• Title/Summary/Keyword: Santonin

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Synthesis of Diacetoxy Acetal Derivatives of Santonin and their Enhancing Effects on HL-60 Leukemia Cell Differentiation

  • Kim, Seung-Hyun;Chung, Sun-Young;Kim, Tae-Sung;Choi, Bo-Gil
    • Archives of Pharmacal Research
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    • v.29 no.1
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    • pp.40-45
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    • 2006
  • Several diacetoxy acetal analogues have been synthesized from santonin and assessed for their ability of inducing or enhancing the differentiation of human HL-60 leukemia cells. The compounds themselves had little effect on HL-60 cell differentiation. However, three analogues, 2a, 3a, and 5b, synergistically enhanced 1,25-dihydroxyvitamin $D_3[1,25-(OH)_2D_3]-induced$ HL-60 cell differentiation when combined with 5 nM of dihydroxyvitamin $D_3[1,25(OH)_2O_3]$, a well-known differentiation inducer. Especially, the compound 5b profoundly enhanced the $1,25-(OH)2O_3]-induced$ HL-60 cell differentiation.

Synthesis of Sesquiterpene Derivitives as Potential Antitumor Agents; Elemance Derivatives

  • Choi, Bo-Gil;Kwak, Eun-Yee;Chung, Byung-Ho;Cho, Won-Jae;Cheon, Seung-Hoon
    • Archives of Pharmacal Research
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    • v.22 no.6
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    • pp.575-578
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    • 1999
  • Derivatives of elema-1,3-diene were synthesized in several steps as polar analogs of $\beta$-elemene, antitumor agent under clinical phase. The lactone ring of compound 1 was opened by LiAlH4 to give diol 2 which was selectively protected by TBDPSCI. After acetylation of the secondary alcohol, the acetylated product was ozonolyzed and reduced to give elemene derivative 4 which was converted to diolefin 8 via selenides subsequent deprotection by tetrabutylammonium fluoride gave two compounds 9, 10.

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Sesquiterpene Lactones: A Review of Biological Activities (세스퀴테르펜 락톤류: 생리활성 재검토)

  • Karadeniz, Fatih;Oh, Jung Hwan;Kong, Chang-Suk
    • Journal of Life Science
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    • v.31 no.4
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    • pp.430-441
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    • 2021
  • Sesquiterpene lactones (STLs) are terpenoids found mostly in the Asteraceae family and are known for their strong cytotoxic properties, among other notable bioactivities. Some STLs, such as artemisinin and mipsagargin, are already commercially available and are used to fight malaria and tumor growth, respectively. Although the interest in STLs was low for a time after their discovery due to their toxic nature, past decades have witnessed a soar in STL-based studies focused on developing novel pharmaceuticals via chemical diversification. These studies have reported several promising physiological effects for STLs, including lower toxicity and diverse modes of action, and have demonstrated the antimicrobial, antioxidant, hepatoprotective, antiviral, antiprotozoal, phytotoxic, antitumor, and antiaging properties of STLs. STLs are mainly considered as valuable natural molecules for the fight against cancer since most STLs induce death of different types of cancer cells, as shown by in vitro and in vivo studies. Some STLs can also enhance the effects of drugs that are already in clinical use. Medicinal chemists use various STLs as starting molecules for the synthesis of new STLs or different bioactive compounds. All these developments warrant future research to provide more information on STLs, their bioactivities, and their mode of action. In this context, this review has summarized the bioactivities of some of the widely studied STLs, namely artemisinin, costunolide, thapsigargin, arglabin, parthenolide, alantolactone, cynaropicrin, helenalin, and santonin.

The Effect of Mugwort(Artemisia asiatica Nakai) Juice on the Motility of the Isolated Rabbit Duodenum (쑥(Artemisia asiatica Nakai)이 가토(家兎)의 척출장관운동(剔出腸管運動)에 미치는 영향)

  • Kim, Kee-Yong;Shin, Hong-Kee;Kim, Kee-Soon
    • The Korean Journal of Physiology
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    • v.14 no.1
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    • pp.41-45
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    • 1980
  • It has long teen known in herbal medicine that the mugwort not only exerts a strong hemostatic and parasiticidal actions but also has therapeutic effects for stomachache and diarrhea. In recent pharmaceutical botany the mugwort is known to have antipyretic and astringent actions also. Among the major principles which have been found in the leaves and stems of mugwort are inulin, alkaloids, vitamines, and esestial oil. It is well known that santonin, one of the well known parasiticides, is one of the glucosides extracted from the limited species of mugwort. The present study was undertaken to investigate effects of mugwort(Artemisia asiatica Nakai) on the motility of isolated rabbit duodenum. The results obtained are as follows: At does of 0.2%, 0.5% and 1. 0% AAJ(Artemisia asiatica juice) markedly enhanced contractility of isolated duodenum and tonus of the intestine was also augmented with doses of 0.5% and 1.0%. The augmentative effect of AAJ on intestinal motility was not affected by pretreatment with epinephrine and avil while it was completely abolished by atropine. Therefore it is strongly suggested that augmentative action of AAJ on duodenal motility was exerted solely through muscarinic cholinergic receptors.

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Depressor Responses to Intravenously Administered Artemisia asiatica Nakai Juice in Cats (애엽(艾葉) (Artemisia asiatica Nakai)의 혈압강하작용(血壓降下作用))

  • Kim, Yun-Ho;Shin, Hong-Kee;Kim, Kee-Soon
    • The Korean Journal of Physiology
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    • v.15 no.2
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    • pp.91-96
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    • 1981
  • The wormwood is one of the plants which occur widely throughout the world. Though the precise data on the entire chemical composition of mugwort leaves are not available, the major principles which have been found so far include inulin, alkaloid, thujon, sesquiterpene and several vitamins. Santonin, a parasiticide, is one of the glucosides extracted from the limited species of wormwood. It has long been known in herb medicine that the plants of this family has not only strong hemostatic, analgesic and parasiticidal actions but also therapeutic effects for diarrhea, stomachache and asthma. In recent pharmaceutical botany the wormwood is introduced to have antipyretic and astringent actions also. The mugwort(Artemisia asiatica Nakai) is the most common species of wormwood that occurs in Korea. The usage of this edible leaves of mugwort is rather various. It is used not only for wormwood bath but also as forage, moxa and medicinal agents. Recently Kim et al reported from their study on the effect of mugwort on the motility of isolated intestine of rabbits that tonus and motility were markedly enhanced by mugwort but this effect of mugwort on intestinal motility was almost completely blocked by atropine suggesting that activity of mugwort was exerted through its cholinergic effect. It was the findings of Kim et al that prompted the authors to do the present experiment. The present study was undertaken to investigate effects of mugwort(Artemisia asiatica Nakai) juice on the respiration and blood pressure in cats. And also studied was the mechanism of depressor action of Artemisia asiatica Nakai Juice (AAJ). The results obtained are as follows; 1) It was observed that mean arterial blood pressure and heart rate were decreased markedly by AAJ. Following administration of 0.15 ml/kg and 0.3 ml/kg AAJ into cats the maximum depressor responses observed were $77.5{\pm}2.2\;mmHg$ and $94.0{\pm}3.7\;mmHg$ respectively. 2) Depressor responses to AAJ were blocked markedly by atropine whereas the responses were not affected by propranolol and dibenamine. Therefore it is strongly inferred that depressor action of AAJ results mainly from its cholinergic effect. This inference was further substantiated by the fact that heart rate change which invariably accompanies depressor responses to AAJ was almost completely abolished by atropinization. 3) After administration of AAJ into cats frequency of respiration was markedly increased while depth of respiration decreased during first 2-3 seconds.

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