Unique Physical Behavior with Two Main Integrated Types of Chemical Substances of Herbal Medicine based Insulin Leaf (Tithonia diversifolia (Hemsley) A. Gray (Asteraceae)): A Healthy Simple Natural Drink

A healthy simple natural drink is introduced based on a deep physical research investigation into insulin leaf (Tithonia diversifolia (Hemsley) A. Gray (Asteraceae)). Such drink was simply fabricated using two steps process of heating and cooling, and then exposed according to 2 main unique physical properties of optical and electrical behaviors. It was well-known that Tithonia diversifolia (Hemsley) A. Gray (Asteraceae)) had been very attractive in the east Africa continent and in the most of areas in Asia continent, as well as in Indonesia country of over 14,480 islands as Daun Kembang bulan because of its various biological and chemical properties to sustain human being life on earth. In present paper, our findings are focused on the unique physical characters sustained with a simple theoretical model to explain the interplay quantity of mechanical vibration of 2 main compounds of Tagitinine A (C19H28O7) and Tagitinine C or artemisinic acid (C15H22O2) identified using HPLC in such natural healthy drink produced by our Herbal Blessing standard products in nanotechnology research center and innovative creation (PPNRI) at Pattimura university. Such interesting finding suggests that the interactive vibration only involved about ~23.763 % mass of the total conserved mass

Network Analysis, and Experimental Validation to Uncover the Mechanism of the Four Compounds in Artemisia annua (Qing Hao) Antimalarial

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.

The anti-mycobacterial activity of Artemisia annua L is based on deoxyartemisinin and artemisinic acid

The discovery of antimalarial artemisinin from Artemisia annua L. is an example of how Traditional Chinese Medicine (TCM) may be exploited to meet a recognized need. In this study, we systemically investigated A. annua L. for its antimicrobial activity and assessed it as a source of bioactive natural products for anti-mycobacterial activity.We used a silica gel column to perform antimicrobial activity-guided purification of the A. annua leaf, whose identity was confirmed by rbcL DNA barcoding, and used UHPLC-HRMS and NMR to elucidate the structure of purified active compounds. The antimicrobial activity of crude extracts, isolated compounds and the control artemisinin (Apollo Scientific Ltd) was assessed against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, methicillin-resistant Staphylococcus aureus (MRSA), Mycobacterium smegmatis strains by serial micro dilution method (31.25-1000 μg/mL). The isolated compounds were tested for synergistic effects against mycobacterium.Bioactive compounds were purified and identified as deoxyartemisinin and artemisinic acid. Artemisinic acid (MIC 250 μg/mL) was more effective in comparison to deoxyartemisinin (MIC 500 μg/mL) and artemisinin (MIC 1000 μg/mL) against M. smegmatis. We used a molecular docking approach to investigate the interactions between selected anti-mycobacterial compounds and proteins involved in vital physiological functions in M. tuberculosis, namely MtPks13, MtPknB, MtPanK, MtKasA, MtInhA and MtDprE1 and found artemisinic acid showed docking scores superior to the control inhibiters for MtKasA, suggesting it to be a potential nick for further in vitro biological evaluation and anti-TB drug design.

Network Analysis, and Experimental Validation to Uncover the Mechanism of the Four Compounds in Artemisia Annua (Qing Hao) Antimalarial

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.

Synthesis of artemisinic acid derived glycoconjugates and their anticancer studies

Twenty-four artemisinic acid glycoconjugate hybrids were synthesized using click reaction and evaluated for their anticancer activities against the MCF7 cell line.

Comparative in vitro cytotoxicity and binding investigation of artemisinin and its biogenetic precursors with ctDNA

Artemisinin (ART) and its biogenetic precursors artemisinic acid (AA) and dihydroartemisinic acid (DHAA) are important traditional medicinal herb compounds with tumor growth inhibition properties.

Lipid Transfer Proteins (AaLTP3 and AaLTP4) Are Involved in Sesquiterpene Lactone Secretion from Glandular Trichomes in Artemisia annua

In Artemisia annua plants, glandular trichomes (GTs) are responsible for the biosynthesis and secretion of sesquiterpene lactones including artemisinin/arteannuin B. Nonspecific lipid transfer proteins (LTPs) in plants bind and carry lipid molecules across the cell membrane and are also known as secretary proteins. Interestingly, the transcripts of LTP genes are exceptionally abundant in the GTs of A. annua. In the present study, we isolated two trichome-specific LTP genes (AaLTP3 and AaLTP4) from a Korean ecotype of A. annua. AaLTP3 was expressed abundantly in shoots, whereas AaLTP4 was expressed in flowers. The GUS signal driven by the AaLTP3 or AaLTP4 promoter in transgenic A. annua plants revealed that the AaLTP3 promoter was active on hair-like non-GTs and that the AaLTP4 promoter was active on GTs. Analysis of enhanced cyan fluorescent protein (ECFP) fluorescence fused with the AaLTP3 or AaLTP4 protein in transgenic tobacco revealed that ECFP florescence was very bright on secreted lipids of long GTs. Moreover, the florescence was also bright on the head cells of short trichomes and their secreted granules. Immunoblotting analysis of GT exudates in petioles of A. annua revealed a strong positive signal against the AaLTP4 antibody. Overexpression of AaLTP3 or AaLTP4 in transgenic A. annua plants resulted in enhanced production of sesquiterpene lactones (arteannuin B, artemisinin, dihydroartemisinic acid and artemisinic acid) compared with those of wild type. The present study shows that LTP genes (AaLTP3 or AaLTP4) play important roles in the sequestration and secretion of lipids in GTs of A. annua, which is useful for the enhanced production of sesquiterpene lactones by genetic engineering.

Simultaneous Quantification of Five Sesquiterpene Components after Ultrasound Extraction in Artemisia annua L. by an Accurate and Rapid UPLC–PDA Assay

Objective: To develop an accurate and rapid ultra-performance liquid chromatography (UPLC) coupled with a photodiode array (PDA) method for the simultaneous determination of artemisinin (Art), arteannuin B (Art B), arteannuin C (Art C), dihydroartemisinic acid (DHAA) and artemisinic acid (AA) in Artemisia annua L. Methodology: Chromatography separation was performed on an ACQUITY UPLC BEH C18 Column with isocratic elution; the mobile phase was 0.1% formic acid aqueous solution (A) and acetonitrile (B) (A:B = 40:60, v/v). Data were recorded at an ultraviolet (UV) wavelength of 191 nm for Art, Art C, DHAA and AA, and 206 nm for Art B. Results: The calibration curves of the five sesquiterpene components were all linear with correlation coefficients more than 0.9990. The linear ranges were 31.44–1572 μg/mL, 25.48–1274 μg/mL, 40.56–2028 μg/mL, 31.44–1572 μg/mL and 26.88–1396 μg/mL for Art, Art B, Art C, DHAA and AA, respectively. The precision ranged from 0.08% to 2.88%, the stability was from 0.96% to 1.66%, and the repeatability was all within 2.42% and had a mean extraction recovery of 96.5% to 100.6%. Conclusion: The established UPLC–PDA method would be valuable for improving the quantitative analysis of sesquiterpene components in Artemisia annua L.