Objecive: To explore the effect of gibberellic acid(GA_3) and its inhibitor paclobutrazol(PBZ)on chemical composition and their pharmacological effects on Andrographis paniculata(Burm.f.) Wall. ex Nees, and to clarify...Objecive: To explore the effect of gibberellic acid(GA_3) and its inhibitor paclobutrazol(PBZ)on chemical composition and their pharmacological effects on Andrographis paniculata(Burm.f.) Wall. ex Nees, and to clarify action mode of andrographolide.Methods: The chemical composition was extracted by sequential extraction with hexane, dichloromethane, ethyl acetate and methanol, respectively. Andrographolide and its derivatives were evaluated by HPLC. Moreover, the metabolic profiling was analyzed by GC-MS. Inhibitory effect of crude extracts was tested against Staphylococcus aureus using agar well diffusion method. Mode of action was tested against mutant yeast by spotting assay. Andrographolide were tested for their mode of action against eukaryotes. Rsults: Among different solvents, dichloromethane gave the highest yield of crude(3.58% DW), with the highest andrographolide content(8.3 mg/g DW). The effect of plant hormone(10 mg/L GA_3 or PBZ) on phytochemical variations and bioactivity of Andrographis paniculata was demonstrated. It was found that PBZ promoted sesquiterpene compounds about 3.5 times over than GA_3 treatment. But inhibitory effect of extracts against Staphylococcus aureus was highest in GA_3 treated plants; andrographolide and 14-deoxy-11,12-didehydroandrographolide contents were significantly higher than those of water or PBZ. It was found that there were 11 strains involving in ergosterol biosynthesis, V-ATPase activity and homeostasis, and superoxide detoxification process. In this regard, andrographolide might cause the damage on the lipid bilayer of yeast cell and plasma membrane by interfering ergosterol biosynthesis.Conclusions: It is found that GA_3 promotes andrographolide and 14-deoxy-11,12-didehydroandrographolide content while PBZ promotes sesquiterpene content. Andrographolide might cause the damage on the lipid bilayer of yeast cell and plasma membrane by interfering ergosterol biosynthesis. It might also affect mitochondria electron transport chain, leading to the occurrence of ROS, which can further harm cell organelles. However, the library screening is the first step to investigate mode of action of andrographolide.展开更多
To study the pesticide effect, action mode, structure-activity relationships (SARs) of anthranilic diamide insecticide and screen highly active pesticides, novel anthranilic diamide derivatives were synthesized.Bioass...To study the pesticide effect, action mode, structure-activity relationships (SARs) of anthranilic diamide insecticide and screen highly active pesticides, novel anthranilic diamide derivatives were synthesized.Bioassays indicated that all of the title compounds displayed 100% mortality against diamondback moth and oriental armyworm at 100 mg/L, among which 12 v and 12 w showed 100% insecticidal acitvity at 5 mg/L. Surprisingly compound 12 w exhibited better insecticidal acitvity than commercialized chlorantraniliprole against Pyrausta nubilalis (0.1 mg/L) and Cnaphalocrocis Medinalis (2 mg/L). 3 D-QSAR and SARs statistical analysis revealed that title compounds with R^2 fixed as methoxy had the highest probability possessing high activity. The calcium fluorescence measurements on neurons revealed that E series compounds containing pyrazinyl may have a molecular target different from caffeine on ryanodine receptors rather than the voltage-gated calcium channel present on cytomembran.展开更多
Common beans are affected by many insect pests such as bean leaf beetle, aphids, legume pod borer and bean beetles. Traditional and cultural practices such as site selection, crop rotation, intercropping and seed sele...Common beans are affected by many insect pests such as bean leaf beetle, aphids, legume pod borer and bean beetles. Traditional and cultural practices such as site selection, crop rotation, intercropping and seed selection, sowing date are used to reduce the infestation of insect pests of common beans in the field and in storage rooms. Natural enemies such as predators, parasitoids and pathogens can control the insect pests. Synthetic pesticides such as cypermethion, carbaryl, and lambda-cyhalothrin have reported to be effective, but are toxic to people, destroy natural enemies and contaminate the environment. Botanical pesticides are the promising alternatives. This review paper explains toxicity, persistence and mode of actions of active ingredients of botanical pesticides. Rotenone from T. vogelii has the oral lethal dose (LD<sub>50</sub>) of 132 - 1500 mg/kg to mammals. It delays the electron transport chain in mitochondria of the insects and limits the cellular energy production. Azadirachtin is antifeedant and growth disruptor of insects. It has low toxicity to mammals. The oral LD<sub>50</sub> in mammals is greater than 3540 mg/kg. Azadirachtin displays strong effects on chemoreceptors of the insects. Pyrethrins are axonic poisons and have repellent effects to insects. It is less toxic to mammals with the LD<sub>50</sub> of about 1500 mg/Kg. It attacks the nervous systems of insects. Sesquiterpene lactones from T. diversifolia, Pentacyclic triterpenoids from Lantana camara, Vernodalin, Vernodalol and Epivernodalol from V. amygdalina have repellent and feeding deterrents chemicals which discourage the insects from feeding the crop. Most active ingredients of botanical pesticides have short life span in the environment.展开更多
Safety and practicability of the HELP procedure
Compared to standard plasma exchange, HELP-apheresis is much better tolerated, primarily be-cause heparin rather than citrate is used for anti-coagulation and t... Safety and practicability of the HELP procedure
Compared to standard plasma exchange, HELP-apheresis is much better tolerated, primarily be-cause heparin rather than citrate is used for anti-coagulation and therefore problems due to hypercalce-mia do not play a role.……展开更多
基金financially supported by Agricultural Research Development Agency(Public Organization)or"ARDA"(Grant No.CRP6005020350)
文摘Objecive: To explore the effect of gibberellic acid(GA_3) and its inhibitor paclobutrazol(PBZ)on chemical composition and their pharmacological effects on Andrographis paniculata(Burm.f.) Wall. ex Nees, and to clarify action mode of andrographolide.Methods: The chemical composition was extracted by sequential extraction with hexane, dichloromethane, ethyl acetate and methanol, respectively. Andrographolide and its derivatives were evaluated by HPLC. Moreover, the metabolic profiling was analyzed by GC-MS. Inhibitory effect of crude extracts was tested against Staphylococcus aureus using agar well diffusion method. Mode of action was tested against mutant yeast by spotting assay. Andrographolide were tested for their mode of action against eukaryotes. Rsults: Among different solvents, dichloromethane gave the highest yield of crude(3.58% DW), with the highest andrographolide content(8.3 mg/g DW). The effect of plant hormone(10 mg/L GA_3 or PBZ) on phytochemical variations and bioactivity of Andrographis paniculata was demonstrated. It was found that PBZ promoted sesquiterpene compounds about 3.5 times over than GA_3 treatment. But inhibitory effect of extracts against Staphylococcus aureus was highest in GA_3 treated plants; andrographolide and 14-deoxy-11,12-didehydroandrographolide contents were significantly higher than those of water or PBZ. It was found that there were 11 strains involving in ergosterol biosynthesis, V-ATPase activity and homeostasis, and superoxide detoxification process. In this regard, andrographolide might cause the damage on the lipid bilayer of yeast cell and plasma membrane by interfering ergosterol biosynthesis.Conclusions: It is found that GA_3 promotes andrographolide and 14-deoxy-11,12-didehydroandrographolide content while PBZ promotes sesquiterpene content. Andrographolide might cause the damage on the lipid bilayer of yeast cell and plasma membrane by interfering ergosterol biosynthesis. It might also affect mitochondria electron transport chain, leading to the occurrence of ROS, which can further harm cell organelles. However, the library screening is the first step to investigate mode of action of andrographolide.
基金supported by the National Natural Science Foundation of China(Nos. 20772060 and 21172114)
文摘To study the pesticide effect, action mode, structure-activity relationships (SARs) of anthranilic diamide insecticide and screen highly active pesticides, novel anthranilic diamide derivatives were synthesized.Bioassays indicated that all of the title compounds displayed 100% mortality against diamondback moth and oriental armyworm at 100 mg/L, among which 12 v and 12 w showed 100% insecticidal acitvity at 5 mg/L. Surprisingly compound 12 w exhibited better insecticidal acitvity than commercialized chlorantraniliprole against Pyrausta nubilalis (0.1 mg/L) and Cnaphalocrocis Medinalis (2 mg/L). 3 D-QSAR and SARs statistical analysis revealed that title compounds with R^2 fixed as methoxy had the highest probability possessing high activity. The calcium fluorescence measurements on neurons revealed that E series compounds containing pyrazinyl may have a molecular target different from caffeine on ryanodine receptors rather than the voltage-gated calcium channel present on cytomembran.
文摘Common beans are affected by many insect pests such as bean leaf beetle, aphids, legume pod borer and bean beetles. Traditional and cultural practices such as site selection, crop rotation, intercropping and seed selection, sowing date are used to reduce the infestation of insect pests of common beans in the field and in storage rooms. Natural enemies such as predators, parasitoids and pathogens can control the insect pests. Synthetic pesticides such as cypermethion, carbaryl, and lambda-cyhalothrin have reported to be effective, but are toxic to people, destroy natural enemies and contaminate the environment. Botanical pesticides are the promising alternatives. This review paper explains toxicity, persistence and mode of actions of active ingredients of botanical pesticides. Rotenone from T. vogelii has the oral lethal dose (LD<sub>50</sub>) of 132 - 1500 mg/kg to mammals. It delays the electron transport chain in mitochondria of the insects and limits the cellular energy production. Azadirachtin is antifeedant and growth disruptor of insects. It has low toxicity to mammals. The oral LD<sub>50</sub> in mammals is greater than 3540 mg/kg. Azadirachtin displays strong effects on chemoreceptors of the insects. Pyrethrins are axonic poisons and have repellent effects to insects. It is less toxic to mammals with the LD<sub>50</sub> of about 1500 mg/Kg. It attacks the nervous systems of insects. Sesquiterpene lactones from T. diversifolia, Pentacyclic triterpenoids from Lantana camara, Vernodalin, Vernodalol and Epivernodalol from V. amygdalina have repellent and feeding deterrents chemicals which discourage the insects from feeding the crop. Most active ingredients of botanical pesticides have short life span in the environment.
文摘 Safety and practicability of the HELP procedure
Compared to standard plasma exchange, HELP-apheresis is much better tolerated, primarily be-cause heparin rather than citrate is used for anti-coagulation and therefore problems due to hypercalce-mia do not play a role.……
