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Improving Prostamide Anti-Cancer Activity Through Derivatization and Micellar Delivery.

Record Type:	Language materials, manuscript : Monograph/item
Title/Author:	Improving Prostamide Anti-Cancer Activity Through Derivatization and Micellar Delivery./
Author:	Halatek, David.
Description:	1 online resource (60 pages)
Notes:	Source: Masters Abstracts International, Volume: 84-12.
Contained By:	Masters Abstracts International84-12.
Subject:	Biochemistry. -
Online resource:	click for full text (PQDT)
ISBN:	9798379744434

Improving Prostamide Anti-Cancer Activity Through Derivatization and Micellar Delivery.
Halatek, David.

Improving Prostamide Anti-Cancer Activity Through Derivatization and Micellar Delivery. - 1 online resource (60 pages)

Source: Masters Abstracts International, Volume: 84-12.

Thesis (M.S.)--East Carolina University, 2023.

Includes bibliographical references

Colorectal cancer is the fourth most common cancer diagnosis per year as well as the fourth highest rate of death per year according to the Centers for Disease Control. Approximately 1/3rd of the diagnosed colorectal cancer cases per year will result in death. Prior research from our group has shown that the prostaglandin-ethanolamide 15-deoxy, Δ12,14 prostamide J2 (15d-Δ12,14-PMJ2) is selectively toxic to murine melanoma cells (B16F10) and murine colorectal cells (CT-26) both in vitro and in vivo and significantly reduces tumor growth. Further, 15d-Δ12,14-PMJ2 induces cell death in primary patient melanoma cells and thus may be a promising therapeutic. As 15d-Δ12,14-PMJ2 can be made by the condensation of ethanolamine with 15-deoxy, Δ12,14 prostaglandin J2 (15d-Δ12,14-PGJ2), we sought to test the cytotoxicity of other prostamide derivatives to determine the structural features required for activity. Based on prior results in a study of related prodrugs, 15d-Δ12,14-PMJ2-Arvanil was selected as the top candidate for testing anti-cancer activity. After testing in both a human and murine cell line, it was determined that 15d-Δ12,14-PMJ2-Arvanil was not as cytotoxic as 15d-Δ12,14-PMJ2. It is possible that the bulkier functional group on the α-chain of the prostamide prevents transport into the cell the same way or to the same degree 15d-Δ12,14-PMJ2 enters. In an effort to test this hypothesis, and to develop an improved means for systemic delivery for this class of hydrophobic prostamides, engineered micelles composed of 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000] and D-α-tocopherol polyethylene glycol 1000 succinate were investigated as drug carriers.

Electronic reproduction.
Ann Arbor, Mich. :
ProQuest,
2024

Mode of access: World Wide Web

ISBN: 9798379744434Subjects--Topical Terms:

582831
Biochemistry.
Subjects--Index Terms:

Cancer therapeuticsIndex Terms--Genre/Form:

554714
Electronic books.

Improving Prostamide Anti-Cancer Activity Through Derivatization and Micellar Delivery.
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520 $a Colorectal cancer is the fourth most common cancer diagnosis per year as well as the fourth highest rate of death per year according to the Centers for Disease Control. Approximately 1/3rd of the diagnosed colorectal cancer cases per year will result in death. Prior research from our group has shown that the prostaglandin-ethanolamide 15-deoxy, Δ12,14 prostamide J2 (15d-Δ12,14-PMJ2) is selectively toxic to murine melanoma cells (B16F10) and murine colorectal cells (CT-26) both in vitro and in vivo and significantly reduces tumor growth. Further, 15d-Δ12,14-PMJ2 induces cell death in primary patient melanoma cells and thus may be a promising therapeutic. As 15d-Δ12,14-PMJ2 can be made by the condensation of ethanolamine with 15-deoxy, Δ12,14 prostaglandin J2 (15d-Δ12,14-PGJ2), we sought to test the cytotoxicity of other prostamide derivatives to determine the structural features required for activity. Based on prior results in a study of related prodrugs, 15d-Δ12,14-PMJ2-Arvanil was selected as the top candidate for testing anti-cancer activity. After testing in both a human and murine cell line, it was determined that 15d-Δ12,14-PMJ2-Arvanil was not as cytotoxic as 15d-Δ12,14-PMJ2. It is possible that the bulkier functional group on the α-chain of the prostamide prevents transport into the cell the same way or to the same degree 15d-Δ12,14-PMJ2 enters. In an effort to test this hypothesis, and to develop an improved means for systemic delivery for this class of hydrophobic prostamides, engineered micelles composed of 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-2000] and D-α-tocopherol polyethylene glycol 1000 succinate were investigated as drug carriers.
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653 $a J-series prostaglandins
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