Bioactivity-guided isolation of compounds from Sophora flavescens with antibacterial activity against Acinetobacter baumannii.

Bioactivity-guided fraction of an extract of Sophora flavescens to identify antibacterial compounds against Acinetobacter baumannii, led to the isolation of two new compounds, (2″R)-5-methoxy-7-hydroxy-8-lavandulylchromone (13) and (2S,ßS)-(-)-sophobiflavonoid CE (19), and 18 known flavonoids, (6aR,11aR)-(-)-maackiain (1), (2S)-(-)-8-prenylnaringenin (2), (2S)-(-)-exiguaflavanone K (3), (2S)-(-)-sophoraflavanone G (4), (2S)-(-)-leachianone A (5), (2S)-(-)-kushenol E (6), (2S)-(-)-leachianone G (7), (±)-kushenol F (8), (2S)-(-)-kurarinone (9), (2S)-(-)-kurarinol (10), (2 R,3R)- (+)-3,7,4'-trihydroxy-5-methoxy-8-prenylflavanone (11), (2S)-(-)-isoxanthohumol (12), (2S)-(-)-2'-methoxykurarinone (14), (2 R,3R)-(+)-kushenol I (15), calycosin (16), kuraridin (17), (2S)-(-)-kushenol A (18), and trifolirhizin (20). Their structures were elucidated based on NMR, MS, and CD spectroscopic analysis. Among them, 1, 2, 5, and 15 exerted modest antibacterial activity against A. baumannii, with MIC95 of 128-256 µg/mL for 2 and 256-512 µg/mL for 1, 5 and 15.

Cytotoxicity and Apoptosis Induced by Chenopodium ambrosioides L. Essential Oil in Human Normal Liver Cell Line L02 via the Endogenous Mitochondrial Pathway Rather Than the Endoplasmic Reticulum Stress.

Chenopodium ambrosioides L. (C. ambrosioides) has been used as dietary condiments and as traditional medicine in South America. The oil of Chenopodium ambrosioides L. (C. ambrosioides) can be used as a natural antioxidant in food processing. It also has analgesic, sedating, and deworming effects, and can be used along with the whole plant for its medical effects: decongestion, as an insecticide, and to offer menstruation pain relief. This study was conducted to investigate the cytotoxicity and apoptosis effects of an essential oil from C. ambrosioides in vitro. The cytotoxicity evaluation of the essential oil from C. ambrosioides on human normal liver cell line L02 was assessed by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide (MTT) assay. AO/EB dual fluorescent staining assay and Annexin V-FITC were used for apoptosis analysis. The changes in mitochondrial membrane potential (MMP) were analyzed with 5,5,6,6'-tetrachloro-1,1,3,3,-tetraethyl-imidacarbocyanine iodide (JC-1) dye under a fluorescence microscope. The level of apoptosis related protein expression was quantified by Western blot. The L02 cells were treated with the essential oil from C. ambrosioides at 24, 48, and 72 h, and the IC50 values were 65.45, 58.03, and 35.47 µg/mL, respectively. The AO/EB staining showed that viable apoptotic cells, non-viable apoptotic cells, and non-viable non-apoptotic cells appeared among the L02 cells under the fluorescence microscope. Cell cycle arrest at the S phase and cell apoptosis increased through flow cytometry in the L02 cells treated with the essential oil. MMP decreased in a concentration-dependent manner, as seen through JC-1 staining under the fluorescence microscope. In the L02 cells as shown by Western blot and qPCR, the amount of the apoptosis-related proteins and the mRNA expression levels of cytochrome C, Bax, Caspase-9, and Caspase-3 increased, Bcl-2 decreased, and Caspase-12, which is expressed in the endoplasmic reticulum, showed no obvious changes in protein amount or mRNA expression level. The essential oil form C. ambrosioides had a cytotoxic effect on L02 cells. It could inhibit L02 cell proliferation, arrest the cell cycle at the S phase, and induce L02 cell apoptosis through the endogenous mitochondrial pathway.

[Protective effects of tianji capsule on vascular endothelial cells from oxidative injury induced by hydrogen peroxide in vitro].

OBJECTIVE: To study the protective effects of Tianji capsule (TJ) on vascular endothelial cells from oxidative injury induced by hydrogen peroxide and its possible mechanism of anti-oxidation. METHODS: The effect of TJ on the proliferation of normal human umbilical vascular endothelial cells (HUVECs) as well as its cytotoxicity was evaluated with methylthiazolyl tetrazolium (MTT) assay. After the establishment of oxidative injury model of HUVECs, control, oxidative injury model, TJ and CoQ10 treatment groups were set up. HUVECs were incubated with 37.5, 75, 150 and 300 microg/mL TJ or 100 microg/mL CoQ10 for 24 h, and 0.1 mmol/L H2O2 (final concentration) was added to HUVECs in each groups for 30 min. Then collected the cells for proliferation detection with MTT assay, and the levels of MDA and NO, the activities of SOD, GSH-Px and NOS, as well as the releasing rate of LDH in HUVECs were also determined. RESULTS: No cytotoxicity was observed in HUVECs with less than 400 microg/ mL TJ incubated for 48 h, but increased proliferation rates were noticed. Pretreated with TJ (37.5, 75, 150 and 300 microg/mL), increased proliferation rate, the activities of SOD, GSH-Px, NOS were observed, but the decreased level of MDA and releasing rate of LDH were also found. CONCLUSION: TJ could protect HUVECs against oxidative injury induced by H2O2.

[Study on protective effect of Tianji soft capsule on blood lipids, internal antioxidant system and vascular endothelial system in hyperlipidemia rats].

OBJECTIVE: To study the protective effects of Tianji soft capsule (TJSC) on blood lipids, internal antioxidant system and vascular endothelial system in hyperlipidemia rats. METHODS: Seventy two healthy male rats were divided into six groups. The rats in control group were administered with ordinary diet. The rats in model group were fed with high cholesterol/lipid diet to induce hyperlipidemia. The rats in TJSC and CoQ10 groups were fed with high cholesterol/lipid diet, and treated with TJSC at different doses of 83 (low-dose group, L), 250 (middle-dose group, M), 750 (high-dose group, H) mg/kg, and CoQ10 at the dose of 83 mg/kg, respectively. All animals were put to death after four weeks, effects on lipid level; antioxidant system and endothelial system were evaluated through detection of total cholesterol (TC), triglyceride (TG), very low density lipoprotein (VLDL), atherogenic index (AI), malondidehyde (MDA) and plasma endothelin (ET), HDL/TC ratio, activities of superoxide dismutase (SOD) and nitric oxide (NO). RESULTS: Compared with model group, serum TC, TG, VLDL, AI, MDA and ET reduced and the HDL/TC ratio increased, meanwhile activities of SOD and NO were enhanced. CONCLUSION: TJSC can regulate the lipid metabolism, enhance antioxidant system and protect the vascular endothelia system in hyperlipiemic rats.