The pharmacology and pharmacokinetics of the retinoids

Allen, John G.; Bloxham, David P.

doi:10.1016/0163-7258(89)90071-5

Cited by 71 publications

(42 citation statements)

References 80 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…This need may be ascribed to the presence of serum in the culture medium and of albumin in the salt solution used for the aggregation assay (see Materials and methods). Albumin is known to bind RA as it serves as its carrier protein in the blood (Allen and Bloxham, 1989). Our co-immunoprecipitation data failed to demonstrate an effect of RA on the composition of the E-cadherin/catenin complex.…”

Section: Discussioncontrasting

confidence: 46%

Activation of the E-cadherin/catenin complex in human MCF-7 breast cancer cells by all-trans-retinoic acid

Vermeulen

Bruyneel²,

Roy³

et al. 1995

Br J Cancer

View full text Add to dashboard Cite

Summary All-trans-retinoic acid (RA), like insulin-like growth factor I (IGF-I) and tamoxifen, inhibit invasion of human MCF-7/6 mammary cancer cells in vitro. For tamoxifen and for IGF-I, activation of the invasion-suppressor function of the E-cadherin/catenin complex was shown to be the most probable mechanism of the anti-invasive action. We did a series of experiments to determine whether the anti-invasive effect of RA also implicated the invasion-suppressor E-cadherin/catenin complex. Human MCF-7/6 mammary and HCT-8/R1 colon cancer cells, both with a dysfunctional E-cadherin/catenin complex, were treated with RA and the function of the complex was evaluated through Ca2+-dependent fast aggregation. Fast aggregation of both MCF-7/6 and HCT-8/RI cells was induced by 1 gtM RA. This effect was abolished by antibodies against E-cadherin. RA-induced fast aggregation was not sensitive to cycloheximide, tyrosine kinase inhibitors or antibodies against IGF-I or against the IGF-I receptor. RA did not stimulate IGF-I receptor phosphorylation or alter the E-cadherin/catenin complex, as evidenced by immunoprecipitation. RA up-regulates the function of the invasion-suppressor complex E-cadherin/catenin. Its action mechanism is different from that of IGF-I. RA may act as an anti-invasive agent with unique mechanisms of action.

show abstract

Section: Discussioncontrasting

confidence: 46%

Activation of the E-cadherin/catenin complex in human MCF-7 breast cancer cells by all-trans-retinoic acid

Vermeulen

Bruyneel²,

Roy³

et al. 1995

Br J Cancer

View full text Add to dashboard Cite

show abstract

“…In some patients, 13-cis-RA use produces side effects similar to those described for hypervitaminosis A (Allen and Bloxham, 1989). Frequently reported blood chemistry abnormalities in 13-cis-RA users include elevated levels of triglycerides, cholesterol, apolipoprotein B, calcium and creatine kinase activity as well as hyperglycemia (Barth et al, 1993;Fex et al, 1996;Stoll et al, 2004) and some of these effects are apparent within a few days of treatment onset (Stoll et al, 2004).…”

Section: Introductionmentioning

confidence: 93%

Serum levels of albumin, triglycerides, total protein and glucose in rats are altered after oral treatment with low doses of 13-cis-retinoic acid or all-trans-retinoic acid

Cisneros¹,

Gough²,

Patton³

et al. 2005

J. Appl. Toxicol.

View full text Add to dashboard Cite

Currently used to treat severe acne, 13-cis-retinoic acid (13-cis-RA) is under investigation for its anticancer effects as is the isomer, all-trans-retinoic acid (all-trans-RA). Here, the effects of oral 13-cis-RA or all-trans-RA treatment on serum chemistry, leptin and adiponectin levels were evaluated. Adult Sprague-Dawley rats were gavaged once daily for 7 consecutive days with 13-cis-RA (7.5 or 15 mg kg(-1)), all-trans-RA (10 or 15 mg kg(-1)) (n=24/sex/dose), or soy oil (n=16/sex) and blood was sampled 30-480 min after the last gavage. The body weight was unaffected; however, the liver/body weight ratios were increased by both doses of all-trans-RA. Sex differences were noted for levels of cholesterol, creatine, triglycerides, albumin, alanine aminotransferase and total protein. Both doses of all-trans-RA reduced albumin levels to approximately 90% of the control and total protein levels to approximately 93% of the control while substantially elevating triglyceride levels to approximately 66%-99% above the control. Additionally, triglyceride levels of the 15 mg kg(-1) 13-cis RA group were approximately 62% higher than the controls and total protein levels were approximately 5% less. Glucose levels were affected by sex and RA treatment in that males treated with 15 mg kg(-1) of 13-cis-RA or 10 mg kg(-1) all-trans-RA had lower (13%-19%) levels than the same-sex controls; however, females were not similarly affected. Neither 13-cis-RA nor all-trans-RA treatment had significant effects on the levels of blood urea nitrogen, aspartate amino transferase, leptin or adiponectin. On a mg kg(-1) basis, all-trans-RA was more potent than 13-cis-RA. These results replicate previous findings of RA-induced increased triglyceride levels. Additionally, several new findings indicate there may be sex-specific effects of RA treatment. Finally, neither treatment appeared to alter the typical diurnal cycles of these endpoints.

show abstract

“…Topical retinoids like Acitretin (Act) or 13 cis-trans retinoic acid is a metabolite of vitamin A. Possible mechanism is to inhibit the keratinocyte hyperproliferation and differentiation, but it has gained great potential due to its multitude of physiological effects such as regulation of epithelial cell growth and differentiation, sebum production and collagen synthesis [44]. Oral Acitretin is indicated for severe psoriasis, but its use is restricted due to systemic side effects and teratogenicity.…”

Section: Topical Treatmentmentioning

confidence: 99%

Classical to Current Approach for Treatment of Psoriasis: A Review

Rahman¹,

Alam²,

Ahmad³

et al. 2012

EMIDDT

100

View full text Add to dashboard Cite

Psoriasis is a genetic predisposition with T-cell mediated autoimmune inflammatory skin disorder, characterized by cutaneous inflammation, increased epidermal proliferation, hyperkeratosis, angiogenesis, and abnormal keratinization that affects up to 2 - 3% of the population worldwide. Common therapies that are used for the treatment of psoriasis include topical, systemic, phototherapy, combination, herbal therapy and novel molecules. Topically used agents include Vit D, calcipotriol, corticosteroids, dithranol and retinoids etc. Systemically used agents include methotrexate and cyclosporine etc. Phototherapy includes UV-B, Psoralen plus ultraviolet therapy and excimer laser etc. These therapies have a number of potential problems, such as limited in efficacy, inconvenience, organ toxicity, carcinogenic and broadband immunosuppression. In natural treatment a variety of natural agents such as methanolic extracts of duzhong (Eucommia ulmoides Oliv.), yerba mate (Ilex paraguariensis,) linseed oil, fish oil, and Indigo naturalis etc., that modulates T cell and cytokine action at various steps along with the pathogenic sequence have been developed. But till now there is no more in vivo, dose and its efficacy data has been established. Current therapy includes biologicals, small molecules inhibitor and enzyme inhibitors etc, which serve as novel therapeutic options for psoriasis treatment. All these avoid the side effects of the prebiologically developed systemic agents including hepatotoxicity, nephrotoxicity, and bone marrow suppression. Currently, Denilukin diftitox, Efalizumab, Alefacept, Ustekinumab and Etanercept are approved by the FDA, and others molecules are at clinical stage. Patents issued by the US office are also included in current psoriasis treatment scenario. In the United States, biologicals are widely used for moderate-to-severe psoriasis. But because of the high cost of medication and their availability in injection form, it remains to be seen how widely these agents will be utilized worldwide. Still, developing countries prefer conventional drugs.

show abstract

The pharmacology and pharmacokinetics of the retinoids

Cited by 71 publications

References 80 publications

Activation of the E-cadherin/catenin complex in human MCF-7 breast cancer cells by all-trans-retinoic acid

Activation of the E-cadherin/catenin complex in human MCF-7 breast cancer cells by all-trans-retinoic acid

Serum levels of albumin, triglycerides, total protein and glucose in rats are altered after oral treatment with low doses of 13-cis-retinoic acid or all-trans-retinoic acid

Classical to Current Approach for Treatment of Psoriasis: A Review

Contact Info

Product

Resources

About