Castalagin and vescalagin purified from leaves of Syzygium samarangense (Blume) Merrill & L.M. Perry: Dual inhibitory activity against PARP1 and DNA topoisomerase II.

08:00 EDT 18th June 2018 | BioPortfolio

Summary of "Castalagin and vescalagin purified from leaves of Syzygium samarangense (Blume) Merrill & L.M. Perry: Dual inhibitory activity against PARP1 and DNA topoisomerase II."

Inhibition of poly(ADP-ribose) polymerase 1 (PARP1) is one of the most promising strategies for cancer chemotherapy, and a number of inhibitors possessing nicotinamide-like structures are being developed. To discover new types of PARP1 inhibitors, we screened a large number of substances of plant origin and isolated two inhibitory substances from the leaves of Syzygium samarangense (Blume) Merrill & L.M. Perry. The inhibitory substances were identified as vescalagin and its epimer castalagin by analyses using nuclear magnetic resonance and mass spectrometry. The IC of purified vescalagin and castalagin for PARP1 inhibition were 2.67 and 0.86 μM, respectively. Unlike most of synthetic PARP1 inhibitors, castalagin showed a mixed type inhibition, of which Ki was 1.64 μM. When SH-SY5Y cells were treated with these ellagitannins at concentrations of less than 5 μM, cellular poly(ADP-ribosyl)ation was obviously attenuated. Castalagin and vescalagin also possessed inhibitory activity against DNA topoisomerase II, implying that they function as dual inhibitors in cells.


Journal Details

This article was published in the following journal.

Name: Fitoterapia
ISSN: 1873-6971


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Medical and Biotech [MESH] Definitions

A plant genus in the family Myrtaceae. It is known for cloves, which is the flower bud of Syzygium aromaticum and is the source of an oil rich in EUGENOL.

A plant genus in the family MYRTACEAE, order Myrtales, subclass Rosidae. It is best known for cloves, which is the flower bud that is the source of an oil rich in EUGENOL. The botanical name has varied: Syzygium aromaticum (L.) Merr. & L. M. Perry = Eugenia caryophyllata Thunb. = Caryophyllus aromaticus L. The Eugenia-Syzygium name is discussed in Amer. J. Bot 59:423 1972.

Plant-derived ribosome-inactivating protein (RIP) purified from the Chinese medicinal herb tian-hua-fen which is obtained from the root tubers of Trichosanthes kirilowii. It has been used as an abortifacient and in the treatment of trophoblastic tumors. GLQ223 (Compound Q), a highly purified form of trichosanthin, has been proposed as antiviral treatment for AIDS.

An oil from flower buds of SYZYGIUM trees which contains large amounts of EUGENOL.

The burning of a small, thimble sized, smoldering plug of dried leaves on the SKIN at an ACUPUNCTURE point. Usually the plugs contain leaves of MUGWORT or moxa.

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