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the 4th letter of the Roman alphabet (同)d
any of various red antibiotics isolated from soil bacteria

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deuteriumの化学記号
(おもに人称代名詞・固有名詞(人名),thereの後で)had, wouldの短縮形 / (疑問文でwhere,what,whenの後で)didの短縮形;Where'd he go?=Where did he go?

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/08/12 04:05:29」(JST)

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Dactinomycin (INN, BAN, AAN and USAN also known generically as actinomycin D), is the most significant member of actinomycines, which are a class of polypeptide antitumor antibiotics isolated from soil bacteria of the genus Streptomyces.^[1] It is one of the older anticancer drugs, and has been used for many years.

History

Actinomycin D was the first antibiotic shown to have anti-cancer activity.^[1] It was first isolated by Selman Waksman and his co-worker H. B. Woodruff in 1940.^[2] It was approved by the U.S. Food and Drug Administration (FDA) on December 10, 1964 and launched by Merck Sharp and Dohme under the trade name Cosmegen.

Mechanism

In cell biology, Actinomycin D is shown to have the ability to inhibit transcription. Actinomycin D does this by binding DNA at the transcription initiation complex and preventing elongation of RNA chain by RNA polymerase.^[3]

Clinical use

Actinomycin is a clear, yellow liquid administered intravenously and most commonly used in treatment of a variety of cancers, including:

Gestational trophoblastic neoplasia^[4]
Wilms' tumor^[5]
Rhabdomyosarcoma^[6]
Ewing's sarcoma^[7]
Malignant hydatidiform mole^[8]

Sometimes it will be combined with other drugs in Chemotherapy regimens, like the VAC regimen (with Vincristine and Cyclophosphamide) for treating rhabdomyosarcoma and Ewing's Sarcoma.

It is also used as a radiosensitizer in adjunct to radiotherapies, since it can increase the radiosensitivity of tumor cells by inhibiting repair of sublethal radiation damage and delay the onset of the compensatory hyperplasia that occurs following irradiation.^[9]

Side effects

Common adverse drug reaction includes bone marrow suppression, fatigue, hair loss, mouth ulcer, loss of appetite and diarrhea. Actinomycin is a vesicant, if extravasation occurs.

Research use

Because Actinomycin can bind DNA duplexes, it can also interfere with DNA replication, although other chemicals such as hydroxyurea are better suited for use in the laboratory as inhibitors of DNA synthesis.

Actinomycin D and its fluorescent derivative, 7-aminoactinomycin D (7-AAD), are used as stains in microscopy and flow cytometry applications. The affinity of these stains/compounds for GC-rich regions of DNA strands makes them excellent markers for DNA. 7-AAD binds to single stranded DNA; therefore it is a useful tool in determining apoptosis and distinguishing between dead cells and live ones.^[10]

References

^ ^a ^b Hollstein, U. (1974). "Actinomycin. Chemistry and mechanism of action". Chemical Reviews 74 (6): 625–652. doi:10.1021/cr60292a002.
^ Waksman S A, Woodruff H B (1940). "Bacteriostatic and bacteriocidal substances produced by soil actinomycetes". Proc Soc Exper Biol 45: 609–614.
^ Sobell H (1985). "Actinomycin and DNA transcription". Proceedings of the National Academy of Sciences of the United States of America 82 (16): 5328–31. doi:10.1073/pnas.82.16.5328. PMC 390561. PMID 2410919.
^ Turan T, Karacay O, Tulunay G, Boran N, Koc S, Bozok S, Kose M (2006). "Results with EMA/CO (etoposide, methotrexate, actinomycin D, cyclophosphamide, vincristine) chemotherapy in gestational trophoblastic neoplasia". Int J Gynecol Cancer 16 (3): 1432–8. doi:10.1111/j.1525-1438.2006.00606.x. PMID 16803542.
^ D'Angio GJ, Evans A, Breslow N, Beckwith B, Bishop H, Farewell V, Goodwin W, Leape L, Palmer N, Sinks L, Sutow W, Tefft M, Wolff J (1981). "The treatment of Wilms' tumor: results of the Second National Wilms' Tumor Study.". Cancer 47 (9): 2302–11. PMID 6164480.
^ Khatua S, Nair C, Ghosh K (2004). "Immune-mediated thrombocytopenia following dactinomycin therapy in a child with alveolar rhabdomyosarcoma: the unresolved issues". J Pediatr Hematol Oncol 26 (11): 777–9. doi:10.1097/00043426-200411000-00020. PMID 15543019.
^ Jaffe, N.; Paed, D.; Traggis, D.; Salian, S.; Cassady, J. R. (1976). "Improved outlook for Ewing's sarcoma with combination chemotherapy (vincristine, actinomycin D and cyclophosphamide) and radiation therapy". Cancer 38 (5): 1925–1930. doi:10.1002/1097-0142(197611)38:5<1925::AID-CNCR2820380510>3.0.CO;2-J. PMID 991106.
^ Uberti, E. M. H.; Fajardo, M. D. C.; Ferreira, S. V. V. R.; Pereira, M. C. V.; Seger, R. C.; Moreira, M. A. L. R.; Torres, M. D.; De Nápoli, G.; Schmid, H. (2009). "Reproductive outcome after discharge of patients with high-risk hydatidiform mole with or without use of one bolus dose of actinomycin D, as prophylactic chemotherapy, during the uterine evacuation of molar pregnancy". Gynecologic Oncology 115 (3): 476–481. doi:10.1016/j.ygyno.2009.09.012. PMID 19818481.
^ Hagemann, R. F.; Concannon, J. P. (1973). "Mechanism of intestinal radiosensitization by actinomycin D". British Journal of Radiology 46 (544): 302–308. doi:10.1259/0007-1285-46-544-302. PMID 4720744.
^ Toba, K.; Koike, T.; Watanabe, K.; Fuse, I.; Takahashi, M.; Hashimoto, S.; Takahashi, H.; Abe, T.; Yano, T.; Shibazaki, Y.; Itoh, H.; Aizawa, Y. (2000). "Cell kinetic study of normal humanbone marrow hematopoiesis andacute leukemia using 7AAD/PY". European Journal of Haematology 64 (1): 10–21. doi:10.1034/j.1600-0609.2000.09005.x. PMID 10680701. edit

External links

MedlinePlus DrugInfo medmaster-a682224

UpToDate Contents

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1. 低リスク妊娠性絨毛腫瘍の初期マネージメント initial management of low risk gestational trophoblastic neoplasia
2. 抵抗性または再発性の妊娠性絨毛腫瘍のマネージメント management of resistant or recurrent gestational trophoblastic neoplasia
3. ユーイング肉腫ファミリーの腫瘍の治療 treatment of the ewing sarcoma family of tumors
4. 高リスク妊娠性絨毛腫瘍の初期マネージメント initial management of high risk gestational trophoblastic neoplasia
5. ウィルムス腫瘍の治療および予後 treatment and prognosis of wilms tumor

English Journal

Decrease in transient receptor potential melastatin 6 mRNA stability caused by rapamycin in renal tubular epithelial cells.

Ikari A, Sanada A, Sawada H, Okude C, Tonegawa C, Sugatani J.SourceDepartment of Pharmaco-Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.
Biochimica et biophysica acta.2011 Jun;1808(6):1502-8. Epub 2010 Nov 10.
Rapamycin, an inhibitor of mammalian target of rapamycin (mTOR), is used in treatments for transplantation and cancer. Rapamycin causes hypomagnesemia, although precisely how has not been examined. Here, we investigated the effect of rapamycin on the expression of transient receptor potential melast
PMID 21073857

Luteolin inhibits Nrf2 leading to negative regulation of the Nrf2/ARE pathway and sensitization of human lung carcinoma A549 cells to therapeutic drugs.

Tang X, Wang H, Fan L, Wu X, Xin A, Ren H, Wang XJ.SourceDepartment of Biochemistry and Genetics, School of Medicine, Zhejiang University, Hangzhou 310058, People's Republic of China.
Free radical biology & medicine.2011 Jun 1;50(11):1599-609. Epub 2011 Mar 12.
Nuclear factor erythroid 2-related factor 2 (Nrf2) is a redox-sensitive transcription factor regulating the expression of a battery of cytoprotective genes. Constitutive Nrf2 activation in many tumors enhances cell survival and resistance to anticancer drugs. Using a cell-based ARE-reporter assay we
PMID 21402146

Japanese Journal

ヌードマウス移植ヒト神経芽腫および横紋筋肉腫に対するイリノテカン(CPT-11)の抗腫瘍作用

金子節子,金子道夫
小児がん : 小児悪性腫瘍研究会記録 47(1), 98-104, 2010-02-25
10種類の抗腫瘍剤を用いたヌードマウス移植ヒト神経芽腫および横紋筋肉腫の感受性試験で通常用量CPT-11はCPAと並ぶ優れた増殖抑制作用を有した.さらに,通常用量CPT-11・間欠投与法に比べ,低用量CPT-11・連日投与法の抗腫瘍効果は6系統の移植腫瘍のうち5系統で有意に高かった.低用量CPT-11投与では休薬期間を長くしない方がより有効であった.CPT-11の投与用量に関わらずマウスにスコア1 …
NAID 110007575324

Selective Regulation of Multidrug Resistance Protein in Vascular Smooth Muscle Cells by the Isoquinoline Alkaloid Coptisine

Suzuki Hiroka,Tanabe Hiroki,Mizukami Hajime,Inoue Makoto
Biological & Pharmaceutical Bulletin 33(4), 677-682, 2010
… In A10 cells (a rat VSMC line), coptisine upregulated the mRNAs of Mdr1a and Mdr1b, rodent homologues of human MDR1, and these effects were completely abrogated by actinomycin D. …
NAID 130000248018

Related Pictures

Actinomycin D | Buy Actinomycin D from Actinomycin D | Apoptosis Inducers structure of a complex between actinomycin Actinomycin D sticks.png Actinomycin D Prices,Actinomycin D Actinomycin D (Dactinomycin) is an

★リンクテーブル★

リンク元	「アクチノマイシンD」
関連記事	「D」「actinomycin」

「アクチノマイシンD」

Actinomycin D
Systematic (IUPAC) name
	2-Amino-N,N′- bis[(6S,9R,10S,13R,18aS)-6,13-diisopropyl-2,5,9-trimethyl-1,4,7,11,14-pentaoxohexadecahydro-1H-pyrrolo[2,1-i][1,4,7,10,13]oxatetraazacyclohexadecin-10-yl]-4,6-dimethyl-3-oxo-3H-phenoxazine-1,9-dicarboxamide
Clinical data
Trade names	Cosmegen
AHFS/Drugs.com	monograph
MedlinePlus	a682224
Pregnancy; category	AU: D; US: D (Evidence of risk);
Legal status	AU: Prescription Only (S4); CA: ℞-only; UK: Prescription-only (POM); US: ℞-only;
Routes of; administration	IV
Pharmacokinetic data
Protein binding	5%
Biological half-life	36 hours
Identifiers
CAS Registry Number	50-76-0
ATC code	L01DA01
PubChem	CID: 2019
DrugBank	DB00970
ChemSpider	10482167
UNII	1CC1JFE158
KEGG	C06770
ChEBI	CHEBI:27666
ChEMBL	CHEMBL1554
NIAID ChemDB	009885
Synonyms	2-Amino- 4,6-dimethyl- 3-oxo- 3H-phenoxazine- 1,9-dicarboxylic acid bis- [(5,12-diisopropyl- 9,13,16-trimethyl- 4,7,11,14,17-pentaoxo- hexadecahydro- 10-oxa- 3a,6,13,16-tetraaza- cyclopentacyclohexadecen- 8-yl)- amide]
Chemical data
Formula	C62H86N12O16
Molecular mass	1255.42 g/mol
	InChI InChI=1S/C62H86N12O16/c1-27(2)42-59(84)73-23-17-19-36(73)57(82)69(13)25-38(75)71(15)48(29(5)6)61(86)88-33(11)44(55(80)65-42)67-53(78)35-22-21-31(9)51-46(35)64-47-40(41(63)50(77)32(10)52(47)90-51)54(79)68-45-34(12)89-62(87)49(30(7)8)72(16)39(76)26-70(14)58(83)37-20-18-24-74(37)60(85)43(28(3)4)66-56(45)81/h21-22,27-30,33-34,36-37,42-45,48-49H,17-20,23-26,63H2,1-16H3,(H,65,80)(H,66,81)(H,67,78)(H,68,79)/t33-,34-,36+,37+,42-,43-,44+,45+,48+,49+/m1/s1 ; Key:RJURFGZVJUQBHK-IIXSONLDSA-N ;
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　　[★]

英: actinomycin D　actinomycin-D ACT-D
同: アクチノマイシン actinomycin、ダクチノマイシン dactinomycin DACT、Cosmegen
商: コスメゲン Cosmegen

first aid step1 2006 p.307,309,326

分類

抗悪性腫瘍薬

抗生物質

構造

作用機序

intercalates in DNA

適応

Wilms' tumor, Ewing's sarcoma, rhabdomyosarcoma(first aid step1 2006 p.309) ← 子供の腫瘍

副作用

myelosuppression

「D」

　　[★]

アスパラギン酸
ジヒドロウリジン
遠位の distal,
うつ病 depression
下行結腸 descending colon(大腸内視鏡検査の結果を記載するときに用いる)

「actinomycin」

　　[★] アクチノマイシンD、アクチノマイシン　

[gen-1] Hollstein, U. (1974). "Actinomycin. Chemistry and mechanism of action". Chemical Reviews 74 (6): 625–652. doi:10.1021/cr60292a002.

[2] Waksman S A, Woodruff H B (1940). "Bacteriostatic and bacteriocidal substances produced by soil actinomycetes". Proc Soc Exper Biol 45: 609–614.

[3] Sobell H (1985). "Actinomycin and DNA transcription". Proceedings of the National Academy of Sciences of the United States of America 82 (16): 5328–31. doi:10.1073/pnas.82.16.5328. PMC 390561. PMID 2410919.

[4] Turan T, Karacay O, Tulunay G, Boran N, Koc S, Bozok S, Kose M (2006). "Results with EMA/CO (etoposide, methotrexate, actinomycin D, cyclophosphamide, vincristine) chemotherapy in gestational trophoblastic neoplasia". Int J Gynecol Cancer 16 (3): 1432–8. doi:10.1111/j.1525-1438.2006.00606.x. PMID 16803542.

[5] D'Angio GJ, Evans A, Breslow N, Beckwith B, Bishop H, Farewell V, Goodwin W, Leape L, Palmer N, Sinks L, Sutow W, Tefft M, Wolff J (1981). "The treatment of Wilms' tumor: results of the Second National Wilms' Tumor Study.". Cancer 47 (9): 2302–11. PMID 6164480.

[6] Khatua S, Nair C, Ghosh K (2004). "Immune-mediated thrombocytopenia following dactinomycin therapy in a child with alveolar rhabdomyosarcoma: the unresolved issues". J Pediatr Hematol Oncol 26 (11): 777–9. doi:10.1097/00043426-200411000-00020. PMID 15543019.

[7] Jaffe, N.; Paed, D.; Traggis, D.; Salian, S.; Cassady, J. R. (1976). "Improved outlook for Ewing's sarcoma with combination chemotherapy (vincristine, actinomycin D and cyclophosphamide) and radiation therapy". Cancer 38 (5): 1925–1930. doi:10.1002/1097-0142(197611)38:5<1925::AID-CNCR2820380510>3.0.CO;2-J. PMID 991106.

[8] Uberti, E. M. H.; Fajardo, M. D. C.; Ferreira, S. V. V. R.; Pereira, M. C. V.; Seger, R. C.; Moreira, M. A. L. R.; Torres, M. D.; De Nápoli, G.; Schmid, H. (2009). "Reproductive outcome after discharge of patients with high-risk hydatidiform mole with or without use of one bolus dose of actinomycin D, as prophylactic chemotherapy, during the uterine evacuation of molar pregnancy". Gynecologic Oncology 115 (3): 476–481. doi:10.1016/j.ygyno.2009.09.012. PMID 19818481.

[9] Hagemann, R. F.; Concannon, J. P. (1973). "Mechanism of intestinal radiosensitization by actinomycin D". British Journal of Radiology 46 (544): 302–308. doi:10.1259/0007-1285-46-544-302. PMID 4720744.

[10] Toba, K.; Koike, T.; Watanabe, K.; Fuse, I.; Takahashi, M.; Hashimoto, S.; Takahashi, H.; Abe, T.; Yano, T.; Shibazaki, Y.; Itoh, H.; Aizawa, Y. (2000). "Cell kinetic study of normal humanbone marrow hematopoiesis andacute leukemia using 7AAD/PY". European Journal of Haematology 64 (1): 10–21. doi:10.1034/j.1600-0609.2000.09005.x. PMID 10680701. edit

匿名

検索

案内

案内

actinomycin-D