• 제목/요약/키워드: artemisinin

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Enhancement of artemisinin content by constitutive expression of the HMG-CoA reductase gene in high-yielding strain of Artemisia annua L.

  • Nafis, Tazyeen;Akmal, Mohd.;Ram, Mauji;Alam, Pravej;Ahlawat, Seema;Mohd, Anis;Abdin, Malik Zainul
    • Plant Biotechnology Reports
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    • v.5 no.1
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    • pp.53-60
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    • 2011
  • Artemisinin is effective against both chloroquine-resistant and -sensitive strains of Plasmodium species. However, the low yield of artemisinin from cultivated and wild plants is a serious limitation to the commercialization of this drug. Optimization of artemisinin yield either in vivo or in vitro is therefore highly desirable. To this end, we have overexpressed the 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase (HMGR) gene (hmgr) from Catharanthus roseus L. in Artemisia annua L. and analyzed its influence on artemisinin content. PCR and Southern blot analyses revealed that the transgenic plants showed stable integration of the foreign hmgr gene. The reverse transcriptase-PCR results suggested that the hmgr was expressed at the transcriptional level in transgenic lines of Artemisia annua L., while the high-performance liquid chromatography analysis showed that artemisinin content was significantly increased in a number of the transgenic lines. Artemisinin content in one of the A. annua transgenic lines was 38.9% higher than that in non-transgenic plants, and HMGR enzyme activity in transgenic A. annua L. was also higher than that in the non-transgenic lines.

Antiarrhythmic Effect of Artemisinin in an Ex-vivo Model of Brugada Syndrome Induced by NS5806

  • Hyung Ki Jeong;Seo Na Hong;Namsik Yoon;Ki Hong Lee;Hyung Wook Park;Jeong Gwan Cho
    • Korean Circulation Journal
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    • v.53 no.4
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    • pp.239-250
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    • 2023
  • Background and Objectives: Brugada syndrome (BrS) is an inherited arrhythmia syndrome that presents as sudden cardiac death (SCD) without structural heart disease. One of the mechanisms of SCD has been suggested to be related to the uneven dispersion of transient outward potassium current (Ito) channels between the epicardium and endocardium, thus inducing ventricular tachyarrhythmia. Artemisinin is widely used as an antimalarial drug. Its antiarrhythmic effect, which includes suppression of Ito channels, has been previously reported. We investigated the effect of artemisinin on the suppression of electrocardiographic manifestations in a canine experimental model of BrS. Methods: Transmural pseudo-electrocardiograms and epicardial/endocardial transmembrane action potentials (APs) were recorded from coronary-perfused canine right ventricular wedge preparations (n=8). To mimic the BrS phenotypes, acetylcholine (3 μM), calcium channel blocker verapamil (1 μM), and Ito agonist NS5806 (6-10 μM) were used. Artemisinin (100-150 μM) was then perfused to ameliorate the ventricular tachyarrhythmia in the BrS models. Results: The provocation agents induced prominent J waves in all the models on the pseudo-electrocardiograms. The epicardial AP dome was attenuated. Ventricular tachyarrhythmia was induced in six out of 8 preparations. Artemisinin suppressed ventricular tachyarrhythmia in all 6 of these preparations and recovered the AP dome of the right ventricular epicardium in all preparations (n=8). J wave areas and epicardial notch indexes were also significantly decreased after artemisinin perfusion. Conclusions: Our findings suggest that artemisinin has an antiarrhythmic effect on wedge preparation models of BrS. It might work by inhibition of potassium channels including Ito channels, subsequently suppressing ventricular tachycardia/ventricular fibrillation.

Investigation of Medicinal Substances from in vitro Cultured Cells and Leaves of Artemisia princeps var. Orientalis (쑥의 잎과 기내 배양세포로부터 약용물질의 탐색)

  • Shin, Dong-Ho;In, Jun-Gyo;Yu, Sang-Ryul;Choi, Kwan-Sam
    • Korean Journal of Medicinal Crop Science
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    • v.13 no.3
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    • pp.69-76
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    • 2005
  • The young leaves of A. princeps have been a well known for a crude medicine and used in treatment of colic pain, vomiting and menstrual irregularity. Based on TLC and HPLC and used an artemisinin, an anti-malarial compounds which is believed to be detected only in A. annuaup so far can be biosynthesized in A. princeps. To investigate the production of secondary metabolites like artemisinin in cultured cells, the cell culture of A. princeps was established. Callus and suspension cultured cells of A. princeps were induced and grown highest in MS media containing $0.2\;mg/{\ell}$ 2,4-D, $0.1\;mg/{\ell}$ BAP and 2% sucrose. Different metabolites from in vitro cultured cells (callus and suspension cultured cell) and intact plants were analyzed by TLC analysis. As a result, we can confirm that in vitro culture has a potential for mass production of secondary metabolites from A. princeps.

Molecular Cloning of a Partial Cadinane Synthase Gene from Artemisia annua

  • Song, Seung-hwan;Chang, Yung-jin;Kim, Jeong-gu;Kim, Soo-Un
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1998.11a
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    • pp.121-121
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    • 1998
  • Artemisia annua, an indigenous plant in Korea, contains a clinically important potent antimalarial principle, artemisinin. Artemisinin is a cadinane-type sesquiterpene endoperoxide. Cadinane synthase catalyzes the first committed step in artemisinin biosynthesis by cyclizing farnesyldiphosphate. In hopes of finding a cadinane synthase gene involved in artemisinin biosynthesis, oligonucleotides were synthesized on. the basis of the consensus nucleotide sequences and Nco I restriction sites for convenience in cloning. Specifically, nucleotide sequences of two highly conserved regions were deduced from the genes of similar function of Hyoscyamus muticus, Nicotiana tabacum, Abies grandis, Lycopersicon esculentum, and Gossypium hirsutum to construct a set of primers for polymerase chain reation (PCR). A 184 bp fragment was found to be amplified by PCR, and subsequently cloned. The gene revealed 62.8% identity in nucleotide and 55.6% in amino acid sequence to correspondent gene of N. tabacum. The gene was different from another sesquiterpene cyclase gene of A. annua, germacranadiene synthase gene, recently reported by Mercke and Bordelius (1998).

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Anti-inflammatory, Antioxidant and Antimicrobial Effects of Artemisinin Extracts from Artemisia annua L.

  • Kim, Wan-Su;Choi, Woo Jin;Lee, Sunwoo;Kim, Woo Joong;Lee, Dong Chae;Sohn, Uy Dong;Shin, Hyoung-Shik;Kim, Wonyong
    • The Korean Journal of Physiology and Pharmacology
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    • v.19 no.1
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    • pp.21-27
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    • 2015
  • The anti-inflammatory, antioxidant, and antimicrobial properties of artemisinin derived from water, methanol, ethanol, or acetone extracts of Artemisia annua L. were evaluated. All 4 artemisinin-containing extracts had anti-inflammatory effects. Of these, the acetone extract had the greatest inhibitory effect on lipopolysaccharide-induced nitric oxide (NO), prostaglandin $E_2$ ($PGE_2$), and proinflammatory cytokine ($IL-1{\beta}$, IL-6, and IL-10) production. Antioxidant activity evaluations revealed that the ethanol extract had the highest free radical scavenging activity, ($91.0{\pm}3.2%$), similar to ${\alpha}$-tocopherol (99.9%). The extracts had antimicrobial activity against the periodontopathic microorganisms Aggregatibacter actinomycetemcomitans, Fusobacterium nucleatum subsp. animalis, Fusobacterium nucleatum subsp. polymorphum, and Prevotella intermedia. This study shows that Artemisia annua L. extracts contain anti-inflammatory, antioxidant, and antimicrobial substances and should be considered for use in pharmaceutical products for the treatment of dental diseases.

Cultivation Characteristics and Variation of Artemisinin Contents by Harvest Time of Artemisia annua L. Distributed in Korea (한국산 개똥쑥의 재배특성 및 수확시기에 따른 Artemisinin의 함량변이)

  • Lee, Jeong Hoon;Lee, Sang Hoon;Park, Chun Geun;Park, Chung Berm;Kim, Ok Tae;Choi, Ae Jin;Kim, Yong Joo;Cha, Seon Woo
    • Korean Journal of Medicinal Crop Science
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    • v.21 no.6
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    • pp.433-438
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    • 2013
  • This study was conducted to obtain the basic data for using the Artemisia anuua as a new economic crop, thus Artemisia anuua was investigated their cultivation characteristics, yield, and variation of artemisinin contents by planting density and harvesting times. Seed characteristics of A. anuua have observed micro-size, and their germination optimum temperature was at 15 to 20 celsius degree. Planting density on the yield of A. anuua was increased high density better than low density. The highest yield was planted in the space of $30{\times}10$cm. Moreover, optimum harvesting time of A. anuua was investigated in early september and a periods of most highly detected artemisinin was time of before and after blooming of A. anuua.

Antimalarial activity of thiophenyl- and benzenesul-fonyl-dihydroartemisinin

  • LEE Seokjoon;OH Sangtae;PARK Gab-Man;KIM Tong-Soo;RYU Jae-Sook;CHOI Han-Kyu
    • Parasites, Hosts and Diseases
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    • v.43 no.3 s.135
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    • pp.123-126
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    • 2005
  • Each diastereomer of 10-thiophenyl- and 10-benzenesulfonyl-dihydroartemisinin was synthesized from artemisinin in three steps, and screened against chloroquine-resistance and chloroquine-sensitive Plasmodium falciparum. Three of the four tested compounds were found to be effective. Especially, 10$\beta$-benzenesulfonyl-dihy-droartemisinin showed stronger antimalarial activity than artemisinin.

Electrochemical Determination of Artemisinin in Artemisia annua L Herbal Tea Preparation and Optimization of Tea Making Approach (개똥쑥 약초차 제조에서 아르테미시닌의 전기화학적 측정과 차를 만드는 최적화로의 접근법)

  • Debnath, Chhanda;Dobernig, Andrea;Saha, Pijus;Ortner, Astrid
    • Journal of the Korean Chemical Society
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    • v.55 no.1
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    • pp.57-62
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    • 2011
  • Sometimes inhabitants in remote areas have inadequate or no access to modern medicines or medical services. They can get benefit in term of the treatment against malaria by cultivating selected breeding of A. annua and making teas or decoctions from the plant materials following the proper way of tea preparation. In order to have the maximum extraction efficiency for artemisinin, different ways of tea preparations of A. annua were investigated by applying the developed DPP method and described in this article. Tea was prepared by three different ways (cooking, without cooking with/without shaking and microwave oven) with different times. From the results, it has been found that higher concentration of artemisinin (84.7%) can be attained by following the approach for tea preparation without cooking with shaking for 15 minutes (R.S.D. 2.34%). The concentration of artemisinin decreases with cooking more than 1.5 min in microwave oven. The utmost extraction (88.9% of artemisinin) is possible to extract by shaking with boiled 5% ethanol in distilled water (R.S.D. 2.28%).