Research progress on hypoxia-induced imbalance of calcium homeostasis in pulmonary artery smooth muscle cells and its treatment / 中国药理学通报

Chronic hypoxic lung diseases are major causes of disability and mortality worldwide, which are typically aggravated by hypoxic pulmonary hypertension.The pathogenesis of hypoxic pulmonary hypertension is complex, and its mechanism has not been fully elucidated.The previous studies have shown abnormally elevated levels of free Ca + in the cytoplasm of pulmonary artery smooth muscle cells to be the predominant drivers of pulmonary hypertension , causing continuous contraction and remodeling of the pulmonary vessels.This article briefly summarizes the mechanism of hypoxia-induced imbalance in calcium homeostasis in pulmonary artery smooth muscle cells, together with its related drug research, based on the existing literature.Hypoxia induces an imbalance in calcium homeostasis in pulmonary artery smooth muscle cells by regulating hypoxia-inducible factor-1, K+ , store-operated calcium channel, receptor-operated calcium channel, the Ca +-sensing myosin contractile mechanism by binding to calmodulin, leading to pulmonary vasoconstriction.Ca + can also activate PKC/ MAPKs and PI3K/Akt/mTOR pathways, leading to pulmonary vascular remodeling.

Bioactive neolignans and lignans from the roots of Paeonia lactiflora / 中国天然药物

Two new neolignans and one new lignan (1-3) were obtained from the roots of Paeonia lactiflora. Their structures were unambiguously elucidated based on extensive spectroscopic analysis, single-crystal X-ray crystallography, and the calculated and experimental electronic circular dichroism (ECD) spectra. Compound 1 was a racemic mixture and successfully resolved into the anticipated enantiomers via chiral-phase HPLC. Compound 3 demonstrated moderate inhibitory activity against human carboxylesterase 2A1 (hCES2A1) with an IC50 value of 7.28 ± 0.94 μmol·-1.

Three new ursane-type triterpenoids from Rosmarinus officinalis and their biological activities / 中国天然药物

Three new ursane-type triterpenoids, 3-oxours-12-en-20, 28-olide (1), 3β-hydroxyurs-12-en-20, 28-olide (2) and 3β-hydroxyurs-11, 13(18)-dien-20, 28-olide (3), were isolated from a potent anti-inflammatory and antibacterial fraction of the ethanolic extract of Rosmarinus officinalis. Their structures were elucidated by a combination of extensive 1D- and 2D-NMR experiments, MS data and comparisons with literature reports. Compounds 1-3 exhibited significantly inhibitory effects on nitric oxide production in lipopolysaccharide-activated mouse RAW264.7 macrophages, but no antibacterial activity was found at a concentration of 128 μg·mL-1.

Construction and application of pharmacophore model of human carboxylesterase 2 inhibitors / 中国中药杂志

According to human carboxylesterase 2(hCE2) inhibitors reported in the literature, the pharmacophore model of hCE2 inhibitors was developed using HipHop module in Discovery Studio 2016. The optimized pharmacophore model, which was validated by test set, contained two hydrophobic, one hydrogen bond acceptor, and one aromatic ring features. Using the pharmacophore model established, 5 potential hCE2 inhibitors(CS-1,CS-2,CS-3,CS-6 and CS-8) were screened from 20 compounds isolated from the roots of Paeonia lactiflora, which were further confirmed in vitro, with the IC_(50) values of 5.04, 5.21, 5.95, 6.64 and 7.94 μmol·L~(-1), respectively. The results demonstrated that the pharmacophore model exerted excellent forecasting ability with high precision, which could be applied to screen novel hCE2 inhibitors from Chinese medicinal materials.

Research progress on chemical constituents and pharmacological activities of Trigonella foenum-graecum / 中国中药杂志

Trigonella foenum-graecum is an annual plant of the genus Trigonella in the Leguminosae family. It is widely distributed in China and has a long history of application. According to phytochemistry research, the seeds, stem, and leaves of this herb contain not only a variety of bioactive ingredients, including alkaloids, saponins, polysaccharides, flavonoids, and phenols, but also abundant nutrients such as unsaturated fatty acids and amino acids and various trace elements. Pharmacological studies have shown that both the extract of T. foenum-graecum and its chemical constituents exhibit hypoglycemic, hypolipidemic, antitumor, antioxidative, antimicro-bial, and hepatoprotective activities. This paper reviews the research progress on the chemical constituents and pharmacological effects of T. foenum-graecum, which may contribute to further development, application, and clinical research of this herb.

Bioactive sesquineolignans from the twigs of Litsea cubeba / 中国天然药物

In a continuing search for biological natural products with structure diversity from traditional Chinese herbs, five new sesquineolignans (1-5) were isolated from an ethyl acetate extract of the twigs of Litsea cubeba. Their structures were elucidated based on MS, 1D and 2D NMR spectroscopic data, as well as experimental electronic circular dichroism (ECD) spectra. Compounds 1-5 showed moderate inhibitory effects against LPS-induced NO production in RAW264.7 macrophages, with IC

Research progress in lipid-drug conjugates / 药学学报

The technology of lipid-drug conjugates is developed on the basis of prodrug principle, which overcomes some drawbacks of drugs via increasing the lipophilicity of hydrophilic or poorly soluble drugs to promote the absorption of drugs and enhance the curative effect. This article sums up the research progress of lipid-drug conjugates from the chemical synthesis methods of conjugates, the types of conjugates, the influence on biological activity of drugs, the application in nanoparticles for drug delivery and the mechanism of absorption and degradation.

Regional suitability analysis of endangered medicinal plant Dactylorhiza hatagirea / 中国中药杂志

The wild plant Dactylorhiza hatagirea commonly used in Tibetan medicine. In recent years, it is on the verge of extinction due to improper excavation and habitat deterioration. Based on the literature review, and the meteorological and ecological data of Qinghai Province and data derived from the field survey, this study took the altitude, humidity index, annual average wind speed, monthly average sunshine, precipitation and temperature in growing season, soil type and vegetation type as the zoning indexes, and applied ArcGIS software for spatial superposition analysis. The results showed that the D. hatagirea was primarily found in the alpine meadow in the east and south of Qinghai Province. The overall suitable area was about 30 700 km~2. Taking Qinghai Lake as the boundary for reference, the area in the south appeared to be more suitable, while the area in the east appeared to be secondary in suitability. Henan County, Zeku County, Jiuzhi County and Banma County were the main suitable areas covering the expanse of 12 454 km~2. Through the field verification, such zoning results appeared to be accurate, precise and illustrative. The spatial distribution of ecological suitability provides the decision-making basis for the resource investigation, environment protection and comprehensive resource management. It also provides the empirical case for developing the interdisciplinary research method in the suitability study of medicinal plants.

Extraction technology, composition analysis and antioxidant and antimicrobial activities of volatile oil from fenugreek leaves / 中国中药杂志

To define the extraction process, main components and antioxidative and antimicrobial activities of volatile oil from fenugreek(Trigonella foenum-graecum) leaves and its active substance basis. Response surface methodology was used for optimum supercritical CO_2 extraction conditions of essential oil from fenugreek leaves. The main components of volatile oil were analyzed by GC-MS, its antioxidant activity was evaluated by measuring the scavenging ability of 1,1-diphenyl-2-picrylhydrazyl(DPPH) and 2, 2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid, ABTS) free radical, and the antimicrobial effect of volatile oil was evaluated by K-B paper AGAR diffusion method. The results showed that the optimal extraction temperature was 50 ℃, the extraction time was 89 min, and the extraction pressure was 35 MPa. Under the conditions, the optimum extracting yield of volatile oil was 1.72%,which was about 1.5 times higher than that of the conventional steam distillation. A total of 52 compounds were found based on reference substance retention time and GC-MS fragmentation information or the existing literatures, and the major compounds were oleic acid(9.65%), carveol(9.41%), n-hexadecanoic acid(9.1%), linoleic acid(6.95%), methyl linolenate(5.4%), petroselinic acid(5.3%), testosterone(3.4%), sotolon(1.75%). The volatile oil of fenugreek showed moderate antioxidant activities in DPPH assay(IC_(50) value of 0.473 mg·mL~(-1)) and ABTS test(IC_(50) value of 0.107 mg·mL~(-1)). The oil had a stronger antimicrobial activity in vitro. MIC of the volatile oil ranged from 0.375 to 1.5 mg·mL~(-1). The results showed that the optimized volatile oil extraction process was stable, and the extraction yield was high. Fenugreek leaves contained a variety of volatile components, with obvious antioxidant and antibacterial activities. This study provides a certain theoretical basis for the comprehensive development and utilization of fenugreek.

Three new polyoxygenated bergamotanes from the endophytic fungus Penicillium purpurogenum IMM 003 and their inhibitory activity against pancreatic lipase / 中国天然药物

Purpurolides D-F (1-3), three new polyoxygenated bergamotanes bearing a 6/4/5/5 tetracyclic ring system, were isolated from the endophytic fungus Penicillium purpurogenum IMM 003. Their structures were unambiguously elucidated based on extensive spectroscopic data analyses, C NMR chemical shifts calculations coupled with the DP4+ probability method, and the calculated and experimental electronic circular dichroism (ECD) spectra. Compounds 1-3 showed significant inhibitory activity against pancreatic lipase (PL). The result highlights that the presence of 3-hydroxylated decanoic acid moiety at C-14 is important for increasing the inhibition potency against PL.

Study on sustainable development of Tibetan medicine resources on Qinghai-Tibet Plateau / 中国中药杂志

Through using the theoretical research results of traditional Chinese medicine resource management and sustainable utilization as references,this article systematically analyzes the relationship between economic subsystems for utilization of wild renewable resources in Tibetan medicine,resources,environment and social systems. It sorts out and designs the relationship diagram of the sustainable utilization system for Tibetan medicine resources,input and output relationship diagrams of economics subsystems for Tibetan medicine resources,development model diagram for Tibetan medical industrial chain,market development flow chart of wild herb resources of Tibetan medicine,causal circuit diagram of sustainable use mechanism for Tibetan medicine resources,cause tree of the stock and function for Tibetan medicine resources,cause tree of total income for Tibetan medicine resource utilization and tree diagram of compensation fund usage of Tibetan medicine resources. It provides an innovative research method for Tibetan medicine resources,and theoretical basis and relevant countermeasure for constructing sustainable approaches to development of wild renewable resources in Tibetan medicine.

Limonoids from seeds of Azadirachta indica and their antibacterial activity / 中国中药杂志

Fifteen limonoids were isolated from 95% ethanol extracts of the dry seeds of neem( Azadirachta indica) by various column chromatography techniques including silica gel,Pharmadex LH-20 gel and ODS resin. Based on spectroscopic analysis,their structures were determined as nimbocinol( 1),17β-hydroxynimbocinol( 2),1α,3α,7α-triacetylvilasinin( 3),7α-benzoyltrichilinin( 4),1,3-diacetyl-7-tigloyl-12-hydroxyvilasinin( 5),3-deacetylsalannin( 6),1-O-acetyl-1-detigloylsalannin( 7),2'( R),3'-dihydrosalannin( 8),2'( S),3'-dihydrosalannin( 9),2,3-dihydronimbolide( 10),6-homodesacetylnimbin( 11),gedunin( 12),7-deacetyl-7-epi-dihydrogedunin( 13),7-deacetoxy-7α-hydroxygedunin( 14) and nimbinene( 15). Compound 7 is a new natural product. 4,8,9,13 and 14 are isolated from the genus Azadirachta for the first time. Compound 2 showed inhibitory activity against Escherichia coli and Staphylococcus epidermidis,with MIC values of 32 and 128 mg·L~(-1),respectively. Compound 10 showed moderate inhibitory activity against S. epidermidis with a MIC value of 64 mg·L~(-1). Compound 11 inhibited the growth of E. coli and Pseudomonas aeruginosa,both with MIC values of 128 mg·L~(-1). Compound 15 exhibited inhibitory activity against P. aeruginosa,with a MIC value of128 mg·L~(-1).

Taraxastane-type triterpenoids from the medicinal and edible plant Cirsium setosum / 中国天然药物

Guided by TNF-α secretion inhibitory activity assay, four taraxastane-type triterpenoids, including two new ones, 22-oxo-20-taraxasten-3β, 30-diol (1) and 22α-hydroxy-20-taraxasten-30β, 30-triol (2), have been obtained from an active fraction of the petroleum ether-soluble extract of the the medicinal and edible plant Cirsium setosum. Their structures were elucidated by spectroscopic data and CD data analysis. In the TNF-α secretion inhibitory activity assay, compounds 1 and 2 were active with the IC of 2.6 and 3.8 μmol·L, respectively. In addition, compounds 1 and 2 showed moderately selective cytotoxicity against the human ovarian cancer (A2780) and colon cancer (HCT-8) cell lines.

Study on structural conversion of dihydrochelerythrine in different solvents / 中国中药杂志

Dihydrochelerythrine was isolated from the ethanol extract of Corydalis yanhusuo by chromatographic and recrystallization techniques. To our knowledge, this is the first report that dihydrochelerythrine was found to be unstable. The NMR, HPLC, and LC-MS were applied to monitor the structural conversion process of dihydrochelerythrine. The results showed that when dissolved in polar deuteration solvent (e.g., DMSO-₆ & MeOD), dihydrochelerythrine is directly converted to chelerythrine gradually. However, if used non-polar reagent (e.g.,CD₂Cl₂), the sample of dihydrochelerythrine undergoes the formation of pseudobase, chelerythrine, and bimolecular ether then followed by oxidation to oxychelerythrine as the major final product. Which leads to this phenomenon maybe is that the C-6 in dihydrochelerythrine is highly reactive to nucleophiles, and is easily converted to different derivatives in different solvents attributed to the solvent effect. This finding will contribute to the extraction and isolation, bioactivity screening, and quality evaluation of medicinal materials containing dihydrochelerythrine and other similar derivatives.

Temperature-dependent development and reproduction of rice leaffolder, Marasmia exigua (Lepidoptera: Pyralidae).

Marasmia exigua (Butler) (Lepidoptera: Pyralidae) is one of the major rice leaffolders negatively affecting the rice production in the world. The growth and development of M. exigua was studied at seven constant temperatures (10, 15, 20, 25, 27, 30 and 35°C). The results showed that M. exigua eggs failed to hatch at 10°C and the larvae could not complete development at 15 and 35°C. The developmental times of each stage, survival rates of pre-adult, adult longevity, fecundities and oviposition days of M. exigua at 20, 25, 27 and 30°C were investigated using age-stage, two-sex life table. The total pre-adult development time decreased with the increase in temperature decreasing from 61.58 days at 20°C to 28.94 days at 30°C. The highest survival rate was observed at 25°C (73%). Male adult longevities were generally longer than that of females, except at 30°C. The highest mean fecundity, age-stage specific fecundity and age-specific fecundity peak values were all observed at 27°C. The maximum intrinsic rate of increase r and finite rate of increase λ were observed at 27°C, while the maximum net reproduction rate R0 was observed at 25°C. The longest mean generation time occurred at 20°C and the shortest at 27°C. These results provide better understanding on the development, reproduction and dynamic of M. exigua populations, their distribution, and might be utilized to forecast and manage M. exigua outbreaks in China.

[Effect of application of cow manure and green manure on corn yield and soil physical-chemical properties in land restoration area]. / 施用牛粪和绿肥对土地整治区玉米产量和土壤理化性质的影响.

The effects of cow manure and green manure on maize yield, soil respiration and soil physical-chemical properties in land restoration area was evaluated through field experiments. The results indicated that the maize yield and thousand-grain mass with cow manure were increased by 7.2%-29.9% and 2.5%-18.2%, respectively compared with the application of chemical fertilizer (CF), while the soil active organic carbon and organic matter contents of cow manure were 5.3%-34.6% and 8.0%-17.6% higher than that obtained in CF. The maize yield and thousand-grain mass were increased by 10.8%-15.6% and 4.5%-8.4% with application of green manure, respectively compared with CF. The content of active organic carbon in green manure was 14.1%-48.6% higher than that detected in CF. In the second year, the content of organic matter in green manure treatment was 7.2% higher than that of CF. The soil respiration rates under cow manure and green manure treatments increased by 20.0%-69.3% compared with CF. CF and green manure could improve the soil bulk density and increase the aggregate ratios of ＜0.01 mm and 0.05-1 mm fractions, respectively. On the other hand, the cow manure and green manure could decrease the soil total porosity and the capillary porosity. In conclusion, the application of cow manure and green manure in land restoration region could increase maize yield during the two consecutive seasons, which showed a positive response to improvement of soil physical-chemical properties.

[Nutrient spatial variability of tobacco soil restoration area and fertility suitability level evaluation].

By using geographic information system technology (GIS) and geostatistics methods, this paper studied the spatial variability of soil properties and available nutrients in the new regulation area units located in Qingjiangyuan modern tobacco agriculture science and technology park (Enshi, Hubei), suburb of Enshi City and the Baiyang base of Lichuan City, and further evaluation of the soil fertility suitability index (SFI) was carried out by use fuzzy mathematics. The results indicated that the effects of land restoration on the soil available phosphorus content variability and spatial distribution were very obvious, possibly due to the landform characteristics and restoration extent. The effect of land restoration on soil pH was small, however, serious soil acidification was detected in the soil sampled from Baiyang (pH < 5.5). Low SFI was found in 77.6%, 17.1% and 31.4% of the soils taken from the suburb, Baiyang and Qingjiangyuan, respectively. In conclusion, attentions should be paid on soil acidification in Baiyang, soil fertility and equalization in the suburb, and soil fertility in the region of Qingjiangyuan with low SFI.

Chemical constituents from Litsea greenmaniana / 中国中药杂志

A new compound (1), together with ten known compounds (2-11), have been isolated from the branch of Litsea greenmaniana by using various chromatographic techniques. Their structures were identified by spectroscopic data analysis as N-trans-3, 4-methylenecinnamoyl-3-methoxytyramine (1), N-trans-feruloyltyramine (2), N-cis-feruloyltyramine (3), (+)-sesamin (4), (+)-pinoresinol(5), cinnamophilin (6), dihydrodehydrodiconiferyl alcohol (7), benzoic acid (8), 4-hydroxy ethylbenzoate (9), p-hydroxybenzaldehyde(10), and 4-hydroxy-3-methoxy-benzyl alcohol (11). Compound 1 was a new compound, and compounds 2-11 were obtained from this plant for the first time.

Identification and field bioassay of the sex pheromone of Trichophysetis cretacea (Lepidoptera: Crambidae).

The jasmine bud borer Trichophysetis cretacea (Butler) (Lepidoptera Crambidae) is an important agricultural pest of jasmine flowers Jasminum sambac in China. The extract from the pheromone gland of the female moth was analyzed by gas chromatography coupled to mass spectroscopy (GC-MS). (Z)-11-hexadecenyl acetate (Z11-16:Ac), (Z)-11-hexadecenal (Z11-16:Ald),and (Z)-11-hexadecenol (Z11-16:OH) were identified as the probable sex pheromone components. The electroantennogram (EAG) bioassay confirmed the results from the chemical analysis. Field bioassays conducted in the late summer and fall in Quanwei, Sichuan, China, showed that the synthetic chemical blend of Z11-16:Ac, Z11-16:Ald, and Z11-16:OH was highly attractive to male T. cretacea moths, and none of the three components was attractive by itself. All three components were necessary and the ratio of the three was critical. The highest number of male moths was captured when the ratio of Z11-16:Ac: Z11-16:Ald:Z11-16:OH was 10:10:1 at a dosage per lure of 200 microg Z11-16:Ac. The binary mixture of 200 microg Z11-16:Ac and 25 microg Z11-16:OH captured a number of Nymphicula mesorphna (10.3 +/- 4.4). The results indicate that traps with synthetic pheromone lures can be used to monitor jasmine bud borer populations in the field and potentially to control this pest.

[An image acquisition & processing system of the wireless endoscope based on DSP].

This paper covers an image acquisition & processing system of the capsule-style endoscope. Images sent by the endoscope are compressed and encoded with the digital signal processor (DSP) saving data in HD into PC for analyzing and processing in the image browser workstation.