Preliminary study on blood coagulation and hemostatic effect and acute toxicity of Oxalis corniculata L. ethanol extract

In the present study, we aimed to observe the effects of ethanol extract of Oxalis corniculata L. on bleeding time (BT) and coagulation time (CT) and determine its acute toxicity in mice. Firstly, the ethanol extract of O. corniculata was administered to 40 mice, which were randomly divided into the normal control group, Yunnan Baiyao control group, low-dose group, and high-dose group. The low-dose (0.6 g/kg) and high-dose (1.2 g/kg) groups received ethanol extract of O. corniculata by gavage, and the BT and CT of the mice were measured by the slide method and tail clipping method, respectively. Secondly, the median lethal dose method was used with 50 mice to observe the physiological state, poisoning reaction, and death of the mice after intragastric administration. Finally, on the 14th day of the experiment, a necropsy was performed to observe any abnormality of the organs. In conclusion, in the coagulation and hemostasis tests, there were no statistical differences between the groups (P > 0.05), while there was a significant dose-response relationship, and the BT and CT were significantly shorter than those of the negative control group, which were comparable to the Yunnan Baiyao control group. Moreover, in the acute toxicity test, the median lethal dose of ethanol extract of O. corniculata was 6.0291 g/kg, with a 95% confidence interval of 5.3065–6.7829 mg/kg.     

The key role of macrophage depolarization in the treatment of COPD with ergosterol both in vitro and in vivo

Macrophages are the most abundant immune cells in the lung, which play an important role in COPD. The anti-inflammatory and anti-oxidation of ergosterol are well documented. However, the effect of ergosterol on macrophage polarization has not been studied. The objective of this work was to investigate the effect of ergosterol on macrophage polarization in CSE-induced RAW264.7 cells and Sprague-Dawley (SD) rats COPD model. Our results demonstrate that CSE-induced macrophages tend to the M1 polarization via increasing ROS, IL-6 and TNF-α, as well as increasing MMP-9 to destroy the lung construction in both RAW264.7 cells and SD rats. However, treatment of RAW264.7 cells and SD rats with ergosterol inhibited CSE-induced inflammatory by decreasing ROS, IL-6 and TNF-α, and increasing IL-10 and TGF-β, shuffling the dynamic polarization of macrophages from M1 to M2 both in vitro and in vivo. Ergosterol also decreased the expression of M1 marker CD40, while increased that of M2 marker CD163. Moreover, ergosterol improved the lung characters in rats by decreasing MMP-9. Furthermore, ergosterol elevated HDAC3 activation and suppressed P300/CBP and PCAF activation as well as acetyl NF-κB/p65 and IKKβ, demonstrating that HDAC3 deacetylation was involved in the effect of ergosterol on macrophage polarization. These results also provide a proof in immunoregulation of ergosterol for therapeutic effects of cultured C. sinensis on COPD patients.     

The effects of grape seed extract on glycemic control,serum lipoproteins,inflammation, and body weight: A systematic review and meta‐analysis of randomized controlled trials

The aim of this systematic review and meta‐analysis was to analyze the effects of grape seed extract (GSE) on glycemic control and serum lipoproteins, inflammation and body weight. Two independent authors systematically searched online databases including EMBASE, Scopus, PubMed, Cochrane Library, and Web of Science from inception until May 30, 2019. Cochrane Collaboration risk of bias tool was applied to assess the methodological quality of included trials. The heterogeneity among the included studies was assessed using Cochrane's Q test and I‐square (I²) statistic. Data were pooled using a random‐effects model and weighted mean difference (WMD) was considered as the overall effect size. Fifty trials were included in this meta‐analysis. Pooling effect sizes from studies demonstrated a significant decrease in fasting plasma glucose (FPG) (WMD): ?2.01; 95% confidence interval (CI): ?3.14, ?0.86), total cholesterol (TC; WMD: ?6.03; 95% CI: ?9.71, ?2.35), low‐density lipoprotein (LDL) cholesterol (WMD: ?4.97; 95% CI: ?8.37, ?1.57), triglycerides (WMD: ?6.55; 95% CI: ?9.28, ?3.83), and C‐reactive protein (CRP) concentrations (WMD: ?0.81; 95% CI: ?1.25, ?0.38) following GSE therapy. Grape seed did not influence HbA1c, HDL cholesterol levels, and anthropometric measurements. This meta‐analysis demonstrated that GSE intake significantly reduced FPG, TC, LDL cholesterol, triglycerides, and CRP levels.     

Preparation,characterization, and antibacterial activity of plaunotol and plaunoi extracts complexed with hydroxypropyl-β-cyclodextrin

Croton stellatopilosus (Plaunoi) leaves accumulate several diterpenes and possess various pharmacological activities. The present study aimed to prepare, characterize and assess the antibacterial activity of inclusion complexes prepared by mixing plaunotol (PL) or plaunoi extract (PE) with cyclodextrins (CD), including α-CD, β-CD, γ-CD, and hydroxypropyl-β-cyclodextrin (HP-β-CD). The inclusion complexes were characterized using SEM, XRD, DSC, and FT-IR and evaluated for aqueous solubility and thermal stability. The PL and PE lyophilized complexes with HP-β-CD were further evaluated for their antibacterial activity against acne-causing bacteria. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) of PL, PE, and the inclusion complexes evaluated using the agar dilution method revealed that the MIC and MBC values of the inclusion complexes were lower than those of PL or PE alone. Interestingly, the complexes had a synergistic activity with clindamycin after testing with checkerboard assay. The hydrogel containing the inclusion complex and clindamycin were assessed for antibacterial activity using the agar well diffusion method. The results indicated that the hydrogels showed significant inhibition of bacterial growth. In conclusion, the prepared solid dispersion of PL or PE with HP-β-CD could enhance antibacterial activity by increasing the drug solubility. The hydrogels containing PL or PE complex and clindamycin could be considered as a candidate for the treatment of acne vulgaris.     

Effect of Human Placental Extract Treatment on Random-Pattern Skin Flap Survival in Rats

Background: Human placental extract (HPE), prepared from the placentas of healthy, postpartum females, displays various physiological activities, including antioxidative properties. In this study, a dorsal skin flap model was used to investigate the effect of HPE on flap viability in rats. Materials and methods: Forty male Sprague-Dawley rats underwent random-pattern skin flap surgeries. The animals were randomly divided among a control group and three treatment groups (localized injection (LI), 10 mg/kg/d localized HPE injections; low-dose treatment (LT), 10 mg/kg/d systemic HPE injections; high-dose treatment (HT), 40 mg/kg/d systemic HPE injections). Surviving skin flap areas were measured 7 days after surgery and tissue samples were stained with hematoxylin and eosin; vascular endothelial growth factor expression was determined immunohistochemically. To evaluate the antioxidant and antiapoptotic effects of HPE, malondialdehyde, glutathione peroxidase, and caspase-3 levels were examined. Results: Seven days after surgery, HPE-treated animals had significantly reduced necrotic areas, rats receiving the highest HPE dose demonstrated the greatest flap survival. In the HPE groups, the histopathological scores were lower than for the control group. Immunohistochemistry showed markedly more numerous vascular endothelial growth factor-positive cells in the HT group than in the C group. Malondialdehyde levels were significantly lower and glutathione peroxidase levels were higher in the HT group than in the C group. HPE treatment significantly inhibited apoptosis by lowering caspase-3 activity. Conclusions: HPE treatment yielded positive effects on flap survival, due to its antioxidant and antiapoptotic properties. These results suggest a new therapeutic approach for enhancing flap viability and accelerating wound repair.     

阿萨伊油、醇提及水提物对虚热及虚寒小鼠温度趋向性及代谢水平的影响

通过考察阿萨伊油、醇提物和水提物等拆分组分对虚热及虚寒证小鼠的温度趋向性动物行为学表征,环核苷酸及代谢水平等内在生化指标的影响,探讨阿萨伊各拆分组分的寒热药性特点以及寒凉的物质基础。将昆明种雄性小鼠随机分为空白组、虚热模型组、虚热+阿萨伊冻干原粉组、虚热+阿萨伊油组、虚热+阿萨伊醇提物组、虚热+阿萨伊水提物组、虚寒模型组、虚寒+肉桂组、虚寒+阿萨伊冻干原粉组、虚寒+阿萨伊油组、虚寒+阿萨伊醇提物组、虚寒+阿萨伊水提物组共12个组。虚热组小鼠每天下午灌胃给予甲状腺片溶液160 mg·kg-1,虚寒组小鼠给予氢化可的松溶液25 mg·kg-1,连续14 d,各给药组灌胃相关药物,实验结束后测定动物温度趋向性、环核苷酸及代谢水平等相关指标。阿萨伊醇提物同阿萨伊原粉一致,表现出对虚热模型小鼠的调整作用;阿萨伊油及其水提物同肉桂一致,表现出对虚寒模型小鼠的调整作用。该研究基于中药性味可拆分理论,采用同类比较异类反证的方法证明了阿萨伊醇提物性偏凉,油及其水提物性偏温的特征,并明确了醇提物为阿萨伊性凉的物质基础。     

海莲叶提取物对胃癌细胞增殖的抑制作用及对小鼠急性毒性实验

目的:探究海莲叶提取物对胃癌细胞增殖的抑制作用及对小鼠急性毒性实验。方法:先通过实验证实海莲叶提取物可对患者的胃癌细胞SGC-7091、MGC80-3可起到促进作用,应对实验小鼠皮下建立移植瘤模型,随后对小鼠注射海莲叶提取物,观察对胃癌细胞增殖的抑制情况,随后对药物的毒性进行分析。结果:给药组与溶媒对照组急性毒性反应相比显著较高,差异具有统计学意义(P<0.05)。结论:海莲叶提取物可对胃癌细胞增殖的抑制作用,并均已经在实验中得到了证实,海莲叶提取物可明显降低小鼠的急性毒性反应。     

陈皮水提物指纹图谱的化学计量学分析及与糖尿病认知功能障碍的谱效关系

目的:建立陈皮水提物的HPLC指纹图谱,并研究其与糖尿病大鼠认知功能的谱效关系。方法:采用HPLC建立21批陈皮水提物的指纹图谱,流动相乙腈(A)-0.1%的磷酸(B)梯度洗脱,检测波长270 nm;采用指纹图谱软件中的相似度评价,SPSS 24.0二维聚类分析和SIMCA 14.1主成分分析对结果进行分析;采用腹腔注射链脲佐菌素(STZ,50 mg·kg^-1)复制糖尿病大鼠模型,模型复制成功后给予陈皮水提物灌胃,定期检测空腹血糖值,诱导第12周Morris水迷宫检测实验大鼠的空间学习记忆能力,灰色关联度分析和偏最小二乘回归分析研究谱效关系。结果:确定了陈皮水提物中25个共有峰,鉴定出5种物质,并且将21个不同品种、产地的陈皮分成了2类;与模型组比较,灌胃陈皮水提物的各组大鼠空腹血糖下降,认知能力得到改善;灰色关联分析及最小偏二乘回归分析谱效关系表明,19,15,4,17,6号峰与糖尿病大鼠认知功能关联性较大。结论:不同品种、产地之间的陈皮水提物存在一定的差异,通过化学计量学可以方便、快捷的对不同产地的陈皮水提取物质进行全面的质量评价,并且陈皮水提物可降低糖尿病大鼠的空腹血糖值及改善认知能力,其发挥作用是多种有效成分共同起效的结果,其中19,15,4,17,6号峰是与糖尿病大鼠认知功能密切相关的成分。     

穿山龙提取物抗急性痛风性关节炎的尿液代谢组学分析

目的:对急性痛风性关节炎大鼠给予穿山龙提取物后的尿液代谢组学进行研究,寻找相关的潜在生物标志物及相关代谢通路。方法:采用尿酸钠(MSU)诱导的急性痛风性关节炎大鼠模型,将SD大鼠40只随机分为空白组、穿山龙提取物组、模型组、穿山龙提取物干预组,每组10只。给药组灌胃给予穿山龙提取物,给药剂量0. 48 g·kg~(-1),每天1次,连续5 d,于末次给药后,收集大鼠尿液,运用UPLC-Q-TOF/MS结合模式识别方法分析,采用正、负离子扫描模式下电喷雾离子源,数据采集范围m/z 100～1 500,采用全扫描方式。结果:鉴别出了12个共同的潜在生物标志物,分别为肌氨酸,二甲基甘氨酸,脱氧胞苷,尿酸,5-HT,L-胱硫醚,4-吡哆酸,脱氧尿苷,褪黑激素,5-甲氧基色胺,富马酸和胞苷。与空白组比较,穿山龙提取物组中这12个潜在生物标志物均明显下调;与模型组比较,在穿山龙提取物干预组的潜在生物标志物中,有10个上调,2个下调,穿山龙提取物对肌氨酸,尿酸,L-胱硫醚,4-吡哆酸,脱氧尿苷,5-甲氧基色胺,胞苷,二甲基甘氨酸,褪黑激素,富马酸这10个标志物均表现出了纠正异常表达的趋势;与急性痛风性关节炎相关性最强的代谢通路为半胱氨酸和甲硫氨酸代谢、色氨酸代谢。结论:穿山龙提取物可能是通过促进半胱氨酸和甲硫氨酸代谢中胱硫醚向半胱氨酸的转化水平,上调色氨酸代谢中褪黑激素,实现对痛风性关节炎的防治作用。