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2021 ◽  
Author(s):  
Yongchun Li ◽  
Hui Zhang ◽  
Shanshan Chen ◽  
Liutao Zhao ◽  
Jie Wu ◽  
...  

Abstract Qing Hao Gan Cao (QHGC), a Chinese medicinal formula containing Artemisia annua and Glycyrrhizae Radix et Rhizoma, has been used to treat sunstroke and as an antiviral agent for more than 800 years. It has not previously been subject to a toxicological safety evaluation in acute and subacute (28 days) studies. Therefore, the acute and subacute toxicity of an aqueous extract of QHGC were evaluated in vivo. For the QHGC preparation, the botanical raw materials were crushed into pieces and mixed in the ratio of 10:1 in distilled water for 12 h, then boiling three times for 2 h each time. The three decoctions were mixed and filtered, then spray-dried with hot air at 160°C for 30 min, and stored at room temperature. For the acute toxicity test, 72.0 g/kg of QHGC extract was administered by gavage to male and female mice. Body weight, general observations, and autopsy results were recorded. No mortality or toxicity signs were observed during the studies. For the subacute toxicity test, 4.0, 8.0, or 16.0 g/kg/day of QHGC extract was administered to rats for 28 days. General observations and mortality, body weight, biochemical and hematological parameters, organ weight, and pathological morphology were analyzed. The acute and subacute toxicity studies did not show significant changes in body weight, general observations, hematology and biochemical parameters, organ weight, and liver, spleen, stomach, duodenum, testis, ovary, lung, heart, and kidney histopathological analyses. The consumption of QHGC aqueous extract can be considered safe within the conditions of this study.


2020 ◽  
Author(s):  
yuping zhao ◽  
Xiao-bo Zhang ◽  
Hai-yu Xu ◽  
Ling Wang ◽  
Lu-qi Huang

Abstract Background: Artemisinin is widely used to treat malaria, but the antimalarial mechanism and coordinative interactions governing the actions of artemisinin, scopoletin, arteannuin B and artemisinic acid have not been elucidated. Methods: Based on the existence of antimalarial drugs, the antimalaria targets of artemisinin, scopoletin, arteannuin B and artemisinic acid were investigated by molecular docking using the similarity theory of chemical structure, and the antimalaria mechanism of scopoletin and its coordinative antimalaria interactions with the other three ingredients of the mixture were subsequently examined. Results: Using the text information excavation method, the relevant proteins involved in the antimalarial effect of artemisinin were IL-6, ACHE, PC3, IPOB, CYC, TNF-α, UGT1A9, CASP3, XDH, IL-1β, VEGF, CAT, CREB, AMPK, UGT1A6, ADR, MAPK, COX2, LB24AB and CYP450. The relevant proteins involved in the antimalarial effect of scopoletin were TNF-α, PI3K, IL-8, IL- 6, VEGF, IL-1β, MAPK, CD4, SP2, CTNNB, CASP3, PRO1400, IgE, IL-4, ICAM1, p38, STAT3, TLR4 and API4. However, arteannuin B and artemisinic acid had little relevance to the abovementioned proteins. The interaction property between TNF-α and Artemisia annua was that the effect of the mixture of artemisinin, scopoletin, arteannuin B and artemisinic acid was greater than that of artemisinin alone, and the synergistic effect of the four elements was considered beneficial to the progress of antimalarial treatment. Conclusion: The antimalarial targets of Artemisia annua ingredients were examined using data mining methods, and the antimalarial effect of scopoletin may be related to TNF. The combined application of the four elements achieved the same antimalarial effect and reduced the clinical use of artemisinin and scopoletin.


2020 ◽  
Author(s):  
yuping zhao ◽  
Xiao-bo Zhang ◽  
Hai-yu Xu ◽  
Ling Wang ◽  
Lu-qi Huang

Abstract Background Artemisinin is widely used to treat malaria, but the antimalarial mechanism and coordinative interactions governing the actions of artemisinin, scopoletin, arteannuin B and artemisinic acid have not been elucidated. Methods Based on the existence of antimalarial drugs, the antimalaria targets of artemisinin, scopoletin, arteannuin B and artemisinic acid were investigated by molecular docking using the similarity theory of chemical structure, and the antimalaria mechanism of scopoletin and its coordinative antimalaria interactions with the other three ingredients of the mixture were subsequently explored. Results Using the text information excavation method, the relevant proteins involved in the antimalarial effect of artemisinin were determined to be IL-6, ACHE, PC3, IPOB, CYC, TNF-α, UGT1A9, CASP3, XDH, IL-1β, VEGF, CAT, CREB, AMPK, UGT1A6, ADR, MAPK, COX2, LB24AB and CYP450. Meanwhile, the relevant proteins involved in the antimalarial effect of scopoletin were TNF-α, PI3K, IL-8, IL- 6, VEGF, IL-1β, MAPK, CD4, SP2, CTNNB, CASP3, PRO1400, IgE, IL-4, ICAM1, p38, STAT3, TLR4 and API4. However, arteannuin B and artemisinic acid had little relevance to the abovementioned proteins. The interaction property between TNF-α and Artemisia annua was that the effect of the mixture of artemisinin, scopoletin, arteannuin B and artemisinic acid was greater than that of artemisinin, and the synergistic effect of the four elements was considered to be beneficial to the progress of antimalarial treatment. Conclusion Antimalarial targets of Artemisia annua ingredients were explored with data mining methods, and the antimalarial effect of scopoletin may be related to TNF. Combined application of the four elements could achieve the same antimalarial effect and reduce the clinical usage of artemisinin and scopoletin.


2020 ◽  
Author(s):  
Yuping Zhao ◽  
Xiaobo Zhang ◽  
Haiyu Xu ◽  
Ling Wang ◽  
Luqi Huang

Abstract Background: Artemisinin is widely used to anti malaria, but the antimalaria mechanism and coordinative interaction of Artemisinin, Scopoletin, Arteannuin B and Artemisic acid are not clear.Methods: Based on the existing of antimalarial drugs, the antimalaria targets of Artemisinin, Scopoletin, Arteannuin B and Artemisic acid were explored by molecular docking with the similarity theory of chemical structure, and then the antimalaria mechanism of Scopoletin and its coordinative antimalaria interaction of the mixture with the three other ingredients.Results: Then through using the text information excavation’s method, the relevance proteins of antimalaria effect of Artemisinin were IL-6, ACHE, PC3, IPOB, CYC, TNF-α, UGT1A9, CASP3, XDH, IL-1β, VEGF, CAT, CREB, AMPK, UGT1A6, ADR, MAPK, COX2, LB24AB and CYP450. Meanwhile, the relevance proteins of Scopoletin were TNF-α, PI3K, IL-8, IL- 6, VEGF, IL-1β, MAPK, CD4, SP2, CTNNB, CASP3, PRO1400, IgE, IL-4, ICAM1, p38, STAT3, TLR4 and API4. But Arteannuin B and Artemisic acid had a little relevance with the above proteins. The interaction characteristic between TNF-α and Artemisia annua was the effect of the mixture of Artemisinin, Scopoletin, Arteannuin B and Artemisic acid was greater than Artemisinin, and the synergistic effect of the four elements was found in the progress of antimalaria.Conclusion: Antimalarial target of Artemisia annua ingredients was explored with data mining methods, and the antimalarial effect of Scopoletin may be related to TNF. Combined application of the four elements could achieve the same antimalarial effect and reduce the clinical usage of Artemisinin and Scopoletin.


2020 ◽  
Author(s):  
yuping zhao ◽  
Xiaobo Zhang ◽  
Haiyu Xu ◽  
Ling Wang ◽  
Luqi Huang

Abstract Background: Artemisinin is widely used to anti malaria, but the antimalaria mechanism and coordinative interaction of Artemisinin, Scopoletin, Arteannuin B and Artemisic acid are not clear. Methods: Based on the existing of antimalarial drugs, the antimalaria targets of Artemisinin, Scopoletin, Arteannuin B and Artemisic acid were explored by molecular docking with the similarity theory of chemical structure, and then the the antimalaria mechanism of Scopoletin and its coordinative antimalaria interaction of the mixture with the three other ingredients. Results: Then through using the text information excavation's method, the relevance proteins of antimalaria effect of Artemisinin were IL-6, ACHE, PC3, IPOB, CYC, TNF-α, UGT1A9, CASP3, XDH, IL-1β, VEGF, CAT, CREB, AMPK, UGT1A6, ADR, MAPK, COX2, LB24AB and CYP450. Meanwhile, the relevance proteins of Scopoletin were TNF-α, PI3K, IL-8, IL- 6, VEGF, IL-1β, MAPK, CD4, SP2, CTNNB, CASP3, PRO1400, IgE, IL-4, ICAM1, p38, STAT3, TLR4 and API4. But Arteannuin B and Artemisic acid had a little relevance with the above proteins. The interaction characteristic between TNF-a and Artemisia annua was the effect of the mixture of Artemisinin, Scopoletin, Arteannuin B and Artemisic acid was greater than Artemisinin, and the synergistic effect of the four elements was found in the progress of antimalaria. Conclusion: Antimalarial target of Artemisia annua ingredients was explored with data mining methods, and the antimalarial effect of Scopoletin may be related to TNF. Combined application of the four elements could achieve the same antimalarial effect and reduce the clinical usage of Artemisinin and Scopoletin.


Molecules ◽  
2010 ◽  
Vol 15 (2) ◽  
pp. 804-812 ◽  
Author(s):  
Colin W. Wright ◽  
Peter A. Linley ◽  
Reto Brun ◽  
Sergio Wittlin ◽  
Elisabeth Hsu

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