AIMTo study the chemical consitituents of the n-butanol-extracts of Anabasis salsa and Various chromatographic techniques were used to the chloroform-extract of Anabasis brevifolia.

METHODSseparate and purify the constituents. Their physico-chemical properties and spectral data were used to elucidate their structures.

RESULTSFive compounds were isolated and identified as 2-O-beta-D-glucopyranosyloxy-4,6-dimethoxy phenylenthanone (1), 2-O-(2)-beta-D-glucopyranosyloxy-4, 6-dimethoxy phenylenthanone (2), 3-methyl-but-2-enoic acid-[2-(4-methoxy phenyl)-ethyl]-amide (3), 5,6,7,2'-tetramethoxy isoflavonoid (4), 2'-hydroxy-5,6,7-trimethoxyisoflavonoid (5).

CONCLUSIONCompounds 2, 3, and 5 are new compounds. And the others were isolated from Anabasis L. for the first time.

Chenopodiaceae ; chemistry ; Crotonates ; chemistry ; isolation & purification ; Glucosides ; chemistry ; isolation & purification ; Isoflavones ; chemistry ; isolation & purification ; Molecular Structure ; Plants, Medicinal ; chemistry

AIMTo study the chemical constituents of the underground part of Ligularia pleurocaulis (Franch.) Hand-Mazz.

METHODSThe dried roots and rhizomes of L. pleurocaulis were extracted with methanol. Isolation and purification were performed by silica gel column chromatography and recrystallization etc. Structures of the pure compounds were established on basis of spectral analysis.

RESULTSTwelve compounds were obtained from L. pleurocaulis, they were 6-angeloyloxy-furanoligularenone (1), 2-oxo-3-hydroxy-eremophila-1(10),3,7(11),8-tetraen-8,12-olide (2), tiglic acid (3), oleanolic acid (4), lupeol (5), beta-sitosterol (6), daucosterol (7), caffeic acid (8), emodin (9), 7-methoxy-coumarin (10), ferulic acid (11) and 4-hydroxy-2,5-dimethoxy-benzaldehyde (12).

CONCLUSIONCompound 1 is a new eremophilane and compound 2 is a new natural compound. All above compounds were obtained for the first time from L. pleurocaulis.

Asteraceae ; chemistry ; Crotonates ; chemistry ; isolation & purification ; Molecular Conformation ; Molecular Structure ; Oleanolic Acid ; chemistry ; isolation & purification ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Rhizome ; chemistry ; Sesquiterpenes ; chemistry ; isolation & purification

OBJECTIVETo provide the foundation for reasonable utilization by analyzing the essential oils of Ligularia virgaurea.

METHODThe essential oils were extracted by using steam distillation and separated with GC capillary columns. The components were quantitatively determined with normalization method, and were identified with GC-MS.

RESULT41 components were identified, which took up 72.73% of the essential oils.

CONCLUSIONThe main components of essential oils were 4-methyl-1-(1-methylethyl)-3-cyclohexen-1-ol(14.369%), crotonic acid, 2,2-dimethyl-butanoic acid, 1-methyl-3-(1-methylethyl)-benzene, (1s-endo)-1,7,7-trimethyl-bicyclo[2,2,1]heptan-2-ol, trans-1-methyl-4-(1-methylethyl)-2-cyclohexen-1-ol, alpha-cadinol and alpha,alpha,4-trimethyl-3-cyclohexene-1-methanol.

Asteraceae ; chemistry ; Butyrates ; analysis ; Crotonates ; analysis ; Gas Chromatography-Mass Spectrometry ; Oils, Volatile ; chemistry ; isolation & purification ; Plant Oils ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry ; Terpenes ; analysis

Background: Disease-modifying therapy is the standard treatment for patients with multiple sclerosis (MS) in remission. The primary objective of the current analysis was to assess the efficacy and safety of two teriflunomide doses (7 mg and 14 mg) in the subgroup of Chinese patients with relapsing MS included in the TOWER study. Methods: TOWER was a multicenter, multinational, randomized, double-blind, parallel-group (three groups), placebo-controlled study. This subgroup analysis includes 148 Chinese patients randomized to receive either teriflunomide 7 mg (n = 51), teriflunomide 14 mg (n = 43), or placebo (n = 54). Results: Of the 148 patients in the intent-to-treat population, adjusted annualized relapse rates were 0.63 (95% confidence interval [CI]: 0.44, 0.92) in the placebo group, 0.48 (95% CI: 0.33, 0.70) in the teriflunomide 7 mg group, and 0.18 (95% CI: 0.09, 0.36) in the teriflunomide 14 mg group; this corresponded to a significant relative risk reduction in the teriflunomide 14 mg group versus placebo (-71.2%, P = 0.0012). Teriflunomide 14 mg also tended to reduce 12-week confirmed disability worsening by 68.1% compared with placebo (hazard ratio: 0.319, P = 0.1194). There were no differences across all treatment groups in the proportion of patients with treatment-emergent adverse events (TEAEs; 72.2% in the placebo group, 74.5% in the teriflunomide 7 mg group, and 69.8% in the teriflunomide 14 mg group); corresponding proportions for serious adverse events were 11.1%, 3.9%, and 11.6%, respectively. The most frequently reported TEAEs with teriflunomide versus placebo were neutropenia, increased alanine aminotransferase, and hair thinning. Conclusions: Teriflunomide was as effective and safe in the Chinese subpopulation as it was in the overall population of patients in the TOWER trial. Teriflunomide has the potential to meet unmet medical needs for MS patients in China. Trial Registration ClinicalTrials.gov, NCT00751881; https://clinicaltrials.gov/ct2/show/NCT00751881?term=NCT00751881&rank=1.
China ; Crotonates ; administration & dosage ; adverse effects ; therapeutic use ; Double-Blind Method ; Drug Administration Schedule ; Humans ; Immunosuppressive Agents ; administration & dosage ; adverse effects ; therapeutic use ; Multicenter Studies as Topic ; Multiple Sclerosis ; drug therapy ; metabolism ; Proportional Hazards Models ; Toluidines ; administration & dosage ; adverse effects ; therapeutic use

Emerging and re-emerging RNA viruses occasionally cause epidemics and pandemics worldwide, such as the on-going outbreak of the novel coronavirus SARS-CoV-2. Herein, we identified two potent inhibitors of human DHODH, S312 and S416, with favorable drug-likeness and pharmacokinetic profiles, which all showed broad-spectrum antiviral effects against various RNA viruses, including influenza A virus, Zika virus, Ebola virus, and particularly against SARS-CoV-2. Notably, S416 is reported to be the most potent inhibitor so far with an EC of 17 nmol/L and an SI value of 10,505.88 in infected cells. Our results are the first to validate that DHODH is an attractive host target through high antiviral efficacy in vivo and low virus replication in DHODH knock-out cells. This work demonstrates that both S312/S416 and old drugs (Leflunomide/Teriflunomide) with dual actions of antiviral and immuno-regulation may have clinical potentials to cure SARS-CoV-2 or other RNA viruses circulating worldwide, no matter such viruses are mutated or not.
Animals ; Antiviral Agents ; pharmacology ; therapeutic use ; Betacoronavirus ; drug effects ; physiology ; Binding Sites ; drug effects ; Cell Line ; Coronavirus Infections ; drug therapy ; virology ; Crotonates ; pharmacology ; Cytokine Release Syndrome ; drug therapy ; Drug Evaluation, Preclinical ; Gene Knockout Techniques ; Humans ; Influenza A virus ; drug effects ; Leflunomide ; pharmacology ; Mice ; Mice, Inbred BALB C ; Orthomyxoviridae Infections ; drug therapy ; Oseltamivir ; therapeutic use ; Oxidoreductases ; antagonists & inhibitors ; metabolism ; Pandemics ; Pneumonia, Viral ; drug therapy ; virology ; Protein Binding ; drug effects ; Pyrimidines ; biosynthesis ; RNA Viruses ; drug effects ; physiology ; Structure-Activity Relationship ; Toluidines ; pharmacology ; Ubiquinone ; metabolism ; Virus Replication ; drug effects