β-Caryophyllene (BCP), a natural bicyclic sesquiterpene, is a selective phytocannabinoid agonist of type 2 receptors (CB2-R). It isn’t psychogenic due to the absence of an affinity to cannabinoid receptor type 1 (CB1). Among the various biological activities, BCP exerts anti-inflammatory action via inhibiting the main inflammatory mediators, such as inducible nitric oxide synthase (iNOS), Interleukin 1 beta (IL-1β), Interleukin-6 (IL-6), tumor necrosis factor-alfa (TNF-α), nuclear factor kapp a-light-chain-enhancer of activated B cells (NF-κB), cyclooxygenase 1 (COX-1), cyclooxygenase 2 (COX-2). Peroxisome proliferator-activated receptors alpha (PPAR-α) effects are also mediated by the activation of PPAR-α and PPAR-γ receptors. In detail, many studies, in vitro and in vivo, suggest that the treatment with β-caryophyllene improves the phenotype of animals used to model various inflammatory pathologies, such as nervous system diseases (Parkinson’s disease, Alzheimer’s disease, multiple sclerosis, amyotrophic lateral sclerosis, stroke), atherosclerosis, and tumours (colon, breast, pancreas, lymphoma, melanoma and glioma cancer). Furthermore, pre-clinical data have highlighted that BCP is potentially useful in Streptococcus infections, osteoporosis, steatohepatitis, and exerts anticonvulsant, analgesic, myorelaxing, sedative, and antidepressive effects. BCP is non-toxic in rodents, with a Lethal dose, 50% (LD50) greater than 5000 mg/kg. Nevertheless, it inhibits various cytochrome P450 isoforms (above all, CYP3A4), which metabolise xenobiotics, leading to adverse effects, due to drug levels over therapeutic window. All the reported data have highlighted that both pharmacological and toxicological aspects need to be further investigated with clinical trials.
Molecular recognition is a useful property shared by various molecules, such as antibodies, aptamers and molecularly imprinted polymers (MIPs). It allows these molecules to be potentially involved in many applications including biological and pharmaceutical research, diagnostics, theranostics, therapy and drug delivery. Antibodies, naturally produced by plasma cells, have been exploited for this purpose, but they present noticeable drawbacks, above all production cost and time. Therefore, several research studies for similar applications have been carried out about MIPs and the main studies are reported in this review. MIPs, indeed, are more versatile and cost-effective than conventional antibodies, but the lack of toxicity studies and their scarce use for practical applications, make it that further investigations on this kind of molecules need to be conducted.
Cancer represents one of the major causes of mortality worldwide; indeed, 19.3 million new cases and almost 10.0 million deaths were estimated last year. Among the different type of cancers, malignant melanoma represents the most aggressive and deadly skin cancer. Unfortunately, the long-term efficacy of melanoma treatments is limited by the lack of clinical efficacy, onset of side effects and resistance. The latter is a major obstacle for the success of the melanoma therapy; thus, the exploration of new potent and safer anticancer agents is of great importance. Recently, numerous plant species, used for therapeutic purposes and containing various non-toxic nutraceuticals have been widely studied. Herein, we investigated the antioxidant and anticancer properties on melanoma cells of the ethanolic, methanolic and aqueous Annona cherimola leaf extracts (ACE, ACM and ACW, respectively). The ethanolic extract showed higher anticancer activity, mostly against the malignant A2058 melanoma cell line (IC50 = 5.6 ± 0.8 ng/mL), together with a very low activity on the normal cells. It blocks the melanoma cells migration process, and induces a clear disorganization of cytoskeleton, triggering cell apoptosis. Finally, some bioactive compounds were identified in the studied extracts.
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