Synthesis and biological evaluation of ethyl 6-alkoxy-7-phenyl-4-hydroxy-3-quinolinecarboxylates against Eimeria tenella

A series of ethyl 6-alkoxy-7-phenyl-4-hydroxy-3-quinolinecarboxylates were designed and synthesized.Their structures were confirmed by ~1H NMR,^(13)C NMR,IR and HRMS.The biological activities were primarily evaluated against Eimeria tenella according to Anticoccidial Index(ACI) method in vivo.The results showed that compounds 5e,5f and 5i exhibited anticoccidial activities against E.tenella at 27 mg kg^(-1).

Synthesis of fused pyran and arylbis(4-hydroxy-6-methyl-2-oxo-2H-pyran-3-yl)methane in ionic liquid

Promoted and mediated by an ionic liquid-[bmim][BF4], fused pyrans or arylbis（4-hydroxy-6-methyl-2-oxo-2H-pyran-3- yl）methanes were efficiently and selectively prepared from the reaction of aldehyde and 4-hydroxy-6-methyl-2-oxo-pyran with or without acetic anhydride. By using these novel procedures, pyrimidine nucleoside-fused pyran and arylbis（pyranon-3-yl）methane hybrids with potential biological activities were constructed.

The new antioxidant 1-benzoyl-6-hydroxy-2,2,4-trimethyl-1,2- dihydroquinoline has a protective effect against carbon tetrachloride-induced hepatic injury in rats

Liver diseases with the central pathogenetic mechanism of oxidative stress are one of the main causes of mortality worldwide.Therefore,dihydroquinoline derivatives,which are precursors of hepatoprotectors and have antioxidant activity,are of interest.We have previously found that some compounds in this class have the ability to normalize redox homeostasis under experimental conditions.Here,we initially analyzed the hepatoprotective potential of the dihydroquinoline derivative 1-benzoyl-6-hydroxy-2,2,4-trimethyl-1,2-dihydroquinoline(BHDQ)for carbon tetrachloride(CCl4)-induced liver injury in rats.Results suggested that BHDQ normalized the alanine aminotransferase,aspartate aminotransferase,and gamma-glutamyl transpeptidase in serum.We also observed an improvement in liver tissue morphology related to BHDQ.Animals with CCl4-induced liver injuries treated with BHDQ had less oxidative stress compared to animals with CCl4-induced liver injury.BHDQ promoted activation changes in superoxide dismutase,catalase,glutathione peroxidase,glutathione reductase,and glutathione transferase on control values in animals with CCl4-induced liver injury.BHDQ also activated gene transcription in Sod1 and Gpx1 via nuclear factor erythroid 2-related factor 2 and forkhead box protein O1 factors.Therefore,the compound of concern has a hepatoprotective effect by inhibiting the development of necrotic processes in the liver tissue,through antioxidation.

A Facile Synthesis of 6β-Hydroxy-7α(H)-eudesma-4-en-3-one

A stereoselective total synthesis of 6β-hydroxy-7α(H)-eudesma-4-en-3- 1startingfrom (+)-dihydrocarvone 7 has been described.

Antioxidant Activity of the Natural Flavonoid 7-Hydroxy-5,6,4’-trimethoxyflavone Isolated from the Leaves of Lippia rugosa A. Chev

Phytochemical studies and antioxidant activities were carried out on n-hexane, ethyl acetate, ethanol and methanol extracts of the leaves of Lippia rugosa A. Chev (Verbenaceae), a medicinal plant used traditionally in the Cameroonian savannah’s region to protect foodstuffs and to cure degenerative diseases. Results indicated that theses extracts contain terpenoids, phenolic and flavonoid compounds. Except the n-hexane extract, all of the obtained extracts exhibit antioxidant activities with the ethanol extract being the most effective with an inhibition percentage of 85.668% ± 1.233% and an inhibition concentration (IC50) of 58 μg/ml (R2 = 0.987, P < 0.01) at a concentration of 100 mg/ml. Chromatographic separation on silica gel of the ethanol extract led to the isolation of a pure organic compound which was characterized as 7-hydroxy-5,6,4'-trimethox- yflavone by extensive 1D and 2D NMR spectroscopy, a flavonoid exhibiting antioxidative activity with an inhibitory percentage of 25.506% ± 0.205% and inhibition concentration (IC50) of 221 μg/ml (R2 = 0.966, P < 0.01). This is the first time that 7-hydroxy-5,6,4'-trimethoxyflavone is being isolated from L. rugosa and its antioxidant activity evaluated.

The First Total Synthesis of Natural 6β-Cinnamoyloxy-1α- hydroxy-5, 10-bis-epi-eudesm-4-en-3-one

The first total synthesis of natural 6β-cinnamoyloxy-1α-hydroxy-5, 10-bis-epi- eudesm-4-en-3-one （1）, a highly complex natural eudesmane, was described.

Argentum 5-Hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate:Synthesis,Crystal Structure and Antitumor Activity

In order to improve the water solubility and bioavailability of 5-hydroxy-7-methoxyflavone,argentum 5-hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate[Ag4(H2O)6](C(16)H(11)O4SO3)4·H2O(1,C(16)H(11)O4SO3=5-hydroxy-7-methoxy-2-phenyl-4H-chromen-4-one-6-sulfonate)was synthesized by sulfonation reaction.The structure of 1 was characterized by FT-IR,elemental analysis and X-ray single-crystal diffraction.Complex 1 belongs to the triclinic system,space group P1,a=8.077(4),b=12.365(4),c=17.735(7)A,V=1685.0(12)A3,Z=1,μ=1.372 mm^–1,Dc=1.936 g/cm^3,F(000)=984,the final R=0.0819 and wR=0.2332 with I>2σ(I).3D structure of 1 exhibits alternating organic and inorganic regions.O–H×××O hydrogen bonds and Ag–O coordination interactions exist among crystal water,coordinated water and sulfo group,which constructed an organic zone.Flavone skeletons form organic region of 1.Sulfo group is the bridge linking these two regions.The in vitro antitumor activity of 1 against human lymphoma cells U937 and human breast cancer cells MCF-7 were evaluated with CCK-8 assay.The result shows that 1 showed inhibitory activity against tumour cell U937 and MCF-7,and indicated that flavone sulfonate derivatives may be potential leads for further biological screenings and may generate drug-like molecules.

A New Halogenated Biindole and A New Apo-carotenone from Green Alga Chaetomorpha basiretorsa Setchell

A new halogenated biindole and a new apo-carotenone have been isolated from the ethanolic extract of the green alga Chaetomorpha basiretorsa Sethcell. On the basis of chemical and spectroscopic methods including 2D NMR technique, their structures have been elucidated as 4,4′-dichloro-5,5′-dibromo-7,7′-dimethoxy-2,2′-bi-1H-indole and 1′S*,4′R*-8-(4′-hydroxy-2′,6′,6′- trimethylcyclohex-2-enyl)-6-methyloct-3E,5E,7E-trien-2-one, respectively.

A New Chromone Derivative from Stellera chamaejasme L

A new chromone derivative, 3-[1- (2, 4, 6-trihydroxyphenyl) 3-di-(4-hydroxyphenyl) 1-propanone-2-yl] 5,7-dihydroxy-8-di(4-hydroxyphenyl)methyl-4H-1-benzopyran-4-one, named as isomohsenone was isolated from the roots of Stellera chamaejasme L. together with known chamaechromone. Its structure was determined by the analysis of MS and NMR data, especially 2D NMR spectra.

A New Bisxanthone from Hypericum japonicum Thunb.ex Murray

A new bisxanthone, named bijaponicaxanthone C, was isolated from the whole plant of Hypericum japonicum. The structure was elucidated as 6-[1’’,5’’,6’’-trihydroxy-2’’’-(β-hydroxy-β- methylethyl)-2’’’,3’’’-dihydrofuran(5’’’,4’’’,3’’,4’’)xanthone-3’’’-oxyl]-1,3,5-trihydroxy-4-isoprenylxant- hone (1) on the basis of the spectral and chemical evidences.

New flavan and unusual chalcone glycosides from Drypetes parvifolia

Two new compounds 7-hydroxy-5-O-（β-D-glucopyranoside） flavan （1） and （Z）-4＇,6＇-dihydroxy-2＇-O-（β-D-glucopyranoside） chalcone （2）, along with eight known compounds, were isolated from the stem bark of Drypetes parvifolia （Euphorbiaceae）. Their structures were established on the basis of spectroscopic analysis and chemical evidence.

A Phenolic Glucoside from Alangium plantanifolium

A novel phenolic glucoside was isolated from stem barks of Alangium plantanifolium, its structure was elucidated to be 1-O-[2-(1-hydroxy-6-oxocyclohex-2-ene-1-carboxymethyl) -phenyl]-4, 6-O-[(S)-4, 4', 5, 5', 6, 6'-hexahydroxydi-phenoyl]-beta -D-glucopyranose 1 by spectroscopic methods including 2D NMR techniques.

A new phenolic compound from Crinum asiaticum L.

A new phenolic compound was isolated from the ethanol extract of the bulbs of Crinum asiaticum L.var.sinicum Baker.Its structure was defined as 1-（2-hydroxy-4-hydroxymethyl）phenyl-6-O-caffeoyl-β-D-gluco-pyranoside on the basis of spectroscopic evidences.

4-(Succinimido)-1-butane sulfonic acid as a Bronsted acid catalyst for synthesis of pyrano[4,3-b]pyran derivatives under solvent-free conditions

4-（Succinimido）-1-butane sulfonic acid as an efficient and reusable Bronsted acid catalyzed the synthesis of pyrano[4,3-b]pyran derivatives under solvent-free conditions.The catalyst can be prepared by mixing succinimide and 1,4-butanesultone that is more simple and safer than the preparation of succinimide sulfonic acid.This method has the advantages of high yield,clean reaction,simple methodology and short reaction time.The catalyst could be recycled without significant loss of activity.

玄参药材中多类型成分的定量分析方法建立及其在脉络宁口服液中的应用

目的建立超高效液相色谱-串联三重四极杆质谱(UPLC-QqQ-MS/MS)方法同时测定玄参Scrophulariae Radix中多类型成分的含量,并将此方法应用于脉络宁口服液(Mailuoning Oral Liquid,MOL),为玄参药材和MOL的质量评价提供依据。方法采用Waters HSS T3色谱柱(100 mm×2.1 mm,1.8μm),以0.1%甲酸水溶液和乙腈为流动相进行梯度洗脱。质谱采用电喷雾离子源(electrospray ionization,ESI),在多反应监测模式(multiple reaction monitoring,MRM)下对环烯醚萜苷、苯丙素苷、有机酸和核苷4类成分进行定量分析,结合化学计量学分析评价不同批次样品的质量。结果化学计量学结果表明,不同地区的玄参药材得到了有效区分,其质量差异可能与其生长环境相关。此外,4个年份(2019、2020、2021和2022年)的MOL各自聚成1类,可能是当年使用的药材质量相对稳定使得同一年份的MOL质量更相近;通过正交偏最小二乘-判别分析(orthogonal partial least squares-discriminate analysis,OPLS-DA)进一步筛选出不同年份MOL中异毛蕊花糖苷、对甲氧基肉桂酸、腺苷、1-(3-hydroxy-4-methoxyphenyl)ethyl-3-α-L-rhamnopyranosyl-6-caffeoyl-β-D-glucopyranoside、对羟基苯甲酸、阿魏酸和原儿茶酸7个差异性化学成分。结论该方法特异性强、准确度高且稳定性好,可为MOL中臣药玄参的药材选择及复方整体质量评价提供科学依据。