Antihyperlipidemic Effect, Identification and Isolation of the Lipophilic Components from Artemisia integrifolia.

Artemisia integrifolia L (Compositae) is a medicinal and edible plant. To investigate its antihyperlipidemic effect, a crude lipophilic extract and the composing compounds were isolated and fractioned from the petroleum ether extract of aerial parts of A. integrifolia using column chromatography on silica gel. The anti-hyperlipidemia effect was studied in a rat model of acute hyperlipidemia, which was induced by triton WR-1339. A new compound, integrinol (4), together with nine known compounds, namely chamazulene (1), acetylenes (E)-2 (2), acetylenes (E)-3 (3), eugenol (5), palmitic acid (6), oleic acid (7), linoleic acid (8), linolenic acid (9) and 12,13-epoxylinolenic acid were isolated from the crude lipophilic extract of A. integrifolia. The LD50 value of the crude extract was more than 4g/kg. In Triton WR-1339-induced acute hyperlipidemia model, the crude lipophilic extract (200 mg/kg) significantly reduced total cholesterol (TC) by 70% (p ≤ 0.01) and triglycerides (TGs) by 94% (p ≤ 0.001). The fractioned compounds, such as chamazulene (1), acetylene-2 (2), and linolenic acid (9), used at 4 mg/kg dose, also significantly decreased the concentrations of TC (32%, 33% and 64%, respectively) and TGs (48%, 33% and 93%, respectively). These compounds (i.e., chamazulene, acetylenes (E)-2, and linolenic acid) were considered to be responsible for the bioactive antihyperlipidemic effect. In conclusion, the crude lipid extract of Artemisia integrifolia L could be used as a potential treatment to avert hyperlipidemia. Further studies to confirm these results in other models of hyperlipidemia (e.g., diet-induced obesity) are warranted.

Randomized, Double-Blind, Placebo-Controlled Studies to Assess Safety and Prophylactic Efficacy of Naphthoquine-Azithromycin Combination for Malaria Prophylaxis in Southeast Asia.

New prophylactic drugs against malaria infections are urgently needed. We conducted randomized, double-blind, placebo-controlled, phase 2 trials of a new antimalarial drug combination, naphthoquine-azithromycin (NQAZ), to determine its safety and protective efficacy in a low-endemicity area of Southeast Asia. In the first trial, 127 healthy volunteers were randomized to receive two single doses of either 400 mg of NQAZ (200 mg of each drug), 800 mg of NQAZ (400 mg of each drug), or placebo on day 0 and day 30. Weekly follow-ups were performed for 2 months, and physical and clinical laboratory exams were done during the second and eighth week. Both drug regimens were well tolerated, without any serious adverse events. Four adverse events (transient and slight elevations of serum transaminase concentrations) were found only in the two drug-treated groups and thus might be drug-related. In the second trial, 353 volunteer villagers were randomized into the same three groups as in the first trial, and malaria infections were followed for a month. For the intention-to-treat analysis, both regimens offered greater than 90% prophylactic efficacies against all malaria infections. When the analysis was done according to parasite species, 400 mg and 800 mg NQAZ provided 81.63 and 90.59% prophylactic efficacies, respectively, against Plasmodium falciparum infections, whereas both offered 100% prophylactic efficacy against Plasmodium vivax and Plasmodium ovale These trials showed that NQAZ had a good safety profile, and monthly single doses of 400 mg or 800 mg for adults offered excellent prophylaxis against malaria infections, especially the two relapsing species.

High-speed countercurrent chromatography isolation of flavans from Ixeris chinensis and their identification by NMR spectroscopy.

High-speed countercurrent chromatography, combined with macroporous resin chromatography were applied to the separation and purification of flavans from Ixeris chinensis. Four flavans, namely, 5-methoxy-7,4'-dihydroxyflavan-3-ol (1), 5,7-dimethoxy-4'-hydroxyflavan-3-ol (2), 5,7-dimethoxy-4'-hydroxyflavan (3), and 5,7-dimethoxy-8-methyl-4'-hydroxyflavan (4), were obtained from I. chinensis for the first time. Their chemical structural identification was carried out by spectroscopic methods, including 1D and 2D NMR spectroscopy. Amounts of 13.2 mg of compound 1, 6.4 mg of compound 2, 5.8 mg of compound 3, and 14.5 mg of compound 4 were separated from 120 mg 75% ethanol fraction. The purities of 1-4 were 99.1, 99.2, 97.3, and 98.6 %, respectively.

[Study on Chemical Constituents of Panzeria alaschanica].

OBJECTIVE: To study the chemical constituents of the ethyl acetate extract from Panzeria alaschanica. METHODS: The chemical constituents of ethyl acetate extract from Panzeria alaschanica were isolated and purified by silica gel. Their structures were i- dentified by means of spectra. RESULTS: Nine compounds were obtained and identified as 7-Methoxy coumarin (1), Isorhamnetin (2), Caf- feic acid (3), 5-Hydroxy-7,3',4'-trimethoxyflavone (4), 5-Hydroxy-7,4'-dimethoxyflavone (5),Kaempferol (6), Isorhamnetin-3-O-ß-D- glucoside (7) Kaempferol-3-O-ß-D-glucoside (8), and Isorhamnetin-7-O-ß-D-glucuronyl-(1-->6)-O-α-L-rhamnoside (9). CONCLUSION: Compounds 1-4,6,7 and 9 are isolated from this plant for the first time.

Structure elucidation and NMR assignments of two unusual xanthones from Lomatogonium carinthiacum (Wulf) Reichb.

Two new unusual xanthones, 5-O-ß-d-glucopyranosyl-1,3,8-trihydroxy-5,6,7,8-tetrahydroxanthone (1) and 1,3,5,8-tetrahydroxy-5,6,7,8-tetrahydroxanthone (2), were isolated from Lomatogonium carinthiacum (Wulf) Reichb. Their structures were elucidated on the basis of spectroscopic methods including UV, IR, ESI-MS, 1D NMR, and 2D NMR.

A new sesquiterpene coumarins from Ferula bungeana Kitagawa.

A new sesquiterpene coumarin, bungeanin A (1), together with four known sesquiterpene coumarins, were isolated from the whole plants of Ferula bungeana Kitagawa. The structure of bungeanin A was elucidated by analysis of its spectroscopic data, including UV, IR, HR-ESI-MS, and extensive 1D and 2D NMR spectroscopy.

A new abietane diterpene tuurgan a from caryopteris mongholica.

Five abietane diterpenes compounds were separated from petroleum ether extraction sites of ethanol extract of Caryopteris Mongholica, and Compound 1 was identified as a new abietane diterpenes compound by NMR and mass spectrometry, named as Tuurgan A of Caryopteris Mongholica; and Compounds 2-5 separated from Caryopteris Mongholica for the first time were identified as Ferruginol (2), Taxodione (3), Caryopterisoid Q (4), and Huperphlegmarin B (5). The anti-lung cancer activity of the Compounds 1-5 were determined, which results showed that they all had high A549 cytotoxicity.

HPLC analysis of 16 compounds from Artemisia ordosica.

Objective: To establish a high-performance liquid chromatographic method (HPLC) for the simultaneous determination of 16 compounds from Artemisia ordosica. Methods: HPLC was used to analyze 16 quality indicators of A. ordosica. The HPLC conditions were as follows: Agilent Eclipse Plus C18 column (250 mm × 4.6 mm, 5 µm) with acetonitrile (A)-water (B) as mobile phase, gradient elution: 0-10 min, 75%-65% B; 10-30 min, 65%-35% B; and finally 30-40 min, 35%-15% B. The flow rate was 1.0 mL/min, the column temperature was 40 °C, the injection volume was 10 µL, and monitored by absorbance at 285 nm for compounds 1-10, 12 and 225 nm for compounds 11, 13-16. Results: Under the selected experimental chromatographic conditions, compounds 1-16 showed good linearity (r > 0.9993) in a wide concentration range. Their average recoveries were 99.50%, 95.38%, 97.75%, 96.00%, 98.20%, 97.50%, 95.50%, 99.33%, 96.75%, 96.50%, 98.50%, 97.83%, 99.20%, 95.33%, 97.33% and 96.30%, respectively, and the RSD were 1.99%, 1.81%, 1.63%, 1.98%, 1.67%, 1.92%, 1.74%, 1.67%, 1.90%, 1.72%, 1.88%, 1.83%, 1.79%, 1.76%, 1.81% and 1.96%, respectively. Conclusion: Based on the results of the HPLC analysis, it was concluded that p-hydroxycinnamic acid (1), O-hydroxycinnamic acid (2), coniferyl alcohol (5), 5,4'-dihydroxy-7,3'-dimethoxyflavanone (8), 5,4'-dihydroxy-7-methoxyflavanone (9), 5-hydroxy-7,4'-dimethoxyflavanone (12), dehydrofalcarindiol (13), arteordoyn A (14), dehydrofalcarinol (15) and capillarin (16) are best suited for the role of quality indicators of A. ordosica grown in different ecological environments.

Structure elucidation and NMR assignments of an unusual triterpene saponin derivative from Ilex kudincha.

One unusual triterpenoid derivative, ilekudinchoside E (1), was isolated from the leaves of Ilex kudincha. The structure was established by various spectroscopic techniques, including one- and two-dimensional NMR, HRTOFMS and CD spectra.

Lignans from Syringa pinnatifolia Hemsl. Var. alashanensis.

Two new lignans, syripinnalignans A and B (1 and 2), together with two known lignans, were isolated from the stem of Syringa pinnatifolia Hemsl. Var. alashanensis. The structures of 1 and 2 were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques.

[Study on chemical constituents of Ixeris chinensis].

OBJECTIVE: To study the chemical constituents of Ixeris chinensis. METHODS: The chemical constituents of Ixeris chinensia were isolated and purified by silica gel. LH-20 column chromatography and preparation HPLC etc. Their structures were identified b) means of spectra, in same cases by direct comparison with authentic samples. RESULTS: Ten compounds were obtained and identified as luteolin (1), luteolin-7-O-beta-D-glucopyranoside (2), apigenin-7-O-beta-D-glucopyrano side (3), luteolin-7-O-beta-D-glucopyranoside acatate (4), 3beta-(beta-D-glucopyranosyloxy) -8beta- (p-hydroxyphenylacetyloxy) -guaia-4 (15), 10 (14), 11 (13) -trien-1alpha, 5beta, 6beta, 7alphaH-12, 6-olide (5), beta- (beta-D-glucopyranosyloxy) -8beta- (2-hydroxy-3-methylbutanoyloxy) -guaia-4 (15),10 (14), 11 (13) -trien-1alpha, 5beta, 6beta,7alphaH-12,6-olide (6), 5, 3', 4'-trihydroxy-7-methoxyflavone (7), apigenin (8), 5-hydroxy-7,4'- dimethoxyflavone (9), 5, 7, 4'- trimethoxyflavone (10). CONCLUSION: Compounds (5, 6, 7, 9, 10) are isolated from this plant for the first time.

Ginsenoside Rg1 Inhibits STAT3 Expression by miR-15b-5p to Attenuate Lung Injury in Mice with Type 2 Diabetes Mellitus-Associated Pulmonary Tuberculosis.

Type 2 diabetes mellitus (T2DM) has been regarded as a critical risk factor for pulmonary tuberculosis (PTB). Ginsenoside Rg1 has been identified as a potential therapeutic agent for T2DM by suppressing the inflammatory response. However, the effect of Rg1 on T2DM-associated PTB has not been reported. In this study, we aimed to explore the function of Rg1 in the regulation of T2DM-associated PTB. We established a T2DM-associated PTB mouse model and found that the fibrosis of lung tissues was inhibited by Rg1 in T2DM-associated PTB mice. The lung injury of T2DM-associated PTB mice was repressed by Rg1. Moreover, the levels of IL-6, TNF-α, and IL-1ß in the lung tissues and serum were decreased by Rg1 in T2DM-associated PTB mice. The treatment with Rg1 inhibited the levels of free fatty acid and enhanced the expression of miR-15b-5p in lung tissues of T2DM-associated PTB mice. MiR-15b-5p targeted and inhibited the STAT3 expression. The expression of STAT3 was downregulated by Rg1, while the inhibition of miR-15b-5p reversed the downregulation. The expression of miR-15b-5p was reduced, but the expression of STAT3 was upregulated in the lung tissues of T2DM-associated PTB mice. We validated that miR-15b-5p attenuated inflammation and lung injury in the T2DM-associated PTB mouse model. The overexpression of STAT3 or the suppression of miR-15b-5p restored lung fibrosis and injury inhibited by Rg1 in T2DM-associated PTB mice. Meanwhile, the Rg1-repressed levels of IL-6, TNF-α, and IL-1ß were enhanced by the overexpression of STAT3 or the suppression of miR-15b-5p. In addition, the levels of free fatty acid repressed by Rg1 were reversed by STAT3 overexpression and miR-15b-5p inhibition. Thus, we conclude that ginsenoside Rg1 inhibits the STAT3 expression by miR-15b-5p to attenuate lung injury in mice with type 2 diabetes mellitus-associated pulmonary tuberculosis.

Two new glycosides from Panzerina lanata (L.) Soják.

Two new glycosides, namely panalaside A (1) and panalaside B (2) were isolated from from Panzerina lanata (L.) Soják. The structures of 1 and 2 were elucidated by spectroscopic methods, including UV, IR, HR-ESI-MS and extensive 1 D and 2 D NMR techniques.

Structural elucidation and α­glucosidase inhibitory activity of a new xanthone glycoside from Lomatogonium rotatum (L.) Fries es Nym.

A new xanthone glycoside, 1,8-dihydroxyl-2,5-dimethoxy-xanthone-6-O-ß-D-glucoside (1), along with two known xanthone glycosides and two flavonoid glycosides were isolated from the aerial parts of Lomatogonium rotatum (L.) Fries es Nym. The structure of 1 was elucidated by analysis of its spectroscopic data, including UV, IR, HR-ESI-MS and extensive 1 D and 2 D NMR techniques. In vitro test, compound 1 behaved similarity to swertianolin against α­glucosidase and more potent inhibitory effects than the positive control, acarbose.

Two new compounds from supercritical fluid extract of Artemisia integrifolia L.

Two new compounds, namely integrin A (1) and integrin B (2), were isolated from the supercritical fluid extract (SFE) of Artemisia integrifolia L. Their structures were elucidated by spectroscopic methods, including UV, IR, HR-ESI-MS and extensive 1D and 2D NMR techniques.

Synthesis and antitumor activity of sacroflavonoside.

Sacroflavonoside, a new derivative of diphenylethene, was isolated from Artemisia sacrorum, which have been found to possess the inhibitory effect on the proliferation of gastric carcinoma cells (MKN-45) in vitro in our previous studies. With anisaldehyde (SM-A) as starting material, the sacroflavonoside was synthesized by nucleophilic addition, electrophilic substitution and dehydration cyclization. The structure of sacroflavonoside was established by 1 D (1H NMR and 13C NMR) and 2 D-NMR (HSQC and HMBC) spectral analysis. The antitumor activity and potential mechanism against MKN-45 cells of sacroflavonoside were evaluated in vitro. The results showed that sacroflavonoside could significantly induce MKN-45 cells apoptosis and autophagy by increasing the expression of Bax, Caspase-3, Beclin1 and LC3-II proteins and decreasing the expression of Bcl-2 protein at low micromole level. This investigation provided a valuable lead structure for the development of antitumor drugs.

Structure elucidation and NMR assignments of a new alkaloid from Panzerina lanata (L.) Soják.

A new alkaloid, named as panalasin (1), was isolated from the ethyl acetate extract from Panzerina lanata (L.) Soják. The structure of 1 was elucidated by spectroscopic methods, including UV, IR, HR-ESI-MS and extensive 1D and 2D NMR techniques.

Structure elucidation and NMR assignments of a new sesquiterpene of volatile oil from Artemisia frigida Willd.

A new sesquiterpene, artefrigin (5), together with four known sesquiterpenes were isolated from the volatile oil of Artemisia frigida Willd. The structure of five was elucidated by spectroscopic methods, including UV, IR, HR-ESI-MS and extensive 1D and 2D NMR techniques.