Theoretical Evaluation of Twenty-Cannabinoid Derivatives on Either Androgen Receptor or 5&amp;alpha;-Reductase Enzyme

María, López-Ramos; Figueroa‐Valverde, Lauro; Díaz-Cedillo, Francisco; Marcela, Rosas-Nexticapa; Alvarez-Ramirez, Magdalena

doi:10.51847/5myimtzexf

Cited by 3 publications

(2 citation statements)

References 46 publications

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“…Most of the patients initially responding to ADT will eventually develop castrate resistance. It seems that a protein called TRAF4 is responsible for this conversion of androgen-sensitive prostate cancer cells into castration-resistant cells; TRAF4 is frequently overexpressed in advanced prostate cancers [134]. Most intriguingly, a very recent study demonstrated in silico that theoretically CBD, its acid CBDA, and THC could act as androgen receptor (AR) inhibitors whereas CBDV and cannabinodiol (a natural derivative of CBN produced by photochemical conversion) could act as 5α-reductase inhibitors among other minor phytocannabinoids [135].…”

Section: Prostate Cancermentioning

confidence: 99%

Treatment of malignant diseases with phytocannabinoids: promising observations in animal models and patients

Nahler

2023

Exploration of Medicine

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Amazingly, almost 50 years after the first demonstration of anticancer effects of cannabinoids in vitro and in vivo, well-designed clinical trials that definitively prove tumour-inhibiting effects in man are still missing. Whereas a large number of preclinical studies exist that describe tumour-inhibiting effects of cannabinoids, alone or in combination, but also in the form of medical cannabis or natural extracts in vitro, the number of in vivo studies is still limited. Even more limited are well-documented experiences in man. Most animal studies and experience with cannabinoids in man concern brain tumours. This review summarises the effects of phytocannabinoids in brain, breast, colorectal, head and neck, haematological, liver, lung, pancreatic, ovarian, prostate, and skin cancers in animal models and, if available, in patients. The large majority of animal studies demonstrate tumour-inhibiting effects of cannabinoids, thus confirming in vitro data. Experiences in cancer patients are almost exclusively limited to individual case reports and case series without a control group. Many questions are currently unanswered such as the role of pure cannabinoids compared to combinations, cannabinoids as the eventual sole cancer therapy, optimal dosages, or duration of treatment. Pure cannabidiol (CBD) seems to be superior to pure delta-9-tetrahydrocannabinol (THC) in experimental settings. The role of medical cannabis or extracts is less clear as they vary in their phytochemical composition. In conclusion, cannabis/cannabinoids may slow the progression of tumours. However, the hope that cannabinoids could eventually cure cancer as often spread in social media, is, at present, wishful thinking. Above all, well-designed clinical trials paired with long-term follow-up of cancer patients are needed.

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Section: Prostate Cancermentioning

confidence: 99%

Treatment of malignant diseases with phytocannabinoids: promising observations in animal models and patients

Nahler

2023

Exploration of Medicine

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“…Other report indicate that BCR-ABL (transcript encodes a tyrosine kinase) gene mutations are associated with different forms of leukaemia (Zhang et al, 2016). In addition, some studies suggest that either androgen receptor or 5α-reductase enzyme are two factors associated to prostate cancer (Sowalsky et al, 2022;Lopez-Ramos et al, 2023).…”

Section: Introductionmentioning

confidence: 99%

Evaluation of coumarin and their derivatives as Janus Kinase-3 inhibitors using a theoretical model

et al. 2023

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For several years, cancer has increased in the population, being one of the main causes of death worldwide. This clinical pathology is associated with the activation/release of various biomolecules, including the Janus kinase family (JAKs). It is important to mention that some studies indicate that some JAK inhibitors (ruxolitinib and tofacitinib) may have a significant effect on some autoimmune diseases and cancer; however, some of these drugs can produce secondary effects such as herpes zoster, infectious, acute respiratory distress and others. The aim of this study was to evaluate the interaction of coumarin and its derivatives (compounds 2 to 24) with the JAK-3 surface. In this way, the Interaction of coumarin and their derivatives with JAK-3 was determined using the 3pjc protein and either decernotinib or tofacitinib drugs as theoretical tools on DockinServer program. The results showed differences in the aminoacid residues involved in the interaction of coumarin and their derivatives with 3pjc protein surface compared with decernotinib and tofacitinib. Besides, the inhibition constant (Ki) for coumarin derivatives 7, 9 and 10 was lower compared with tofacitinib. However, Ki was lower for 2, 5, 7, 8, 9, 10, and 24 compared with decernotinib. In conclusion, the coumarin derivatives 2, 5, 7, 8, 9, 10, and 24 could be good alternatives as JAK-3 inhibitors to decrease cancer cells growth.

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Physiological Changes for Rabbits Infected with S. aureus by Using Pharmaceutical Compounds and Plant Extracts as Treatments

Fudllalah,

El-Tahtawi,

Ghanem

2023

Pharmacophore

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Theoretical Evaluation of Twenty-Cannabinoid Derivatives on Either Androgen Receptor or 5α-Reductase Enzyme

Cited by 3 publications

References 46 publications

Treatment of malignant diseases with phytocannabinoids: promising observations in animal models and patients

Treatment of malignant diseases with phytocannabinoids: promising observations in animal models and patients

Evaluation of coumarin and their derivatives as Janus Kinase-3 inhibitors using a theoretical model

Physiological Changes for Rabbits Infected with S. aureus by Using Pharmaceutical Compounds and Plant Extracts as Treatments

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