngeal carcinoma (NPC)-in Sihui County

The mutagenic effect of dichloromethane extract of pickles collected from Sinhui County was examined. Sample I markedly increased the frequency of sister chromatid exchange (SCE) and the rate of micronucleus (MN) in mice. Sample II also induced an increase in SCE frequency significantly, but the increase in MN rate was slight. Chemical analyses showed that two samples of pickles contained 37.83ppb and 33.38ppb of volatile nitrosamines, respectively, which alone could not explain the observed mutagenic effect. These results sug ested that the pickled vegetables taken from NPC high-risk area, Sihui County, may contain some mutagen(s) besides volatile nitrosamines. 本文報告四會縣醃菜二氯甲烷提取液的誘變性試驗。醃菜樣本提取液Ⅰ號引起姐妹染色單體交換(SCE)率及微核(MN)率顯著升高,醃菜樣本提取液Ⅱ號亦引起SCE率明顯升高,但MN率僅略有升高。化學分析表明,該兩份醃菜的揮發性亞硝胺含量分別為37.83、33.38 ppb。醃菜提取液的誘變性似不能單用亞硝胺來解釋。實驗結果提示,鼻咽癌高發區四會縣醃菜中可能含有除揮發性亞硝胺以外的其他誘變性物質

Naringenin Produces Neuroprotection Against LPS-Induced Dopamine Neurotoxicity via the Inhibition of Microglial NLRP3 Inflammasome Activation

Background: Parkinson's disease (PD) is the second most prevalent central nervous system (CNS) degenerative disease and characterized by slow and progressive loss of dopamine (DA) neurons in the midbrain substantia nigra. Microglia-mediated neuroinflammation has been considered as the major central event in the process of DA neuronal loss. Thus, inhibition of neuroinflammation could possess a more viable strategy for PD treatment. Naringenin (NAR), a natural flavanoid contained in citrus fruit and grapefruits, possesses amounts of pharmacological activities. Recent studies indicated that NAR produced neuroprotection against several neurological disorders. However, the mechanisms underlying NAR-generated neuroprotection are not fully illuminated.Methods: In the present study, rat nigral stereotaxic injection of lipopolysaccharide (LPS)-induced DA neuronal loss was performed to investigate NAR-mediated neuroprotection. In addition, BV-2 and MN9D cell lines were applied to explore the underlying mechanisms.Results: NAR protected DA neurons against LPS-induced neurotoxicity. Also, NAR suppressed microglial nod-like receptor protein 3 (NLRP3) inflammasome signaling activation and the subsequent pro-inflammatory factors release. In addition, NAR-mediated DA neuroprotection was dependent on the inhibition of microglial NLRP3 inflammasome activation, as evidenced by the observations that NAR-reduced pro-inflammatory factors production and further NAR-exerted DA neuroprotection against LPS-induced neuronal damage was not discerned after microglial NLRP3 siRNA treatment.Conclusions: This study demonstrated that NAR targeted microglial NLRP3 inflammasome to protect DA neurons against LPS-induced neurotoxicity. These findings suggest NAR might hold a promising therapeutic potential for PD

Physalis pubescens L. branch and leaf extracts inhibit lymphoma proliferation by inducing apoptosis and cell cycle arrest

Physalis pubescens L. is an annual or perennial plant in the family Solanaceae It is used in traditional medicine for treating sore throats, coughs, urinary discomfort, and astringent pain, and externally for pemphigus and eczema in northern China. The proliferation inhibitory activity and mechanisms of the ethyl acetate extract (PHY-EA) from the leaves of Physalis pubescens were investigated. High performance liquid chromatography was used to identify the chemical composition of PHY-EA; sulforhodamine B was used to detect the proliferation inhibitory effect of PHY-EA on MCF-7, CA-46, Hela, HepG2, B16, and other tumor cells; flow cytometry was used to detect the effect of PHY-EA on the lymphoma cell cycle and apoptosis; Western blot was used to detect the expression of the cycle- and apoptosis-related proteins. The expression of Ki-67 and cleaved caspase 3 was detected by immunohistochemistry. The results showed that PHY-EA contained physalin B, physalin O, and physalin L. PHY-EA blocked the cell cycle of G2/M→G0/G1 in lymphoma cells and induced apoptosis in tumor cells. Mouse transplantation tumor experiments showed that PHY-EA had a significant inhibitory effect on mouse transplantation tumors, and the tumor volume and weight were significantly reduced. In conclusion, PHY-EA has a good antiproliferative effect on Burkkit lymphoma, indicating its potential medicinal value