为明确关键栽培措施对菜籽油品质的影响,本研究以“湘杂油518”和“大地199”为材料,分别在武汉和兰州进行播期、密度及氮肥处理单因素试验,籽粒成熟后收获冷榨,测定菜籽油色泽、过氧化值、极性总酚及甾醇含量等关键品质指标,综合评价...为明确关键栽培措施对菜籽油品质的影响,本研究以“湘杂油518”和“大地199”为材料,分别在武汉和兰州进行播期、密度及氮肥处理单因素试验,籽粒成熟后收获冷榨,测定菜籽油色泽、过氧化值、极性总酚及甾醇含量等关键品质指标,综合评价各处理下菜籽油品质。结果表明:本试验条件下,播期、密度、氮肥均显著影响菜籽油关键品质指标,但各指标在两品种、两试验点间的变化规律不尽相同。两试点、两品种均在早播条件下菜籽油的油酸含量较高,且均随播期推迟,色泽加深,叶绿素含量升高,综合品质下降。两试点的湘杂油518品种在D2密度(4.5×10^(5)hm^(–2))下的菜籽油的酸价较低,极性总酚、总植物甾醇和总生育酚含量较高,综合品质较好。两试点的大地199品种则随密度增加菜籽油叶绿素含量增加,色泽加深,亚油酸含量降低,综合品质下降。两试点、两品种均在低氮下(120 kg hm^(–2))有较高的籽粒含油量和出油效率,且均随施氮量的增加菜籽油色泽加深,综合品质下降。主成分分析表明,播期对菜籽油综合品质的影响大于种植密度和施氮量处理,酸价、叶绿素、极性总酚、抗氧化能力和总植物甾醇是影响菜籽油的关键品质指标;相关性分析表明,籽粒含油量与出油效率显著正相关,叶绿素、类胡萝卜素与菜籽油色泽均呈显著正相关,极性总酚与抗氧化性显著正相关。综上所述,生产中适期早播、减少氮肥用量、降低种植密度,可提高压榨菜籽油品质。本试验结果可为高品质菜籽油优质原料的生产提供技术支撑。展开更多
为解决长江流域稻油茬口矛盾,提高冬闲田利用率,亟须迟播油菜(10月25日之后播种)配套技术研究。本研究以早熟品种‘华油杂137’为材料,在湖北武汉进行2年播种期(10月25日至11月15日间,各播种期间隔3 d,用S1~S8表示)和播种量(2.5、5.0、...为解决长江流域稻油茬口矛盾,提高冬闲田利用率,亟须迟播油菜(10月25日之后播种)配套技术研究。本研究以早熟品种‘华油杂137’为材料,在湖北武汉进行2年播种期(10月25日至11月15日间,各播种期间隔3 d,用S1~S8表示)和播种量(2.5、5.0、7.5、10.0和12.5 kg hm^(-2),用R1~R5表示)单因素试验,考察生育期、成苗动态、农艺性状、产量和倒伏指标,统计有效积温,通过线性回归和平滑曲线拟合分析,优化播种期和播种量的配置参数,为迟播油菜生产提供技术支撑。结果表明,(1)播种期推迟,迟播油菜的生育期缩短、根颈粗降低、分枝数减少、产量降低且茎秆倒伏指数增加;4个生育期中,苗期和花期有效积温与产量呈极显著正相关。(2)播种量增加,各生育期成苗数和收获密度提高,但生育期缩短、有效积温减少,角果层厚度降低、倒伏指数先降后增、产量呈先增后降趋势。(3)2年不同播种期产量数据回归分析表明,播种期推迟至S3~S4时,越冬前有效积温保持在317.1℃以上,苗期有效积温达401.1℃,终花35 d收获产量可达2700.0 kg hm^(-2),倒伏指数为1.5左右;2年不同播种量产量数据平滑曲线拟合分析表明,不同播种量下收获密度与产量呈抛物线关系,收获密度为64.2×10^(4)株hm^(-2)时终花35 d收获产量达峰值,为2948.5 kg hm^(-2),而倒伏指数为1.6。综上,配置7.5~10.0 kg hm^(-2)的播种量确保收获密度达64.2×10^(4)株hm^(-2),抢时播种确保冬前有效积温达317.1℃,可显著提高迟播油菜产量与抗倒性。展开更多
Background Solamargine (SM), a steroidal glycoalkaloid isolated from the Chinese herb Solanum incanum, has been shown to inhibit the growth of some cancer cell lines and induce significant apoptosis. However, the ef...Background Solamargine (SM), a steroidal glycoalkaloid isolated from the Chinese herb Solanum incanum, has been shown to inhibit the growth of some cancer cell lines and induce significant apoptosis. However, the effects of SM on multidrug-resistant (MDR) cells and the molecular mechanisms involved are poorly understood. The purpose of this study was to evaluate the anti-MDR effects of SM and the associated mechanisms in MDR K562/A02 cells. Methods The cytotoxicity of SM was measured by 3-(4,5-dimethylthiazol)-2,5-diphenyltetrazolium bromide (MTT) assay. The 14',6-diamidino-2-phenylindole (DAPi) nuclear staining and flow cytometry were used to detect SM-induced apoptosis. The mRNA expression of P-glycoprotein (P-gp) was investigated by real-time PCR (RT-PCR). Western blotting was used to determine the expression of Bcl-2, Bax, and actin. The changes in the morphology of actin were examined with immunofluorescence staining. Results MTT results showed that SM effectively killed the MDR sublines K562/A02, KB/VCR, and H460/paclitaxel (Taxol), and their parental cell lines K562, KB, and H460 to an equivalent or more sensitive degree. Based on the results by flow cytometry and immunostaining, the pro-apoptotic effects of SM were observed in MDR K562/A02 cells. Furthermore, the RT-PCR results showed that SM induced the downregulation of MDR1 mRNA. In addition, the expression of P-gp and actin was decreased in the SM-treated cells, as measured by western blotting and immunostaining. Conclusions These results demonstrate that SM effectively triggers apoptosis in MDR tumor cells, which is associated with actin disruption and downregulation of MDR1 expression. This compound may merit further investigation as a Potential therapeutic aaent that bvDasses the MDR mechanism for the treatment of MDR tumors.展开更多
The present study was designed to determine the effects of puerarin pre-treatment on the pharmacokinetics of the oral anticoagulant agent warfarin and the antiplatelet agent clopidogrel in rats. In the treatment group...The present study was designed to determine the effects of puerarin pre-treatment on the pharmacokinetics of the oral anticoagulant agent warfarin and the antiplatelet agent clopidogrel in rats. In the treatment group, rats was gavaged with warfarin or clopidogrel after repeated treatment with puerarin at intraperitoneal doses of 20, 60, or 200 mg·kg-1 for 7 days, while rats in the control group were administrated only with the same dose warfarin or clopidogrel. Plasma samples were obtained at the prescribed times and analyzed by liquid chromatography tandem mass spectrometry(LC-MS/MS). The results showed that rats treated with puerarin at all the test doses of 20, 60 and 200 mg·kg-1 were found to affect the pharmacokinetics of warfarin, but not clopidogrel, suggesting a potential herb-drug interaction between puerarin and warfarin.展开更多
In the present study, scapaundulin C(1), a new labdane diterpenoid, and four related known compounds scapaundulin A(2), 5?, 8?, 9?-trihydroxy-13E-labden-12-one(3), 5?, 8?-dihydroxy-13E-labden-12-one(4), and(13S)-15-hy...In the present study, scapaundulin C(1), a new labdane diterpenoid, and four related known compounds scapaundulin A(2), 5?, 8?, 9?-trihydroxy-13E-labden-12-one(3), 5?, 8?-dihydroxy-13E-labden-12-one(4), and(13S)-15-hydroxylabd-8(17)-en-19-oic acid(5), were isolated from the Chinese liverwort Scapania undulate(L.) Dum., using column chromatography. The structures of these compounds were determined on the basis of 1D- and 2D-NMR analyses. The acetylcholinesterase(Ach E) inhibitory activity was evaluated using a bioautographic TLC assay and the cytotoxic activity was evaluated by the MTT method. All the compounds were reported for the first time to exhibit moderate Ach E inhibitory activity with minimal inhibitory quantities ranging from 250 to 500 ng. All the compounds were tested for their cytotoxicity against five human tumor cell lines, A549, K562, A2780, Hela, and HT29, and compounds 3 and 4 exhibited moderate inhibitory effects on the growth of A2780 cells.展开更多
Antifungal drug resistance is a significant clinical problem, and antifungal agents that can evade resistance are urgently needed. In infective niches, resistant organisms often co-existed with sensitive ones, or a su...Antifungal drug resistance is a significant clinical problem, and antifungal agents that can evade resistance are urgently needed. In infective niches, resistant organisms often co-existed with sensitive ones, or a subpopulation of antibiotic-susceptible organisms may evolve into resistant ones during antibiotic treatment and eventually dominate the whole population. In this study, we established a co-culture assay in which an azole-resistant Candida albicans strain was mixed with a susceptible strain labeled with green fluorescent protein to mimic in vivo conditions and screen for antifungal drugs. Fluconazole was used as a positive control to verify the validity of this co-culture assay. Five natural molecules exhibited antifungal activity against both susceptible and resistant C. albicans. Two of these compounds, retigeric acid B(RAB) and riccardin D(RD), preferentially inhibited C. albicans strains in which the efflux pump MDR1 was activated. This selectivity was attributed to greater intracellular accumulation of the drugs in the resistant strains. Changes in sterol and lipid compositions were observed in the resistant strains compared to the susceptible strain, and might increase cell permeability to RAB and RD. In addition, RAB and RD interfered with the sterol pathway, further aggregating the decrease in ergosterol in the sterol synthesis pathway in the MDR1-activated strains. Our findings here provide an alternative for combating resistant pathogenic fungi.展开更多
The spread of antibiotic-resistant bacteria and exhausted drug leads render some infections untreatable now and in the future.To deal with these“new challenges”,scientists tend to re-pick up“old antibiotics”.Fusid...The spread of antibiotic-resistant bacteria and exhausted drug leads render some infections untreatable now and in the future.To deal with these“new challenges”,scientists tend to re-pick up“old antibiotics”.Fusidane-type antibiotics have been known for nearly 80 years as potent antibacterial agents against gram-positive bacteria,especially Staphylococci,and represent the only triterpene-derived antibiotic class in clinical setting.These attractive characteristics have drawn renewed attention on fusidane-type antibiotics in recent decades.Isolation,characterization,biological evaluation,as well as chemical modifications of fusidane-type antibiotics are increasingly being reported.Combinatorial biosynthesis of this type of antibiotics has been successfully utilized not only for elucidating the biosynthetic pathways,but also for expanding their structural diversity.Some isolated and synthetic compounds exhibit comparable or even more potent biological activity than fusidic acid.This review provides an overview of progress on the studies of structure and biology of fusidane-type antibiotics from 1943 to April 2021.The informative structure-activity relationship is also highlighted.展开更多
Objective To establish a quality control protocol based on microscopic, TLC, and HPLC methods, and to verify the optimal harvesting time for the leaves of Malus hupehensis(LMH). Methods The LMH were pulverized into po...Objective To establish a quality control protocol based on microscopic, TLC, and HPLC methods, and to verify the optimal harvesting time for the leaves of Malus hupehensis(LMH). Methods The LMH were pulverized into powder for microscopic identification or TLC and HPLC analysis after ultrasonic extraction with methanol. Seasonal variations of the phlorizin content and average leaf weight were determined by HPLC analysis and weighing up the leaves collected from May to October. Results Microscopic and macromorphologic characteristics have been described for the leaf identification. A qualitative TLC assay and a quantitative HPLC method have been established for the quality control of LMH. Phlorizin was selected as a reference marker, which resolved at Rf 0.53 in TLC assay and at 14.0 min in HPLC assay. The content of phlorizin decreased gradually from 17.0% in leaves collected in May to 7.5% in October. The average leaf weight reached the level of 0.6 g in August and maintained until its falling.Conclusion These methods are simple, selective, accurate, and reliable for the quality control of LMH. The period from late August to early September is suggested as the optimal harvesting time of the LMH.展开更多
文摘为明确关键栽培措施对菜籽油品质的影响,本研究以“湘杂油518”和“大地199”为材料,分别在武汉和兰州进行播期、密度及氮肥处理单因素试验,籽粒成熟后收获冷榨,测定菜籽油色泽、过氧化值、极性总酚及甾醇含量等关键品质指标,综合评价各处理下菜籽油品质。结果表明:本试验条件下,播期、密度、氮肥均显著影响菜籽油关键品质指标,但各指标在两品种、两试验点间的变化规律不尽相同。两试点、两品种均在早播条件下菜籽油的油酸含量较高,且均随播期推迟,色泽加深,叶绿素含量升高,综合品质下降。两试点的湘杂油518品种在D2密度(4.5×10^(5)hm^(–2))下的菜籽油的酸价较低,极性总酚、总植物甾醇和总生育酚含量较高,综合品质较好。两试点的大地199品种则随密度增加菜籽油叶绿素含量增加,色泽加深,亚油酸含量降低,综合品质下降。两试点、两品种均在低氮下(120 kg hm^(–2))有较高的籽粒含油量和出油效率,且均随施氮量的增加菜籽油色泽加深,综合品质下降。主成分分析表明,播期对菜籽油综合品质的影响大于种植密度和施氮量处理,酸价、叶绿素、极性总酚、抗氧化能力和总植物甾醇是影响菜籽油的关键品质指标;相关性分析表明,籽粒含油量与出油效率显著正相关,叶绿素、类胡萝卜素与菜籽油色泽均呈显著正相关,极性总酚与抗氧化性显著正相关。综上所述,生产中适期早播、减少氮肥用量、降低种植密度,可提高压榨菜籽油品质。本试验结果可为高品质菜籽油优质原料的生产提供技术支撑。
文摘为解决长江流域稻油茬口矛盾,提高冬闲田利用率,亟须迟播油菜(10月25日之后播种)配套技术研究。本研究以早熟品种‘华油杂137’为材料,在湖北武汉进行2年播种期(10月25日至11月15日间,各播种期间隔3 d,用S1~S8表示)和播种量(2.5、5.0、7.5、10.0和12.5 kg hm^(-2),用R1~R5表示)单因素试验,考察生育期、成苗动态、农艺性状、产量和倒伏指标,统计有效积温,通过线性回归和平滑曲线拟合分析,优化播种期和播种量的配置参数,为迟播油菜生产提供技术支撑。结果表明,(1)播种期推迟,迟播油菜的生育期缩短、根颈粗降低、分枝数减少、产量降低且茎秆倒伏指数增加;4个生育期中,苗期和花期有效积温与产量呈极显著正相关。(2)播种量增加,各生育期成苗数和收获密度提高,但生育期缩短、有效积温减少,角果层厚度降低、倒伏指数先降后增、产量呈先增后降趋势。(3)2年不同播种期产量数据回归分析表明,播种期推迟至S3~S4时,越冬前有效积温保持在317.1℃以上,苗期有效积温达401.1℃,终花35 d收获产量可达2700.0 kg hm^(-2),倒伏指数为1.5左右;2年不同播种量产量数据平滑曲线拟合分析表明,不同播种量下收获密度与产量呈抛物线关系,收获密度为64.2×10^(4)株hm^(-2)时终花35 d收获产量达峰值,为2948.5 kg hm^(-2),而倒伏指数为1.6。综上,配置7.5~10.0 kg hm^(-2)的播种量确保收获密度达64.2×10^(4)株hm^(-2),抢时播种确保冬前有效积温达317.1℃,可显著提高迟播油菜产量与抗倒性。
基金This work was supported by the grants from the National Natural Science Foundation of China (No. 81072660), the Shandong Provincial Natural Science Foundation (No. ZR2009CMI22) and the Shandong Provincial Doctoral Foundation (No. BS2009YY016).
文摘Background Solamargine (SM), a steroidal glycoalkaloid isolated from the Chinese herb Solanum incanum, has been shown to inhibit the growth of some cancer cell lines and induce significant apoptosis. However, the effects of SM on multidrug-resistant (MDR) cells and the molecular mechanisms involved are poorly understood. The purpose of this study was to evaluate the anti-MDR effects of SM and the associated mechanisms in MDR K562/A02 cells. Methods The cytotoxicity of SM was measured by 3-(4,5-dimethylthiazol)-2,5-diphenyltetrazolium bromide (MTT) assay. The 14',6-diamidino-2-phenylindole (DAPi) nuclear staining and flow cytometry were used to detect SM-induced apoptosis. The mRNA expression of P-glycoprotein (P-gp) was investigated by real-time PCR (RT-PCR). Western blotting was used to determine the expression of Bcl-2, Bax, and actin. The changes in the morphology of actin were examined with immunofluorescence staining. Results MTT results showed that SM effectively killed the MDR sublines K562/A02, KB/VCR, and H460/paclitaxel (Taxol), and their parental cell lines K562, KB, and H460 to an equivalent or more sensitive degree. Based on the results by flow cytometry and immunostaining, the pro-apoptotic effects of SM were observed in MDR K562/A02 cells. Furthermore, the RT-PCR results showed that SM induced the downregulation of MDR1 mRNA. In addition, the expression of P-gp and actin was decreased in the SM-treated cells, as measured by western blotting and immunostaining. Conclusions These results demonstrate that SM effectively triggers apoptosis in MDR tumor cells, which is associated with actin disruption and downregulation of MDR1 expression. This compound may merit further investigation as a Potential therapeutic aaent that bvDasses the MDR mechanism for the treatment of MDR tumors.
基金supported by the Natural Science Foundation of China(No.31101241)the Independent Innovation Foundation of Shandong University(IIFSDU,No.2012TS163)
文摘The present study was designed to determine the effects of puerarin pre-treatment on the pharmacokinetics of the oral anticoagulant agent warfarin and the antiplatelet agent clopidogrel in rats. In the treatment group, rats was gavaged with warfarin or clopidogrel after repeated treatment with puerarin at intraperitoneal doses of 20, 60, or 200 mg·kg-1 for 7 days, while rats in the control group were administrated only with the same dose warfarin or clopidogrel. Plasma samples were obtained at the prescribed times and analyzed by liquid chromatography tandem mass spectrometry(LC-MS/MS). The results showed that rats treated with puerarin at all the test doses of 20, 60 and 200 mg·kg-1 were found to affect the pharmacokinetics of warfarin, but not clopidogrel, suggesting a potential herb-drug interaction between puerarin and warfarin.
基金financially supported by National Natural Science Foundation of China(No.30925038)
文摘In the present study, scapaundulin C(1), a new labdane diterpenoid, and four related known compounds scapaundulin A(2), 5?, 8?, 9?-trihydroxy-13E-labden-12-one(3), 5?, 8?-dihydroxy-13E-labden-12-one(4), and(13S)-15-hydroxylabd-8(17)-en-19-oic acid(5), were isolated from the Chinese liverwort Scapania undulate(L.) Dum., using column chromatography. The structures of these compounds were determined on the basis of 1D- and 2D-NMR analyses. The acetylcholinesterase(Ach E) inhibitory activity was evaluated using a bioautographic TLC assay and the cytotoxic activity was evaluated by the MTT method. All the compounds were reported for the first time to exhibit moderate Ach E inhibitory activity with minimal inhibitory quantities ranging from 250 to 500 ng. All the compounds were tested for their cytotoxicity against five human tumor cell lines, A549, K562, A2780, Hela, and HT29, and compounds 3 and 4 exhibited moderate inhibitory effects on the growth of A2780 cells.
基金funded by the National Natural Science Foundation(Nos.81630093,81773786,81402804)the Young Scholars Program of Shandong University
文摘Antifungal drug resistance is a significant clinical problem, and antifungal agents that can evade resistance are urgently needed. In infective niches, resistant organisms often co-existed with sensitive ones, or a subpopulation of antibiotic-susceptible organisms may evolve into resistant ones during antibiotic treatment and eventually dominate the whole population. In this study, we established a co-culture assay in which an azole-resistant Candida albicans strain was mixed with a susceptible strain labeled with green fluorescent protein to mimic in vivo conditions and screen for antifungal drugs. Fluconazole was used as a positive control to verify the validity of this co-culture assay. Five natural molecules exhibited antifungal activity against both susceptible and resistant C. albicans. Two of these compounds, retigeric acid B(RAB) and riccardin D(RD), preferentially inhibited C. albicans strains in which the efflux pump MDR1 was activated. This selectivity was attributed to greater intracellular accumulation of the drugs in the resistant strains. Changes in sterol and lipid compositions were observed in the resistant strains compared to the susceptible strain, and might increase cell permeability to RAB and RD. In addition, RAB and RD interfered with the sterol pathway, further aggregating the decrease in ergosterol in the sterol synthesis pathway in the MDR1-activated strains. Our findings here provide an alternative for combating resistant pathogenic fungi.
基金supported by the National Natural Science Foundation of China(Nos.81903494 and 81903483)。
文摘The spread of antibiotic-resistant bacteria and exhausted drug leads render some infections untreatable now and in the future.To deal with these“new challenges”,scientists tend to re-pick up“old antibiotics”.Fusidane-type antibiotics have been known for nearly 80 years as potent antibacterial agents against gram-positive bacteria,especially Staphylococci,and represent the only triterpene-derived antibiotic class in clinical setting.These attractive characteristics have drawn renewed attention on fusidane-type antibiotics in recent decades.Isolation,characterization,biological evaluation,as well as chemical modifications of fusidane-type antibiotics are increasingly being reported.Combinatorial biosynthesis of this type of antibiotics has been successfully utilized not only for elucidating the biosynthetic pathways,but also for expanding their structural diversity.Some isolated and synthetic compounds exhibit comparable or even more potent biological activity than fusidic acid.This review provides an overview of progress on the studies of structure and biology of fusidane-type antibiotics from 1943 to April 2021.The informative structure-activity relationship is also highlighted.
基金Science and Technology Development Program of Shandong Province(2011GSF11909)
文摘Objective To establish a quality control protocol based on microscopic, TLC, and HPLC methods, and to verify the optimal harvesting time for the leaves of Malus hupehensis(LMH). Methods The LMH were pulverized into powder for microscopic identification or TLC and HPLC analysis after ultrasonic extraction with methanol. Seasonal variations of the phlorizin content and average leaf weight were determined by HPLC analysis and weighing up the leaves collected from May to October. Results Microscopic and macromorphologic characteristics have been described for the leaf identification. A qualitative TLC assay and a quantitative HPLC method have been established for the quality control of LMH. Phlorizin was selected as a reference marker, which resolved at Rf 0.53 in TLC assay and at 14.0 min in HPLC assay. The content of phlorizin decreased gradually from 17.0% in leaves collected in May to 7.5% in October. The average leaf weight reached the level of 0.6 g in August and maintained until its falling.Conclusion These methods are simple, selective, accurate, and reliable for the quality control of LMH. The period from late August to early September is suggested as the optimal harvesting time of the LMH.