Deep eutectic solvent as a green solvent for enhanced extraction of narirutin, naringin, hesperidin and neohesperidin from Aurantii Fructus.

INTRODUCTION: In the present study, a green and efficient extraction method using deep eutectic solvents as extraction solvent was developed for extracting the four major active compounds narirutin, naringin, hesperidin and neohesperidin from Aurantii Fructus. METHODOLOGY: A series of tunable deep eutectic solvents were prepared and investigated by mixing choline chloride or betaine to different hydrogen-bond donors, and betaine/ethanediol was found to be the most suitable extraction solvent. To achieve the best extraction yield, the primary factors affecting the extraction efficiency, such as hydrogen-bond acceptor/hydrogen-bond donor ratio, water content in deep eutectic solvents, extraction temperature, solid/liquid ratio and extraction time, were investigated. RESULTS: The optimal extraction conditions were 40% of water in betaine/ethanediol (1:4) at 60°C for heated extraction of 30 min and solid/liquid ratio 1:100 g/mL. Under the optimum extraction condition, the extraction yields of narirutin, naringin, hesperidin, and neohesperidin were 8.39 ± 0.61, 83.98 ± 1.92, 3.03 ± 0.35 and 35.94 ± 0.63 mg/g, respectively, which were much higher than those of methanol as extraction solvent (5.5 ± 0.48, 64.23 ± 1.51, 2.16 ± 0.15 and 30.14 ± 0.62 mg/g). CONCLUSION: The present results showed that deep eutectic solvents could be promising green and efficient solvents for extraction of the bioactive ingredients from traditional Chinese medicine.

Isolation and identification of antiproliferative compounds from the roots of Tetrastigma hemsleyanum against MDA-MB-435S cell lines.

This present study aimed to elucidate antiproliferative activity of four extracts (CHCl(3), EtOAc, n-BuOH and H(2)O) and chemical constituents isolated from the most potent extract of Tetrastigma hemsleyanum Diels et. Gilg (TDG) against MDA-MB-435S cell lines using the MTT assay at various concentrations in vitro. Ten compounds were isolated and identified as (1) ß-sitosterol, (2) palmitic acid, (3) protocatechuic acid, (4) salicylic acid, (5) p-hydroxybenzoic acid, (6) resveratrol, (7) trans-4-hydroxycinnamic acid, (8) kaempferol, (9) quercetin, and (10) isoquercitrin. Compounds 3, 5-7, 10 were the first report of isolation from this plant. Moreover, antiproliferative activity displayed that the CHCl(3), H(2)O extracts and compounds 6, 8 exhibited obvious inhibitory effects on MDA-MB-435S cell lines with IC(50) values 100.28± 2.64, 127.48±3.45, 92.39±1.68 and 120.30±1.97µ/mL, respectively. Thus the obtained results indicate antiproliferative activity of TDG against MDA-MB-435S cell lines is ascribable to the most potent CHCl(3) extract along with active compounds 6 and 8, which could be considered as a potential chemotherapeutic agent in breast cancer.

Chemical constituents from Sedum aizoon and their hemostatic activity.

CONTEXT: Sedum aizoon L. (Crassulaceae) (SA) is widely used to treat various hemorrhages in folk medicine. However, its hemostatic constituents are not yet clear. OBJECTIVE: The chemical constituents of EtOAc fraction from SA and their hemostatic activity were investigated to provide a basis for the application in folk use. MATERIALS AND METHODS: The chemical constituents were isolated from the aerial parts of SA by column chromatography and identified by IR, MS, and NMR, then tested for hemostatic activity using the capillary method and coagulation assays including blood clotting time in vivo, and prothrombin time (PT), activated partial thromboplastin time (APTT), and thrombin time (TT) in vitro at concentrations of 300.0, 100.0, and 30.0 µg/mL. RESULTS: Eleven compounds were identified as p-hydroxybenzoic acid (1), gallic acid (2), protocatechuic acid (3), vallinic acid (4), thymine (5), caffeic acid (6), 5,7-dihydroxy chromone (7), pyrogallol (8), quercetin (9), kaempferol (10), and luteolin (11). This is the first report of compounds 3-8 being isolated from this plant. Compounds 2 (300.0 and 100.0 µg/mL), 4 (100.0 µg/mL), and 11 (100.0 and 30.0 µg/mL) significantly reduced the clotting time (p < 0.01) with inhibition rates of 34.7, 24.5, 30.3, 25.9, and 36.6%, respectively. For further mechanism study, they also reduced PT (3.5, 2.5, 3.5, 3.5, and 3.8%, respectively), APTT (4.5, 3.3, 11.4, 8.5, and 11.1%, respectively), and TT (20.3, 3.8, 7.6, 6.1, and 10.3%, respectively). DISCUSSION AND CONCLUSION: SA produced hemostatic activity possibly related to the presence of gallic acid, vallinic acid, and luteolin, which may be potent candidates of hemostatic drug.

[Chemical constituents from ethyl acetate extract of Sedum aizoon].

OBJECTIVE: To study the chemical constituents from ethyl acetate extract of Sedum aizoon. METHODS: The chemical constituents were isolated by column chromatography and identified by MS and NMR. RESULTS: 11 compounds were isolated and identified as: protocatechuic acid (1), caffeic acid (2), 5,7-dihydroxy chromone (3), methyl gallate (4), ethyl gallate (5), myricetin (6), luteolin (7), cynaroside (8), 3',4',5,7-tetrahydroxy flavanone (9), iriflophene (10) and iriflophene-2-O-ß-D-glucoside (11). CONCLUSION: Compounds 1-3 and 8-11 are the first report of isolation from this plant.

[Study on mechanism of yangxincao capsule in regulating lipid metabolism].

OBJECTIVE: To investigate the effect and mechanism of Yangxincao Capsule (YXCC) in regulating lipids. METHODS: Sixty rats were randomly divided into 6 groups, the normal control group (A), the hyperlipidemia model group (B), the high, middle and low dose YXCC treated groups (C, D and E), and the Shanzhajing (SZJ) treated group (F) for positive medicine control. Except for the rats in the normal control group, the other 50 were daily fed with fatty emulsion for 10 days to establish hyperlipidemic model. From the I th day on, in the same time of continually feeding with fatty emulsion they were administered with water, high (1.08 g/kg), middle (0.54 g/kg), low dose (0.27 g/kg) of YXCC and SZJ (5.4 mg/kg) respectively for 10 days, while to rats in Group A equal volume of water was given. At the 21th day, after rats were fasted for 16 h, their blood was extracted from post-orbital vein to detect the level of serum lipids, lipoprotein, apolipoprotein (apo) and lipid metabolic enzyme. RESULTS: Compared with Group A, the levels of serum total cholesterol (TC), triglyceride (TG) and low density lipoprotein-cholesterol (LDL-C) increased remarkably, and the level of high density lipoprotein-cholesterol (HDL-C) dropped obviously in Group B. While in the four treated groups the levels of TC, TG and LDL-C were significantly reduced, HDL-C and its sub-components 2 and 3 (HDL2-C and HDL3-C), as well as the ratio of HDL-C/TC were raised. Besides, the content of apo-Al was increased and apo-B was decreased significantly in Group C and D, activity of lecithin cholesterol acyltransferase (LCAT) and lipoprotein lipase (LPL) increased in the three YXCC treated groups, all showed statistical significance (P < 0.05 or P < 0.01) as compared with those in Group B. CONCLUSION: YXCC could remarkably modulate the lipid metabolic disorder in hyperlipidemic rats, and has a certain bi-directional regulating function on lipoprotein, inferring that it could reduce the risk of occurring coronary artery diseases. The mechanism of regulating lipid metabolism might be related with the increasing activity of LCAT, LPL and eliminating of cholesterol by the elevated level of HDL2-C.