Xiao-Hua Liu

Isolation, structure, and bioactivities of abiesadines A–Y, 25 new diterpenes from Abies georgei Orr

Twenty-five new (abiesadines A-Y, 1-25) and 29 known (26-54) diterpenes were isolated from the aerial parts of Abies georgei. Abiesadine A (1) is a novel 8,14-seco-abietane, while abiesadine B (2) is a novel 9,10-seco-abietane. The structures of the new compounds were established on the basis of spectroscopic data analysis. Manool (52) showed the strongest effect against LPS-induced NO production in RAW264.7 macrophages with the IC(50) value of 11.0microg/mL. In another anti-inflammatory assay against TNFalpha-triggered NF-kappaB activity, (12R,13R)-8,12-epoxy-14-labden-13-ol (54) exhibited the strongest effect (IC(50)=8.7microg/mL). For antitumor assays, pomiferin A (26) and 8,11,13-abietatriene-7alpha,18-diol (29) both showed the most significant activity against LOVO cells (IC(50)=9.2microg/mL). While 7-oxocallitrisic acid (46) exhibited significant cytotoxicity against QGY-7703 tumor cells (IC(50)=10.2microg/mL).

Huang-Lian-Jie-Du-Tang exerts anti-inflammatory effects in rats through inhibition of nitric oxide production and eicosanoid biosynthesis via the lipoxygenase pathway

Objectives Huang‐Lian‐Jie‐Du‐Tang (HLJDT) is a traditional Chinese medicine with a long history of anti‐inflammatory use, but its pharmacological effects have not been thoroughly investigated. This study aimed to evaluate the anti‐inflammatory activity of HLJDT in vivo and in vitro.

Terpenoid Constituents of Abies chensiensis with Potential Anti-inflammatory Activity

Six new triterpenes (neoabieslactones A-F, 1-6) and 17 known compounds were isolated from the aerial parts of Abies chensiensis. The structures of the new triterpenes were proposed by 1D and 2D NMR spectroscopy. Compound 1 was confirmed structurally by X-ray crystallography. In a bioassay against LPS-induced NO production in RAW264.7 macrophages, three compounds, neoabieslactone E (5), (12R,13R)-8,12-epoxy-14-labden-13-ol (7), and manool (8), exhibited IC(50) values of 9.1, 1.9, and 9.6 microg/mL, respectively.

Terpenoids from Daphne aurantiaca and their potential anti-inflammatory activity.

Phytochemical examination of the methanolic extract from the stem bark of Daphne aurantiaca led to the isolation of six new sesquiterpenoids, dauca-3,11-dien-2alpha,15-diol (1), 3-oxoguai-4-ene-11,12-diol (2), 4alpha,5alpha,8alpha,11alphaH-3-oxoguai-1(10)-en-12,8-olide-7alpha-diol (3), 4alpha,5alpha,8alpha,11betaH-3-oxoguai-1(10)-en-12,8-olide-7beta-diol (4), 4alpha,5betaH-guai-9,7(11)-dien-12,8-olide-1alpha,8alpha-diol (5), 4alpha,5alphaH-guai-9,7(11)-dien-12,8-olide-1alpha,8alpha-diol (6), and a new diterpenoid, 12-O-benzoylphorbol 13-nonanoate (7), together with 10 known terpenoids. All compounds were tested for inhibitory activity against LPS-induced NO production in RAW 264.7 macrophages. Compounds 7, 8, 9, 10, and 11 showed potent inhibitory activities against NO production with IC(50) values of 0.01, 0.01, 0.06, 0.07, and 0.03 microM, respectively.

Polyacetylenes from Bupleurum longiradiatum

Eight new polyacetylenes (1-8) and six known polyacetylenes were isolated from the entire parts of Bupleurum longiradiatum, a poisonous plant. The structures of the new compounds were determined by spectroscopic data interpretation. The absolute configuration of the known compound bupleurotoxin (9) was established by the modified Moshers method. All isolates were also tested for their cytotoxicity against a human leukemia cell line (HL-60).

Anti-inflammatory and anti-nociceptive activities of compounds from Tinospora sagittata (Oliv.) Gagnep.

Radix Tinosporae is a herb widely used in traditional Chinese medicine for the treatment of various inflammatory diseases. In the present study, its anti-inflammatory and antinociceptive activities were investigated. The ethanol extract of Radix Tinosporae exhibited significant inhibitory effects on xylene-induced ear edema and acetic acid-induced writhing in mice. Using bioassay-guided fractionation, the n-butanol fraction was determined as the active fraction. Further purification of the most active n-butanol fraction led to the isolation of three compounds, palmatine, columbamine and columbinyl glucoside. All three compounds showed inhibitory activities on xylene-induced ear edema, but only palmatine and columbamine exhibited significant inhibitory effects on acetic acid-induced writhing. In addition, palmatine and columbamine markedly inhibited in vitro production of nitric oxide and nuclear factor-κB activation in RAW264.7 macrophage cells in response to lipopolysaccharide or tumor necrosis factor α stimulation. These results provide justification for the utilization of Radix Tinosporae in Chinese folk medicine for the treatment of inflammatory diseases.

Blumeaenes A-J, Sesquiterpenoid Esters from Blumea balsamifera with NO Inhibitory Activity

Chemical examination of the ethanol extract of the aerial parts of Blumea balsamifera led to the isolation of ten new sesquiterpenoid esters, blumeaenes A-J (1- 10), with 13 known flavonoids. Their structures were determined mainly by use of 1D and 2D NMR spectroscopic techniques. All sesquiterpenoid esters were tested for their inhibitory activity against LPS-induced NO production in RAW264.7 macrophages. Compounds 1, 4 and 5 showed slight inhibitory effect on the production of NO with IC(50) values of 40.06, 46.35 and 57.80 microg/mL, respectively.

Antitumor and antiplatelet activity of alkaloids from veratrum dahuricum

Ten steroidal alkaloids – cyclopamine, veratramine, jervine, 3, 15‐diangyloylgermine, 3‐angyloylzygadenine, 3‐veratroyl zygadenine, 15‐veratroylgermine, germine, veratrosine and pseudojervine – from Veratrum dahuricum, together with the ethanol extract and total alkaloids, were evaluated for their antitumor and antiplatelet activities. Cyclopamine, veratramine and germine significantly inhibited the hedgehog pathway in NIH/3T3 cells. Cyclopamine exerted a potent inhibitory effect against the growth of PANC‐1 tumors in mice, with inhibition rates of 40.64%, 44.37%, 46.77% at doses of 5.0, 15.0 and 50.0 mg kg‐1, respectively. Veratroylgermine was found to produce the strongest inhibition against the platelet aggregation induced by arachidonic acid, with inhibition rate of 92.0% at 100 μM. Copyright

Chemometrics-based approach to modeling quantitative composition-activity relationships for Radix Tinosporae

Quantitative composition-activity relationship (QCAR) study makes it possible to discover active components in traditional Chinese medicine (TCM) and to predict the integral bioactivity by its chemical composition. In the study, 28 samples of Radix Tinosporae were quantitatively analyzed by high performance liquid chromatography, and their analgesic activities were investigated via abdominal writhing tests on mice. Three genetic algorithms (GA) based approaches including partial least square regression, radial basis function neural network, and support vector regression (SVR) were established to construct QCAR models of R. Tinosporae. The result shows that GA-SVR has the best model performance in the bioactivity prediction of R. Tinosporae; seven major components thereof were discovered to have analgesic activities, and the analgesic activities of these components were partly confirmed by subsequent abdominal writhing test. The proposed approach allows discovering active components in TCM and predicting bioactivity by its chemical composition, and is expected to be utilized as a supplementary tool for the quality control and drug discovery of TCM.

Determination of two C21 steroidal glycosides of Baishouwu and their metabolites in mice plasma and tumor homogenate by liquid chromatography–tandem mass spectrometry

For the evaluating of the absorption, tumor affinity and metabolism of wilfoside C3N and wilfoside C1N (two main C21 steroidal glycosides from Baishouwu), an LC-MS/MS method was developed. Plasma or tumor homogenate samples were extracted by liquid-liquid extraction with ethyl acetate after internal standard (ginsenoside Rh2) spiked. The separation was performed by a Luna C18 column (3.0 microm, 2.0 mm x 50 mm) with gradient elution. The method was fully validated and successfully applied to determine the concentrations of the parent drugs and metabolites after intragastric administration of wilfoside C3N and wilfoside C1N to mice respectively.