Synergistic interaction of physcion and chrysophanol on plant powdery mildew

The extract of the plant Rheum officinale Baill, mainly containing the anthraquinones physcion and chrysophanol, is highly active against plant powdery mildew. Experiments were conducted in the laboratory and greenhouse to determine the interaction of the two compounds on cucumber powdery mildew [Sphaerotheca fuliginea (Schlecht.) Poll] and on wheat powdery mildew [Blumeria graminis (DC.) Speer f. sp. tritici Marchal]. Physcion was much more bioactive than chrysophanol against these powdery mildews. There was a significant synergistic interaction between the two compounds on the diseases when the ratios of physcion to chrysophanol ranged from 1:9 to 5:5. The synergistic degree increased with increase in the chrysophanol proportion in the combination. The findings indicate that, in order to ensure constant efficacy of the extract on the disease, both the contents and the proportion of the main active ingredients physcion and chrysophanol have to be determined.     

大黄素甲醚、大黄酸的研究进展

2014年世界卫生组织首份全球抗菌素耐药报告显示全世界面临严重的公共卫生威胁,2021年农业农村部制定了《全国兽用抗菌药使用减量化行动方案》(2021-2025),从国家层面实施综合治理策略和措施,鼓励替代抗菌药物的研制和创新。大黄素甲醚、大黄酸作为植物蒽醌类有效成分,具有抗微生物、抗炎、抗氧化、神经保护等药理作用,但对其抗菌、抗病毒、抗炎症相关的作用机制和产业化工艺缺少详细报道。本文对国内外已经发表的专利文献、期刊文献进行综述,总结其抗菌、抗病毒、抗炎作用机制及其生产工艺,以期为进一步开发利用提供科学支撑。     

新型植物源农药0.5%大黄素甲醚水剂对黄瓜白粉病菌的毒力测定及田间药效

0.5%大黄素甲醚水剂是湖北省农科院植保土肥所和内蒙古清源保生物科技有限公司联合创制的一种新颖的植物源杀菌剂,其化学结构式为1,8-二羟基-3-甲氧基-6-甲基蒽醌。室内孢子萌发抑制试验结果表明,大黄素甲醚对黄瓜白粉病菌孢子萌发的抑制中浓度EC50为0.37μg/mL;田间药效试验结果表明,0.5%大黄素甲醚水剂对黄瓜白粉病菌具有良好的保护和防治效果,有效成分用量18~45 g/hm2的防治效果明显高于15%三唑酮可湿性粉剂135 g/hm2的防效。     

大黄素甲醚在黄瓜和土壤中的残留分析方法

建立了用反相高效液相色谱的方法,分析黄瓜和土壤中大黄素甲醚的残留量。样品以乙酸乙酯或乙酸乙酯与甲醇的体积比为1∶1的混合液提取,三氯甲烷萃取净化,液相色谱FLD检测器测定。该方法条件下检测器对大黄素甲醚的最小检出量为8.6×10-11g,黄瓜和土壤中最低检出浓度均为0.01 mg/kg。大黄素甲醚在0.05~1.0 mg/kg添加浓度范围内的试验表明,土壤和黄瓜样品中回收率分别为84.1%~92.2%和84.2%~88.6%,变异系数小于2.72%和2.30%。     

不同粒径大黄中有效成分溶出度对比

目的：测定不同粒径大黄中芦荟大黄素、大黄酸、大黄素、大黄酚、大黄素甲醚的溶出量。方法：用高效液相色谱法测定其溶出量。结果：随着粒径变细,其溶出量都在增加,但粉碎到300目以上时,其溶出量反而下降。结论：大黄超微粉的应用以200目效果最好。     

复方首乌补液大黄素及大黄素甲醚含量的测定方法

为寻求同时测定复方首乌补液中大黄素和大黄素甲醚含量的测定方法,采用高效液相色谱法,建立了该测定方法。结果表明:大黄素和大黄素甲醚含量分别在0.021 6～0.432μg(r=0.999 9)和0.011 4～0.228μg(r=0.999 9)范围内呈良好的线性关系,平均回收率分别为98.50%(RSD=1.32%)和99.13%(RSD=1.89%)。该检测方法简捷、准确、重现性好,可用于复方首乌补液的质量控制检测。     

Physcion,a natural anthraquinone derivative,enhances the gene expression of leaf‐specific thionin of barley against Blumeria graminis

BACKGROUND: Physcion is a key active ingredient of the ethanol extract from roots of Chinese rhubarb (Rheum officinale Baill.) that has been commercialised in China for controlling powdery mildews. The biological mechanism of action of physcion against the barley powdery mildew pathogen was studied using bioassay and microarray methods. RESULTS: Bioassay indicated that physcion did not directly affect conidial germination of Blumeria graminis Speer f. sp. hordei Marchal, but significantly inhibited conidial germination in vivo. Challenge inoculation indicated that physcion induced localised resistance rather than systemic resistance against powdery mildew. Gene expression profiling of physcion‐treated barley leaves detected four upregulated and five downregulated genes (ratio ≥ 2.0 and P‐value < 0.05) by using an Affymetrix Barley GeneChip. The five upregulated probe sequences blasted to the same barley leaf‐specific thionin gene, with significant changes varying from 4.26 to 19.91‐fold. All downregulated genes were defence‐related, linked to peroxidase, oxalate oxidase, bsi1 protein and a pathogenesis‐related protein. These changes varied from ? 2.34 to ? 2.96. Quantitative real‐time PCR data confirmed that physcion enhanced the gene expression of leaf‐specific thionin of barley. CONCLUSION: Results indicated that physcion controls powdery mildew mainly through changing the expression of defence‐related genes, and especially enhancing expression of leaf‐specific thionin in barley leaves. Copyright © 2010 Society of Chemical Industry     

Mitochondrial Targeting in an Anti-Austerity Approach Involving Bioactive Metabolites Isolated from the Marine-Derived Fungus Aspergillus sp.

The tumor microenvironment is a nutrient-deficient region that alters the cancer cell phenotype to aggravate cancer pathology. The ability of cancer cells to tolerate nutrient starvation is referred to as austerity. Compounds that preferentially target cancer cells growing under nutrient-deficient conditions are being employed in anti-austerity approaches in anticancer drug discovery. Therefore, in this study, we investigated physcion (1) and 2-(2′,3-epoxy-1′,3′,5′-heptatrienyl)-6-hydroxy-5-(3-methyl-2-butenyl) benzaldehyde (2) obtained from a culture extract of the marine-derived fungus Aspergillus species (sp.), which were isolated from an unidentified marine sponge, as anti-austerity agents. The chemical structures of 1 and 2 were determined via spectroscopic analysis and comparison with authentic spectral data. Compounds 1 and 2 exhibited selective cytotoxicity against human pancreatic carcinoma PANC-1 cells cultured under glucose-deficient conditions, with IC₅₀ values of 6.0 and 1.7 µM, respectively. Compound 2 showed higher selective growth-inhibitory activity (505-fold higher) under glucose-deficient conditions than under general culture conditions. Further analysis of the mechanism underlying the anti-austerity activity of compounds 1 and 2 against glucose-starved PANC-1 cells suggested that they inhibited the mitochondrial electron transport chain.