OBJECTIVE:To study the relieving cough and eliminating phlegm effects of stemoninine combined with mogrosideⅤ on mice,and select its optimal ratio. METHODS:70 mice were selected in each experiment and randomly divided into 7 groups,namely solvent group(normal saline), codeine(15 mg/kg)or ambroxol(30 mg/kg)group(positive control),stemoni-nine group(30 mg/kg),mogroside Ⅴ group(30 mg/kg),stemoninine-mogroside Ⅴ combination group(30 mg/kg)with mass ra-tio of 2:1,1:1,1:2,ig,once a day. Ammonia-induced cough experiment(positive drug was codeine)and tracheal phenol red ex-cretion experiment(positive drug was ambroxol)were respectively conducted. Using cough latent period,cough times and volume of tracheal phenol red excretion as indexes,the antitussive and expectorant effects of drug in each group were compared. RE-SULTS:Compared with solvent group,cough latent period was obviously shortened,cough times was obviously reduced,volume of tracheal phenol red excretion was obviously increased in each administration group(P<0.05 or P<0.01). Compared with mogro-side Ⅴ group,cough latent period was obviously shortened,cough times was obviously reduced in stemoninine-mogroside Ⅴgroup with different mass ratios(P<0.05),and 2:1,1:1 groups showed the best effects. Compared with stemoninine group,vol-ume of tracheal phenol red excretion was obviously increased in stemoninine-mogroside Ⅴ group with different mass ratios (P<0.05),and 1:1,1:2 groups showed the best effects. CONCLUSIONS:The combination of temoninine and mogroside Ⅴ shows synergistic effects on relieving cough and eliminating phlegm,stemoninine-mogrosideⅤmass ratio of 2:1,1:1 can be used as pre-ferred combination of reference.

The chemical constituents of Taxus chinensis var. mairei cell cultures were investigated by chromatographic methods, including silica gel column chromatography, Sephadex LH-20 and preparative HPLC. Thirteen compounds were isolated from the 80% ethanol extract of cultured cells and their structures were elucidated by spectral data and physicochemical properties, which were identified as 2α,4α,7β,9α,10β-pentaacetoxy-14β-hydroxytax-11-ene (1), 2α,4α,7β,9α,10β-pentaacetoxytax-11-ene (2), 1β-deoxybaccatin VI (3), 2α-acetoxytaxusin (4), taxuyunnanine C (5), yunnanxane (6), 2α,5α,10β-triacetoxy-14β-propionyloxy-4 (20), 11-taxadiene (7), 2α,5α,10β-triacetoxy-14β-isobutyryloxy-4 (20), 11-taxadiene (8), 2α,5α,10β-triacetoxy-14β-(2'-methyl)butyryloxy-4 (20), 11-taxadiene (9), 13-dehydroxylbaccatin III (10), 13-dehydroxy-10-deacetylbaccatin III (11), paclitaxel (12) and (13) β-sitosterol. Among them, compound 1 is a new compound, and compounds 2, 4, 10 and 11 are isolated from the cell culture of Taxus chinensis var. mairei for the first time.

Objective:To assess the value of amide proton transfer weighted (APTw) imaging in the evaluation of pH changes in infarct core (IC) and ischemic penumbra (IP) in subacute cerebral infarction.Methods:The data of twenty-three subacute cerebral infarction patients with unilateral steno-occlusive disease of the middle cerebral artery (subacute infarction group) from April to November 2019 in the First Affiliated Hospital of Dalian Medical University were prospectively analyzed. Fifteen healthy volunteers were enrolled in this study as the control group. All subjects underwent conventional MRI, DWI, 3D-pseudo continuous arterial spin labeling (3D-pCASL) and APTw sequences. Based on DWI images, relative cerebral blood flow (rCBF) and APTw images to determine the region of IC, blood flow penumbra [cerebral blood flow(CBF)-DWI mismatch area, IP CBF] and metabolic penumbra (APTw-DWI mismatched area, IP APT). 3D ROIs were used to semi-automatically measure the APTw signals and the volume of IC and IP CBF of the patients in subacute infarction group. The comparison of APTw signals between the infarct side and the contralateral side in the subacute infarction group, the comparison of bilateral APTw signals in the control group, and the comparison of APTw signals in the IC and IP CBF regions were performed by paired-sample t test or Wilcoxon signed-rank test. The paired-sample t test or Mann-Whitney U test was used to compare the APTw signals between the two groups. The Friedman test was applied to compare the difference of volumes among IP CBF1.5, IP CBF2.5 and IP APT . Results:There was no significant difference of the APTw signals among the IC, the contralateral side in the subacute infarction group and the control group ( P>0.05). The APTw signals of IP CBF and IC of the infarction group were statistically different ( P<0.05). Compared with the contralateral side of IP CBF1.5 (3.7±1.7, -1.84±1.48, 5.57±2.75), the APTwmax (3.07±1.41, t=-3.012, P=0.006), APTw min [-1.30 (-1.74, -0.57), Z=-2.099, P=0.036], and APTwmax-min(4.51±2.58, t=-3.273, P=0.003) signals in the IP CBF1.5 were decreased ( P<0.05). Compared with the contralateral side of IP CBF2.5 [-1.53 (-2.80, -0.91), 5.31±2.61], the APTw min [-1.08 (-1.60, -0.49), Z=-2.616, P=0.009] and APTwmax-min (4.41±2.72, t=-3.228, P=0.004) signals in the IP CBF2.5 were decreased. The volumes of IP CBF1.5 [107.51(50.08, 138.61)mm 3], IP APT [99.00 (53.27, 121.335) mm 3] and IP CBF2.5 [89.91 (51.53, 139.87) mm 3] were successively reduced (χ2=7.913, P=0.019), and the volume of IP CBF2.5 was significantly smaller than that of IP CBF1.5 ( P=0.037). Conclusion:The acid-base metabolism in the IC of subacute cerebral infarction is not obvious, but the blood flow penumbra has local acid-base metabolism imbalance, and the range of metabolic penumbra coincides with the blood flow penumbra.

Chiral drug naftopidil (NAF), a specific-adrenoceptor (AR) antagonist for the treatment of benign prostatic hyperplasia, was used in racemic form for several decades. Our recent work declared that NAF enantiomers showed the same antagonistic effects on the-AR, but the binding mechanism of these two stereochemical NAF isomers to thereceptor remained unclear. Herein, we reported the crystallographic structures of optically pure NAF stereoisomers for the first time and unambiguously determined their absolute configurations. The crystal data ofandenantiomers matched satisfactorily the pharmacophore model for-selective antagonists. Based on the constructedhomology model, molecular docking studies shed light on the molecular mechanism of NAF enantiomers binding to-AR. The results indicated that NAF enantiomers exhibited the very similar binding poses and occupied the same binding pocket.

Nine compounds were isolated from the aerial part of Callicarpa kwangtungensis chun by various column chromatographic methods. Their structures were identified as pinnatifidanoid A(1), blumenol C(2), megastigman-5- ene-3β, 9R-diol(3), 3β-hydroxyurs-12-en-28-oic acid(4), kaji-ichigoside F1(5), 1, 4-terephthalic acid(6), syringic acid(7), vanillic acid(8), and 3, 5-dimethoxy-4-methylbenzyl alcohol(9)on the basis of spectral analysis. C13 nor-isoprenoids of 1-3, and compounds 5, 6 and 9, were isolated from the genus Callicarpa for the first time.