Proscillaridin A

Modify Date: 2024-01-09 16:35:47

Proscillaridin A Structure
Proscillaridin A structure
Common Name Proscillaridin A
CAS Number 466-06-8 Molecular Weight 530.650
Density 1.3±0.1 g/cm3 Boiling Point 716.7±60.0 °C at 760 mmHg
Molecular Formula C30H42O8 Melting Point 233ºC
MSDS Chinese USA Flash Point 232.6±26.4 °C
Symbol GHS06
GHS06
Signal Word Danger

 Use of Proscillaridin A


Proscillaridin A is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively[1].

 Names

Name Proscillaridin A
Synonym More Synonyms

 Proscillaridin A Biological Activity

Description Proscillaridin A is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively[1].
Related Catalog
Target

Topoisomerase I:30 nM (IC50)

Topoisomerase II:100 nM (IC50)

In Vitro Proscillaridin A (0-160 nM; 48 hours) reveals the antiproliferative response in a time- as well as dose-dependent manner in MCF-7 cells[1].
References

[1]. Bielawski K, et al. Inhibition of DNA topoisomerases I and II, and growth inhibition of breast cancer MCF-7 cells by ouabain, digoxin and proscillaridin A.Biol Pharm Bull. 2006 Jul;29(7):1493-7.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 716.7±60.0 °C at 760 mmHg
Melting Point 233ºC
Molecular Formula C30H42O8
Molecular Weight 530.650
Flash Point 232.6±26.4 °C
Exact Mass 530.287964
PSA 129.59000
LogP 3.90
Vapour Pressure 0.0±5.2 mmHg at 25°C
Index of Refraction 1.620
Storage condition 2-8℃

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UK6650000
CHEMICAL NAME :
Proscillaridin A
CAS REGISTRY NUMBER :
466-06-8
LAST UPDATED :
199109
DATA ITEMS CITED :
14
MOLECULAR FORMULA :
C30-H42-O8
MOLECULAR WEIGHT :
530.72
WISWESSER LINE NOTATION :
L E5 B666 MUTJ A1 E1 IQ F- ET6OVJ& O- BT6OTJ CQ DQ EQ F1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
56 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 20,599,1971
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 2,411,1968
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
9 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 20,599,1971
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
30500 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,723,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
4700 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 2,411,1968
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - cat
DOSE/DURATION :
377 ug/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 20,1,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - cat
DOSE/DURATION :
111 ug/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 20,1,1970
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Parenteral
SPECIES OBSERVED :
Mammal - cat
DOSE/DURATION :
1 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
APPHAX Acta Poloniae Pharmaceutica. For English translation, see APPFAR. (Ars Polona, POB 1001, 00-680 Warsaw 1, Poland) V.1- 1937- Volume(issue)/page/year: 34,431,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraduodenal
SPECIES OBSERVED :
Mammal - cat
DOSE/DURATION :
268 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 14,716,1964
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
6810 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4230702
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
280 ug/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 20,1,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Bird - domestic
DOSE/DURATION :
373 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NYKZAU Nippon Yakurigaku Zasshi. Japanese Journal of Pharmacology. (Nippon Yakuri Gakkai, c/o Kyoto Daigaku Igakubu Yakurigaku Kyoshitsu, Konoe-cho, Yoshida, Sakyo-ku, Kyoto 606, Japan) V.40- 1944- Volume(issue)/page/year: 62(3),195S,1966
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Bird - domestic
DOSE/DURATION :
124 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NYKZAU Nippon Yakurigaku Zasshi. Japanese Journal of Pharmacology. (Nippon Yakuri Gakkai, c/o Kyoto Daigaku Igakubu Yakurigaku Kyoshitsu, Konoe-cho, Yoshida, Sakyo-ku, Kyoto 606, Japan) V.40- 1944- Volume(issue)/page/year: 62(3),195S,1966 *** REVIEWS *** TOXICOLOGY REVIEW 85ELDJ "Die Herzwirksamen Glykoside," Baumgarten, G., and W. Forster, Leipzig, Ger. Dem. Rep., VEB Georg Thieme, 1963 Volume(issue)/page/year: -,193,1963

 Safety Information

Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301
Precautionary Statements P301 + P310
Personal Protective Equipment Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges
Hazard Codes T: Toxic;
Risk Phrases R25
Safety Phrases 28-45
RIDADR UN 2811 6.1/PG 3
WGK Germany 3
RTECS UK6650000

 Articles25

More Articles
Pulse pressure correlates in humans with a proscillaridin A immunoreactive compound.

Hypertension 27(5) , 1073-8, (1996)

Endogenous digitalis-like factors in humans are presumably cardenolides and bufadienolides. To test whether bufadienolide-like substances may circulate in human blood, we used antibodies from rabbits ...

Cytotoxic effects of cardiac glycosides in colon cancer cells, alone and in combination with standard chemotherapeutic drugs.

J. Nat. Prod. 72 , 1969-74, (2009)

Cardiac glycosides have been reported to exhibit cytotoxic activity against several different cancer types, but studies against colorectal cancer are lacking. In a screening procedure aimed at identif...

Role of endogenous cardiac glycosides in the spontaneously hypertensive rat--antagonism by active immunization.

Am. J. Hypertens. 9(1) , 81-5, (1996)

The effects of simultaneous active immunization against two cardiac glycoside drugs, digoxin and proscillaridin, have been examined in young spontaneously hypertensive and Wistar-Kyoto rats. Control a...

 Synonyms

Bufa-4,20,22-trienolide, 3-[(6-deoxy-α-L-mannopyranosyl)oxy]-14-hydroxy-, (3β)-
Protasin
14-Hydroxy-3b-(rhamnosyloxy)bufa-4,20,22-trienolide
(3β)-3-[(6-Deoxy-α-L-mannopyranosyl)oxy]-14-hydroxybufa-4,20,22-trienolid
Scillarenin 3β-rhamnoside
3-β-((6-Deoxy-α-L-mannopyranosyl)oxy)-14-hydroxybufa-4,20,22-trienolide
5-[(3S,8R,9S,10R,13R,14S,17R)-14-Hydroxy-10,13-dimethyl-3-{[(2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy}-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]-2H-pyran-2-on
Desgluco-transvaalin
Urgilan
Herzo proscillan
Scillarenin 3b-Rhamnoside
Scillarenin 3a-L-Rhamnopyranoside
3b-Rhamnosido-14b-hydroxy-D4,20,22-bufatrienolide
Proscillaridin
Scillacrist
Desglucotransvaaline
Coratol
Scilla "didier"
(3β)-3-[(6-Deoxy-α-L-mannopyranosyl)oxy]-14-hydroxybufa-4,20,22-trienolide
Purosin-TC
Sandoscill
Wirnesin
Caratol
(3b)-3-[(6-Deoxy-a-L-mannopyranosyl)oxy]-14-hydroxybufa-4,20,22-trienolide
3b-[(6-Deoxy-a-L-mannopyranosyl)oxy]-14-hydroxybufa-4,20,22-trienolide
Tradenal
Herzo
Bufa-4,20,22-trienolide, 3-((6-deoxy-α-L-mannopyranosyl)oxy)-14-hydroxy-, (3β)-
psc-801
Caradrin
Cardion
14-Hydroxy-3β-(rhamnosyloxy)bufa-4,20,22-trienolide
Cardiovite
Prostosin
Proslladin
Solestril
Stellarid
proszin
proscillaridin-A
Talucard
Carmazon
Simeon
Procilan
5-[(3S,8R,9S,10R,13R,14S,17R)-14-Hydroxy-10,13-dimethyl-3-{[(2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy}-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]-2H-pyran-2-one
Talusin
5-[(3S,8R,9S,10R,13R,14S,17R)-14-Hydroxy-10,13-diméthyl-3-{[(2R,3R,4R,5R,6S)-3,4,5-trihydroxy-6-méthyltétrahydro-2H-pyran-2-yl]oxy}-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tétradécahydro-1H-cyclopenta[a]phénanthrén-17-yl]-2H-pyran-2-one
Procardin
Caradrine
Proscillan