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X Demographics
Mendeley readers
Attention Score in Context
| Title |
Structural Requirements for Potent Direct Inhibition of Human Cytochrome P450 1A1 by Cannabidiol: Role of Pentylresorcinol Moiety
|
|---|---|
| Published in |
Biological and Pharmaceutical Bulletin, January 2013
|
| DOI | 10.1248/bpb.b13-00183 |
| Pubmed ID | |
| Authors |
Satoshi Yamaori, Yoshimi Okushima, Kazufumi Masuda, Mika Kushihara, Takashi Katsu, Shizuo Narimatsu, Ikuo Yamamoto, Kazuhito Watanabe |
| Abstract |
Our recent work has shown that cannabidiol (CBD) exhibits the most potent direct inhibition of human cytochrome P450 1A1 (CYP1A1) among the CYP enzymes examined. However, the mechanism underlying this CBD inhibition remains to be clarified. Thus, to elucidate the structural requirements for the potent inhibition by CBD, the effects of CBD and its structurally related compounds on CYP1A1 activity were investigated with recombinant human CYP1A1. Olivetol, which corresponds to the pentylresorcinol moiety of CBD, inhibited the 7-ethoxyresorufin O-deethylase activity of CYP1A1; its inhibitory effect (IC50=13.8 µM) was less potent than that of CBD (IC50=0.355 µM). In contrast, d-limonene, which corresponds to the terpene moiety of CBD, only slightly inhibited CYP1A1 activity. CBD-2'-monomethyl ether (CBDM) and CBD-2',6'-dimethyl ether inhibited CYP1A1 activity with IC50 values of 4.07 and 23.0 µM, respectively, indicating that their inhibitory effects attenuated depending on the level of methylation on the free phenolic hydroxyl groups in the pentylresorcinol moiety of CBD. Cannabidivarin inhibited CYP1A1 activity, although its inhibitory potency (IC50=1.85 µM) was lower than that of CBD. The inhibitory effects of Δ(9)-tetrahydrocannabinol and cannabielsoin (IC50s ≈10 µM), which contain a free phenolic hydroxyl group and are structurally constrained, were less potent than that of CBDM, which contains a free phenolic hydroxyl group and is rotatable between pentylresorcinol and terpene moieties. These results suggest that the pentylresorcinol structure in CBD may have structurally important roles in direct CYP1A1 inhibition, although the whole structure of CBD is required for overall inhibition. |
X Demographics
The data shown below were collected from the profiles of 17 X users who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Japan | 6 | 35% |
| Georgia | 1 | 6% |
| Unknown | 10 | 59% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 15 | 88% |
| Scientists | 1 | 6% |
| Unknown | 1 | 6% |
Mendeley readers
The data shown below were compiled from readership statistics for 56 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United Kingdom | 2 | 4% |
| United States | 1 | 2% |
| Unknown | 53 | 95% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Master | 8 | 14% |
| Student > Bachelor | 8 | 14% |
| Researcher | 8 | 14% |
| Student > Ph. D. Student | 5 | 9% |
| Other | 3 | 5% |
| Other | 6 | 11% |
| Unknown | 18 | 32% |
| Readers by discipline | Count | As % |
|---|---|---|
| Agricultural and Biological Sciences | 9 | 16% |
| Pharmacology, Toxicology and Pharmaceutical Science | 6 | 11% |
| Biochemistry, Genetics and Molecular Biology | 6 | 11% |
| Medicine and Dentistry | 5 | 9% |
| Chemistry | 5 | 9% |
| Other | 6 | 11% |
| Unknown | 19 | 34% |
Attention Score in Context
This research output has an Altmetric Attention Score of 36. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 12 July 2019.
All research outputs
#966,224
of 23,049,027 outputs
Outputs from Biological and Pharmaceutical Bulletin
#21
of 2,973 outputs
Outputs of similar age
#8,536
of 282,297 outputs
Outputs of similar age from Biological and Pharmaceutical Bulletin
#2
of 91 outputs
Altmetric has tracked 23,049,027 research outputs across all sources so far. Compared to these this one has done particularly well and is in the 95th percentile: it's in the top 5% of all research outputs ever tracked by Altmetric.
So far Altmetric has tracked 2,973 research outputs from this source. They receive a mean Attention Score of 3.8. This one has done particularly well, scoring higher than 99% of its peers.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 282,297 tracked outputs that were published within six weeks on either side of this one in any source. This one has done particularly well, scoring higher than 96% of its contemporaries.
We're also able to compare this research output to 91 others from the same source and published within six weeks on either side of this one. This one has done particularly well, scoring higher than 98% of its contemporaries.