13 documents found, page 1 of 2

An Exemestane Derivative, Oxymestane-D1, as a New Multi-Target Steroidal Aromat...

Around 70-85% of all breast cancer (BC) cases are estrogen receptor-positive (ER+). The third generation of aromatase inhibitors (AIs) is the first-line treatment option for these tumors. Despite their therapeutic success, they induce several side effects and resistance, which limits their efficacy. Thus, it is crucial to search for novel, safe and more effective anti-cancer molecules. Currently, multi-target d...

Phytocannabinoids Pharmaceutical Potential

Cannabis sativa L. is a plant used for therapeutic purposes, although it is widely known for its potential abuse. This plant can produce more than 500 chemical substances, including 100 different phytocannabinoids. These substances can act directly in a specific receptor and/or interact with the endocannabinoid system, regulating physiological effects such as analgesia, muscle relaxation, immunosuppression or a...

The endocannabinoid 2-arachidonoylglycerol promotes endoplasmic reticulum stres...

Proliferation, differentiation and apoptosis of trophoblast cells are required for normal placental development. Impairment of those processes may lead to pregnancy-related diseases. Disruption of endoplasmic reticulum (ER) homeostasis has been associated with several reproductive pathologies including recurrent pregnancy loss and preeclampsia. In the unfolded protein response (UPR), specific ER-stress signalli...

Synthetic cannabinoids JWH-018, JWH-122, UR-144 and the phytocannabinoid THC ac...

The increasing use of synthetic cannabinoids (SCBs) in recreational settings is becoming a new paradigm of drug abuse. Although SCBs effects mimic those of the Cannabis sativa plant, these drugs are frequently more potent and hazardous. It is known that endocannabinoid signalling plays a crucial role in diverse reproductive events such as placental development. Moreover, the negative impact of the phytocannabin...

Cannabis and cannabinoids for medical use

Cannabis derivatives, like other natural products, have been used for medicinal purposes for millennia. Although the advent of molecular biology and computational chemistry has reduced the use of natural products as a source of therapeutic agents, nature continues to influence the emergence of new drug candidates. Cannabis and its products (hashish, marijuana) contain more than 500 compounds, including more tha...

Role of autophagy, apoptosis and oxidative stress in the toxicity of β-keto amp...

Methylone and MDPV activate autophagy in human dopaminergic SH-SY5Y cells: a ne...

Autophagy has an essential role in neuronal homeostasis and its dysregulation has been recently linked to neurotoxic effects of a growing list of psychoactive drugs, including amphetamines. However, the role of autophagy in β-keto amphetamine (β-KA) designer drugs-induced neurotoxicity has hitherto not been investigated. In the present study, we show that two commonly abused cathinone derivatives, 3,4-methylene...

Insights into the Synthesis of Steroidal A-Ring Olefins

one (5), from the D1-3-keto enone, (5a,17b)-3-oxo-5-androst-1-en-17-yl acetate (1), through a strategy involving the reaction of D1-3-hydroxy allylic alcohol, 3b-hydroxy-5a-androst-1-en-17b-yl acetate (2), with SOCl2 , was revisited in order to prepare and biologically evaluate 5 as aromatase inhibitor for breast cancer treatment. Surprisingly, the followed strategy also afforded the isomeric D2-olefin 6 as a b...

New steroidal 17b-carboxy derivatives present anti-5a-reductase activity and an...

The androgens testosterone (T) and dihydrotestosterone (DHT), besides playing an important role in prostate development and growth, are also responsible for the development and progression of benign prostate hyperplasia (BPH) and prostate cancer. Therefore, the actions of these hormones can be antagonized by preventing the irreversible conversion of T into DHT by inhibiting 5a-reductase (5a-R). This has been a ...

Apoptosis and autophagy in breast cancer cells following exemestane treatment

Aromatase inhibitors (AIs), which block the conversion of androgens to estrogens, are used for hormone-dependent breast cancer treatment. Exemestane, a steroidal that belongs to the third-generation of AIs, is a mechanism-based inhibitor that binds covalently and irreversibly, inactivating and destabilizing aromatase. Since the biological effects of exemestane in breast cancer cells are not totally understood, ...