Page last updated: 2024-12-10

mezerein

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

mezerein: toxic component of plant Daphne mezereum with anti-leukemic activity against P-388 & P-1210 in mice; can act as a tumor promoter; RN given refers to (12beta(E,E))-isomer; structure [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

FloraRankFlora DefinitionFamilyFamily Definition
DaphnegenusA plant genus of the family THYMELAEACEAE. They are evergreen shrubs much cultivated in garden borders and rock gardens in mild climates. Members contain mezerein, flavonoids, and COUMARINS such as daphnetin and daphnin.[MeSH]ThymelaeaceaeA plant family of the order Myrtales, subclass Rosidae, class Magnoliopsida. They are mainly trees and shrubs. Many members contain mucilage and COUMARINS.[MeSH]
Daphne mezereumspecies[no description available]ThymelaeaceaeA plant family of the order Myrtales, subclass Rosidae, class Magnoliopsida. They are mainly trees and shrubs. Many members contain mucilage and COUMARINS.[MeSH]

Cross-References

ID SourceID
PubMed CID5281382
CHEMBL ID126750
CHEBI ID6918
MeSH IDM0057504

Synonyms (6)

Synonym
SMP2_000004 ,
C09134 ,
34807-41-5
mezerein
chebi:6918 ,
CHEMBL126750 ,

Research Excerpts

Overview

Mezerein is a PKC activator that exhibits antileukemic properties. It is a good second-stage promoter of papillomas, and an effective promoter of carcinomas.

ExcerptReferenceRelevance
"Mezerein is a PKC activator that exhibits antileukemic properties."( Differential activation by daphnetoxin and mezerein of PKC-isotypes alpha, beta I, delta and zeta.
Fresco, P; Gonçalves, J; Pinto, E; Portugal, H; Saraiva, L, 2001
)
1.29
"Mezerein is a good second-stage promoter of papillomas, an inefficient complete promoter of papillomas, and an effective promoter of carcinomas."( Comparison of octahydromezerein and mezerein as protein kinase C activators and as mouse skin tumor promoters.
Blumberg, PM; Hennings, H; Sharkey, NA; Yuspa, SH, 1989
)
1.31

Effects

Mezerein has been described as a weak complete tumor promoter but an effective stage II promoter in the mouse skin initiation-promotion tumor model. MezereIn appears to be a weaker tumor promoter than PMA.

ExcerptReferenceRelevance
"Mezerein (MEZ) has been described as a weak complete tumor promoter but an effective stage II promoter in the mouse skin initiation-promotion tumor model. "( Morphological transformation of Syrian hamster embryo cells by mezerein.
Spalding, JW; Tennant, RW; Tu, AS, 1992
)
1.97
"Mezerein has similarly been reported to have potent inflammatory properties but appears to be a weaker tumor promoter than PMA."( The effects of the anti-tumor agent mezerein on the cytotoxic capacity and oxidative metabolism of human blood cells.
Barton, K; Randall, G; Sagone, AL, 1989
)
1.27

Toxicity

ExcerptReferenceRelevance
"1 to 100 microM), involved a temperature-dependent process, could not be mimicked by addition of hematopoietic growth factors, and was not related to neutralization of toxic or inhibitory substances in high-density medium."( In vitro effects of bryostatin 1 on the metabolism and cytotoxicity of 1-beta-D-arabinofuranosylcytosine in human leukemia cells.
Boise, L; Grant, S; Howe, C; McCrady, C; Pettit, GR; Turner, A; Westin, E, 1991
)
0.28

Dosage Studied

OHM for inducing a comparable degree of acute and chronic hyperplasia to that induced by mezerein was 3- to 10-fold higher. In the same system, 4-O-methyl-phorbol myristate acetate (4- O-Me-PMA) and mezmerein were approximately 50 times less active than PMA.

ExcerptRelevanceReference
" The number of colonies which developed during promoter exposure in cocultures showed a dose-response curve which differed from the dose-response curve for stimulation of growth of 308 colonies in the absence of normal keratinocytes."( Development of an in vitro analogue of initiated mouse epidermis to study tumor promoters and antipromoters.
Hennings, H; Jung, R; Michael, DM; Pettit, GR; Robinson, VA; Yuspa, SH, 1990
)
0.28
" The dosage of OHM for inducing a comparable degree of acute and chronic hyperplasia to that induced by mezerein was 3- to 10-fold higher."( Comparison of octahydromezerein and mezerein as protein kinase C activators and as mouse skin tumor promoters.
Blumberg, PM; Hennings, H; Sharkey, NA; Yuspa, SH, 1989
)
0.8
" In the same system, dose-response studies demonstrated that 4-O-methyl-phorbol myristate acetate (4-O-Me-PMA) and mezerein were approximately 50 times less active than PMA, while phorbol dibutyrate (PDB), phorbol diacetate (PDA), phorbol and the calcium ionophore A23187 did not cause an increase in the number of formazan-positive PECs at the doses used."( Tumor promoters differ in their ability to stimulate superoxide anion radical production by murine peritoneal exudate cells following in vivo administration.
Czerniecki, BJ; Witz, G, 1989
)
0.49
" sn-1,2-Didecanoylglycerol was evaluated as a complete skin tumor promoter in CD-1 mice utilizing a dosing regimen demonstrated to produce epidermal hyperplasia."( Synthetic lipid second messenger sn-1,2-didecanoylglycerol: a complete tumor promoter in mouse skin.
Conney, AH; Hansen, LA; Mills, KJ; Smart, RC, 1989
)
0.28
" Inhibition by topical retinoic acid of ODC induction by TPA was partially overcome in a dose-response fashion by PGE."( The role of prostaglandin E1 in ornithine decarboxylase induction by tumor promoters.
Boutwell, RK; Cleaveland, JS; Ordman, AB; Simsiman, RC, 1986
)
0.27
" Dose-response studies revealed that a cervical carcinoma (HeLa), a melanoma (A375Ag5), and several mammary carcinoma cell lines (MCF-7, BT474, MDA-MB415, and T47D) were growth inhibited by this conditioned medium."( Production of growth-inhibitory activity in serum-free medium by human monocytic leukemia cells.
Dell'Aquila, ML; Gaffney, EV; Lingenfelter, SE; Tsai, SC, 1983
)
0.27
" This study illustrates that PGE2 dose-response curves may reflect different mechanisms of action that may be intimately associated with skin irritant and tumour promoting activity."( Comparison of tumour promoter-induced prostaglandin E2 release in human and rat keratinocytes.
Benford, DJ; Lawrence, JN, 1995
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
diterpenoidAny terpenoid derived from a diterpene. The term includes compounds in which the C20 skeleton of the parent diterpene has been rearranged or modified by the removal of one or more skeletal atoms (generally methyl groups).
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (1)

Assay IDTitleYearJournalArticle
AID144651Inhibition of cell growth in NCI panel of 60 human carcinoma lines2001Journal of medicinal chemistry, Nov-08, Volume: 44, Issue:23
Iridals are a novel class of ligands for phorbol ester receptors with modest selectivity for the RasGRP receptor subfamily.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (341)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990157 (46.04)18.7374
1990's117 (34.31)18.2507
2000's20 (5.87)29.6817
2010's28 (8.21)24.3611
2020's19 (5.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.41

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index23.41 (24.57)
Research Supply Index5.86 (2.92)
Research Growth Index4.59 (4.65)
Search Engine Demand Index29.35 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.41)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews10 (2.87%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other339 (97.13%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]