PLANTA MEDICA
·
2016
·Vol. 83
·期 07
·624-630
·
IF 1.99
Yi-Lin Zhang,Jia-Wen Xu,Xiong-Hao Wu,Peng-Xiao Chen,Fang Wei,Dong-Dong Gao,Xiao-Wen Chen,Yu-Li Luo,Yun-Xin Zhu,Jiehong Huang,Ya-Xia Tan,Lei Zhao,Wen-Liang Zhou
Sodium tanshinone IIA sulphonate, a water-soluble derivative of tanshinone IIA, has been proven to possess versatile biological properties, but its pharmacological effect on tracheal smooth muscle remains elusive. This paper presents a study on the relaxant effect and underlying mechanisms of sodium tanshinone IIA sulphonate on mouse tracheal smooth muscle. The relaxant effect of sodium tanshinone IIA sulphonate was evaluated in mouse tracheal rings using a mechanical recording system. Intracellular Ca2+ concentration was measured in primary cultured tracheal smooth muscle cells using confocal imaging system. The results showed that sodium tanshinone IIA sulphonate induced dose-dependent relaxation of mouse tracheal rings in a β-adrenoceptor- and epithelium-independent manner. Pretreatment with the ATP-sensitive K+ channel blocker glibenclamide partly attenuated the relaxation response. Administration of sodium tanshinone IIA sulphonate notably inhibited the extracellular Ca2+-induced contraction. High KCl or carbachol-evoked elevation in the intracellular Ca2+ concentration was also abrogated by sodium tanshinone IIA sulphonate in tracheal smooth muscle cells. In conclusion, the tracheal relaxant effect of sodium tanshinone IIA sulphonate was independent of β-adrenoceptor and airway epithelium, mediated primarily by inhibition of extracellular Ca2+ influx via L-type voltage-dependent Ca2+ channels and partially by activation of the ATP-sensitive K+ channel. These results indicate the potential therapeutic value of sodium tanshinone IIA sulphonate for asthma treatment.
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PLANTA MEDICA
·
2016
·
IF 1.99
Min Li,Fen Liu,Yong-Ri Jin,Xiao-Zhong Wang,Qian Wu,Ying Liu,Xu-Wen Li
Five new triterpenoid saponins (1–5) and four known triterpenoid saponins, ginsenoside Re5 (6), majonoside R1 (7), 24(R)-majonoside R1 (8), and ginsenoside Rf (9), were isolated from the rhizomes of Panacis majoris. The structures of new compounds were elucidated as (20S,24S,25R*)-6-O-[β-D-glucopyranosyl-(1 → 2)-β-D-glucopyranosyl]-dammar-20,24-epoxy-3β,6α,12β,25,26-pentaol (1), (20S,24R,25R)-6-O-[β-D-glucopyranosyl-(1 → 2)-β-D-glucopyranosyl]-dammar-20,24-epoxy-3β,6α,12β,25,26-pentaol (2), (20S)-6-O-[β-D-glucopyranosyl-(1 → 2)-β-D-glucopyranosyl]-dammar-20,25-epoxy-3β,6α,12β,24α-tetraol (3), 6-O-[β-D-glucopyranosyl-(1 → 2)-β-D-glucopyranosyl]-dammar-3β,6α,12β,20S,24R,25-hexaol (4), and 6-O-[β-D-glucop-yranosyl-(1 → 2)-β-D-glucopyranosyl]-dammar-25(26)-ene-3β,6α,12β,20S,24R-pentaol (5) on the basis of extensive spectral analysis and chemical methods. Ginsenoside Re5 was isolated from the plant for the first time. The similarities of the nine compounds lie in the fact that their aglycones are conjoined with the same glucopyranose moieties, the same linkage of the glycosyl chains, and the same glycosylation sites, while they have a varied C-17 side chain. Compounds 3 and 5 exhibited moderate antiplatelet aggregation activities induced by adenosine diphosphate with IC50 values of 23.24 and 18.43 µM, respectively. Compound 5 displayed moderate inhibition of arachidonic acid-induced platelet aggregation with an IC50 value of 30.11 µM.
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PLANTA MEDICA
·
2016
·Vol. 82
·期 03
·230-237
·
IF 1.99
Xueli Zhang,Jiajia Lv,Liling Wang,Hua Shao
Taxanes are a class of bioactive compounds isolated from the Taxus species. 10-Deacetylbaccatin III is one of the popular taxane compounds with antitumor activity, but the pharmacokinetic profile of this compound remains elusive. Previously, we prepared the taxane fractions from the twigs and leaves of Taxus chinensis var. mairei containing 20.4 % 10-deacetylbaccatin III. This study aimed to investigate the pharmacokinetics of 10-deacetylbaccatin III and biodistribution, and explore the potential changes when it was administered in the form of taxane extracts. A simple, sensitive, and reliable liquid chromatography-tandem mass spectrometry method was developed and validated for the quantitative determination of 10-deacetylbaccatin III in biosamples. The results showed that 10-deacetylbaccatin III, after oral dosing, displayed a quick absorption into the blood and distribution into major organs. Oral administration of 10-deacetylbaccatin III in the form of taxane mixtures led to a 16-fold increase in the systemic exposure of pure 10-deacetylbaccatin III, with the AUC0-U in the plasma increasing from 25.75 ± 11.34 to 231.36 ± 70.12 µg h/L (p T. chinensis var. mairei, which contributed to an enhanced systemic exposure of pharmacologically active taxanes.
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SYNTHESIS-STUTTGART
·
2017
·Vol. 49
·期 08
·1867-1873
·
IF 2.65
Jun Gu,Canbin Qiu,Wenbin Lu,Qun Qian,Kunhua Lin,Hegui Gong
The use of pyridine as the sole ligand for the reductive vinylation of unactivated secondary alkyl halides under Ni-catalyzed conditions has been developed. Both alkyl- and aryl-substituted vinyl bromides are suitable, in which alkyl-decorated α-alkenyl bromides resulted in the α-products in good results.
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PLANTA MEDICA
·
2017
·Vol. 84
·期 02
·123-128
·
IF 2.342
Fang Wang,Huanhuan Zhong,Shiqi Fang,Yunfeng Zheng,Cunyu Li,Guoping Peng,Xinchun Shen
Eupatorium lindleyanum has traditionally been used as folk medicine in Asian countries for its therapeutic effects on tracheitis and tonsillitis. Investigation of the anti-inflammatory active constituents from E. lindleyanum led to the isolation of two novel sesquiterpene lactones, named eupalinolide L (1) and eupalinolide M (2), and seven known sesquiterpene lactones (3–9). The structures and configurations of the new compounds were determined on the basis of spectroscopic analysis, especially 2D NMR techniques. In vivo experiments showed that the sesquiterpenes fraction significantly reduced mouse ear edema induced by xylene (18.6%, p in vitro assays, compounds 1–9 showed excellent anti-inflammatory activities, as they lowered TNF-α and IL-6 levels in lipopolysaccharide-stimulated murine macrophage RAW 264.7 cells (p E. lindleyanum can be developed as novel potential natural anti-inflammatory agents.
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SYNTHESIS-STUTTGART
·
2015
·Vol. 47
·期 19
·3049-3060
·
IF 2.689
Jialin Wang,Jiaqi Liu,Hao Lan,Wenyi Chu,Zhizhong Sun
Intramolecular Friedel–Crafts acylation reactions of 2-arylphenoxyacetic acids are accomplished using trifluoroacetic anhydride or trifluoromethanesulfonic acid at 0 °C or room temperature. Depending on the reaction conditions, dibenzoxepines or arylcoumaranones are obtained in good yields and with high selectivities (83–100%). Plausible mechanistic pathways for the selective formation of the different reaction products are discussed.
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SYNTHESIS-STUTTGART
·
2015
·Vol. 47
·期 23
·3783-3796
·
IF 2.689
Guozhu Li,Mingshu Wu,Fengjiao Liu,Jie Jiang
Various spiro[indole-pyrrolizine], spiro[indole-indolizine], and spiro[indole-pyrrolidine] gem-bisphosphonates were prepared by multicomponent reactions between isatins, tetraethyl vinylidenebis(phosphonate), and amino acids in the presence of montmorillonite. The one-pot reactions proceeded by 1,3-dipole cycloadditions of azomethine ylides formed in a decarboxylative manner. The proposed mechanism is in line with experimental data that confirmed that the azomethine ylide is formed in a decarboxylative manner; this provides new insight into the underlying mechanisms of such cycloadditions. The method has many notable features, such as a broad substrate scope, high efficiency, and high regioselectivity.
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SYNTHESIS-STUTTGART
·
2014
·Vol. 46
·期 05
·621-628
·
IF 2.443
Shengrong Liao,Chun Qin,Peifen Yao,Jinsheng Li,Xuefeng Zhou,Junfeng Wang,Zhishu Huang,Yonghong Liu
A facile and efficient synthesis of novel seven-membered heterocyclic derivatives containing 3-aminoazepan-2-one backbone is described using 1,4-protected piperazine-2,5-diones and alkynes as starting materials. The reaction may undergo Michael addition, unusual nucleophilic attack to an amide group, and keto–enol tautomerization. The reaction showed different reactivity when using substrates with different protecting groups: it had higher efficiency when using either alkanoyl-protecting group with cesium carbonate as the base, or benzoyl-protecting group with triethylamine as the base, but no reaction when using benzyl or allyl protecting groups with a variety of bases (Et3N, DBU, K2CO3, Cs2CO3, KHCO3, CsHCO3, and KOt-Bu).
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PLANTA MEDICA
·
2013
·
IF 2.348
Cui-Ting Luo,Huan-huan Zheng,Shuang-Shuang Mao,Mao-xun Yang,Cheng Luo,Heru Chen
Two new xanthones, 1,8-dihydroxy-3-methoxyxanthone 7-O-[α-L-rhamnopyranosyl(1 → 2)-β-D-glucopyranoside] (1) and 1,8- dihydroxy-3-methoxyxanthone 7-O-[α-L-rhamnopyranosyl(1 → 3)-α-L-rhamno-pyranosyl (1 → 2)-β-D-xylopyranoside] (2), together with 26 known xanthones (3–28), were isolated from the aqueous ethanol extract of the traditional Chinese herb Swertia mussotii. Their structures were elucidated via spectroscopic analyses including 2D NMR. The inhibition of α-glucosidase by the isolated xanthones was evaluated by an in vitro high-throughput screening assay. Our results indicated that 1,3,5,8-tetrahydroxyxanthone is the best inhibitor with an IC50 value of 5.33 ± 0.09 µM, while the O-glycosylated xanthones were poor α-glycosidase inhibitors.
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高影响因子
SYNTHESIS-STUTTGART
·
2014
·Vol. 46
·期 21
·2917-2926
·
IF 2.443
Xin Huang,Chunling Fu,Shengming Ma
We have demonstrated two improved methods for the synthesis of carbohydrate-based terminal allenes from propargyl or homopropargyl glycosides. The reaction of propargyl or homopropargyl glycosides with paraformaldehyde (2.5 equiv) in the presence of copper(I) iodide (10 mol%) and diisopropylamine (1.8 equiv) or copper(I) iodide (50 mol%) and dicyclohexylamine (1.8 equiv) produces sugar-linked terminal allenes in 50–79% yield.
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PLANTA MEDICA
·
2014
·Vol. 80
·期 13
·1107-1112
·
IF 2.339
Yu-xia Mei,Wei Yang,Pei-xin Zhu,Nan Peng,Hai Zhu,Yun-xiang Liang
A novel heteroglycan, Cordyceps sinensis polysaccharide 1 (molecular weight 1 17 × 105 Da), was isolated and purified from mycelia of the fungus C. sinensis obtained by solid-state culture. Structural characterization by chemical analysis, GC-MS, FTIR, and NMR spectroscopy showed that C. sinensis polysaccharide 1 was mainly composed of (1 → 6)-linked α-D-Glc and α-D-Gal, with minor β-(1 → 4)-D-Xyl and β-(1 → 4)-D-Man residues probably located in the side chains with a trace amount of α-(1 → 3)-L-Rha residue. In biological assays, C. sinensis polysaccharide 1 significantly inhibited proliferation of sarcoma 180 cells and induced apoptosis in a dose-dependent manner. Further studies will elucidate the antitumor mechanism of C. sinensis polysaccharide 1 and promote its utilization for the development of novel, effective anticancer drugs.
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SYNTHESIS-STUTTGART
·
2013
·Vol. 45
·期 24
·3349-3354
·
IF 2.5
Haidong Wei,Tianbin Li,Yue Zhou,Lihong Zhou,Qingle Zeng
Alkyl halides, including heteroarylmethyl and arylmethyl halides, bromoacetate, and cinnamyl bromide, are readily prepared via halogenation from basic raw materials, even using green processes. It is essential to replace their downstream products with them to prepare medicinally important heterocycles quinazolin-4(3H)-ones. Copper(I) bromide catalyzed domino reaction of alkyl halides and anthranilamides under air affords 2-substituted quinazolin-4(3H)-ones in good to excellent yields and with wide functional group tolerance. A mechanism for a copper(I) bromide involved organometal-catalyzed reaction via a four-step domino reaction is proposed.
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