The DOI matches its Crossref record; 10 of the 10 references it cites were found in a registry or an index.
Inhibition of Cholesterol Synthesis in vitro and in vivo by ML‐236A and ML‐236B, Competitive Inhibitors of 3‐Hydroxy‐3‐methylglutaryl‐Coenzyme A Reductase
Abstract
1. ML‐236A and ML‐236B, potent inhibitors of 3‐hydroxy‐3‐methylglutaryl‐CoA reductase, were readily absorbed into the liver, the major site of cholesterogenesis, after oral administration in mice; peak concentration of these inhibitors in the liver, which were attained within 60 min after administration, were 4% of the dose for ML‐236A and 10% for ML‐236B, respectively. 2. ML‐236B reduced sterol synthesis from both [14 C]acetate and [14 C]octanoate in rat liver slices to 50% of control at a concentration of 0.05 μg/ml (0.12 μM) but not that from [14 C]mevalonate at higher concentrations up to 1.25 μg/ml. Inhibition of sterol synthesis was also observed in liver slices obtained from rats which had previously received this compound. 3. ML‐236B was also inhibitory in vivo to cholesterol synthesis in various tissues of rats in which [14 C]acetate was intraperitoneally injected to the animals and labeled digitonin‐precipitable sterols synthesized were isolated and determined. Sterol synthesis in the liver was far more strongly inhibited (over 90 % at 4h after oral administration of 50 mg/kg of ML‐236B) than that in other organs tested including kidney, lung, adrenal, spleen, and testis. 4. These findings strongly suggest that hypocholesterolemic activity of ML‐236A and ML‐236B is owing largely to specific inhibition of hepatic cholesterol synthesis.
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Cites
PROTEIN MEASUREMENT WITH THE FOLIN PHENOL REAGENT
Lowry, O., Rosebrough, N., Farr, A. L., & Randall, R. (1951) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(19)52451-6 · Cited by 317,331
ML-236A, ML-236B, and ML-236C, new inhibitors of cholesterogensis produced by Penicillium citrinum.
ENDO, A., KURODA, M., & TSUJITA, Y. (1976) · The Journal of Antibiotics · doi:10.7164/antibiotics.29.1346 · Cited by 954
Self-citationEndo, A., Kuroda, M., & Tanzawa, K. (1976) · FEBS Letters · doi:10.1016/0014-5793(76)80996-9 · Cited by 794
Self-citationRegulation of HMG-CoA Reductase
RODWELL, V. W., NORDSTROM, J. L., & MITSCHELEN, J. J. (1976) · Advances in Lipid Research · doi:10.1016/b978-0-12-024914-5.50008-5 · Cited by 746
Bischoff, K. B., Dedrick, R. L., Zaharko, D. S., & Longstreth, J. A. (1971) · Journal of Pharmaceutical Sciences · doi:10.1002/jps.2600600803 · Cited by 480
Regulation of Cholesterol Metabolism
Dietschy, J. M., & Wilson, J. D. (1970) · New England Journal of Medicine · doi:10.1056/nejm197005142822005 · Cited by 361
Regulation of Cholesterol Metabolism
Dietschy, J. M., & Wilson, J. D. (1970) · New England Journal of Medicine · doi:10.1056/nejm197005212822105 · Cited by 337
Regulation of Cholesterol Biosynthesis in Normal and Malignant Tissues
(1970) · Current Topics in Cellular Regulation · doi:10.1016/b978-0-12-152802-7.50009-8 · Cited by 227
Regulation of Cholesterol Metabolism
Dietschy, J. M., & Wilson, J. D. (1970) · New England Journal of Medicine · doi:10.1056/nejm197005282822206 · Cited by 148
Inhibition of in vitro cholesterol synthesis by fatty acids
Masao, K., & Endo, A. (1977) · Biochimica et Biophysica Acta (BBA) - Lipids and Lipid Metabolism · doi:10.1016/0005-2760(77)90071-6 · Cited by 88
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Cited by
CNS synaptogenesis promoted by glia-derived cholesterol
Mauch, D. H., Nägler, K., Schumacher, S., Göritz, C., Müller, E.-C., Otto, A., & Pfrieger, F. W. (2001) · Science · doi:10.1126/science.294.5545.1354 · Cited by 1,711
Alberts, A. W., Chen, J., Kuron, G., Hunt, V, Huff, J., Hoffman, C., Rothrock, J., Lopez, M., Joshua, H., Harris, E., et al. (1980) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.77.7.3957 · Cited by 1,628
The Methylation Effect in Medicinal Chemistry
Barreiro, E. J., Kümmerle, A. E., & Fraga, C. A. M. (2011) · Chemical Reviews · doi:10.1021/cr200060g · Cited by 1,017
The discovery and development of HMG-CoA reductase inhibitors.
Endo, A. (1992) · Journal of Lipid Research · doi:10.1016/s0022-2275(20)41379-3 · Cited by 847
Self-citationBilheimer, D. W., Grundy, S. M., Brown, M. S., & Goldstein, J. L. (1983) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.80.13.4124 · Cited by 557
Metadata
- Authors
- ENDO, A., TSUJITA, Y., KURODA, M., & TANZAWA, K.
- Venue
- European Journal of Biochemistry
- Publisher
- Wiley
- Published
- 1977-07
- Volume
- 77
- Issue
- 1
- Pages
- 31-36
- ISSN
- 0014-2956 (ISSN-L)
- 1432-1033
- OpenAlex
- W2053770173
- Cited by
- 262
- References
- 10
- FWCI
- 9.80
- Type
- journal article
- Language
- en
- Open access
- closed
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- CoChat. (2026). Citation check: Inhibition of Cholesterol Synthesis in vitro and in vivo by ML‐236A and ML‐236B, Competitive Inhibitors of 3‐Hydroxy‐3‐methylglutaryl‐Coenzyme A Reductase. https://app.cochat.ai/papers/10.1111/j.1432-1033.1977.tb11637.x
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- ENDO, A., TSUJITA, Y., KURODA, M., & TANZAWA, K. (1977). Inhibition of Cholesterol Synthesis in vitro and in vivo by ML‐236A and ML‐236B, Competitive Inhibitors of 3‐Hydroxy‐3‐methylglutaryl‐Coenzyme A Reductase. European Journal of Biochemistry. https://doi.org/10.1111/j.1432-1033.1977.tb11637.x
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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