Natural products in drug discovery: advances and opportunities

Natural products and their structural analogues have historically made a major contribution to pharmacotherapy, especially for cancer and infectious diseases. Nevertheless, natural products also present challenges for drug discovery, such as technical barriers to screening, isolation, characterization and optimization, which contributed to a decline in their pursuit by the pharmaceutical industry from the 1990s onwards. In recent years, several technological and scientific developments — including improved analytical tools, genome mining and engineering strategies, and microbial culturing advances — are addressing such challenges and opening up new opportunities. Consequently, interest in natural products as drug leads is being revitalized, particularly for tackling antimicrobial resistance. Here, we summarize recent technological developments that are enabling natural product-based drug discovery, highlight selected applications and discuss key opportunities

The International Natural Product Sciences Taskforce (INPST) and the power of Twitter networking exemplified through #INPST hashtag analysis

Background: The development of digital technologies and the evolution of open innovation approaches have enabled the creation of diverse virtual organizations and enterprises coordinating their activities primarily online. The open innovation platform titled "International Natural Product Sciences Taskforce" (INPST) was established in 2018, to bring together in collaborative environment individuals and organizations interested in natural product scientific research, and to empower their interactions by using digital communication tools. Methods: In this work, we present a general overview of INPST activities and showcase the specific use of Twitter as a powerful networking tool that was used to host a one-week "2021 INPST Twitter Networking Event" (spanning from 31st May 2021 to 6th June 2021) based on the application of the Twitter hashtag #INPST. Results and Conclusion: The use of this hashtag during the networking event period was analyzed with Symplur Signals (https://www.symplur.com/), revealing a total of 6,036 tweets, shared by 686 users, which generated a total of 65,004,773 impressions (views of the respective tweets). This networking event's achieved high visibility and participation rate showcases a convincing example of how this social media platform can be used as a highly effective tool to host virtual Twitter-based international biomedical research events

Cannabinoids for the Treatment of Schizophrenia: An Overview

Cannabinoids are found to be very useful in psychiatry because of their antipsychotic properties suggesting a therapeutic use as neuroleptic agents in limiting psychotic diseases. Cannabinoids treatments are both able to reduce the typical symptoms of schizophrenia and to slow down the disease aggravation. In the present review, we reported recent studies supporting the idea that the cannabinoid system may modulate the activity of the striatum and temporal cortex linked to psychosis and schizophrenia. Furthermore, anatomical, electrophysiological, pharmacological and biochemical data suggest that the psychotic disorders related to the impaired cannabinoid system may lead to the development of novel compounds that selectively target specific elements of the cannabinoid system

Behavioral effects of 2,3-dihydro- and oxoisoaporphine derivatives in post stroke-depressive like behavior in male BALB/c mice.

In this study, antidepressant-like effects of intra-cerebroventricularly administration of oxoisoaporphine derivatives in post stroke-depressive like behavior were examined through despair swimming and tail suspension models. For this aim, acute ischemic stroke was induced by bilateral common carotid arteries occlusion which significantly changed the normal behaviors of male balb/c mice. We performed stroke-induced anhedonia test as a key result of post strokedepressive like behavior by determination of sucrose consumption. Results show that some 2,3-dihydro- and oxoisoaporphine derivatives modified the abnormality in the behaviors through decreasing in the immobility time in tail suspension and despair swimming models and increasing in the swimming and climbing times in despair swimming model. We concluded that these alkaloids showed antidepressant actions and therefore can be used for treatment of post strokedepressive like behavior in acute ischemic stroke patient

Flavonoids And Dementia: An Update.

Dementia is a strongly age-related syndrome due to cognitive decline that can be considered a typical example of the combination of physiological and pathological aging-associated changes occurring in old people; it ranges from intact cognition to mild cognitive impairment, which is an intermediate stage of cognitive deterioration, and dementia. The spread of this syndrome has induced to study and try to reduce dementia modifiable risk factors. They include insulin resistance and hyperinsulinaemia, high blood pressure, obesity, smoking, depression, cognitive inactivity or low educational attainment as well as physical inactivity and incorrect diet, which can be considered one of the most important factors. One emerging strategy to decrease the prevalence of mild cognitive impairment and dementia may be the use of nutritional interventions. In the last decade, prospective data have suggested that high fruit and vegetable intakes are related to improved cognitive functions and reduced risks of developing a neurodegenerative process. The protective effects against neurodegeneration could be in part due to the intake of flavonoids that have been associated with several health benefits such as antioxidant and anti-inflammatory activities, increased neuronal signaling, and improved metabolic functions. The present article is aimed at reviewing scientific studies that show the protective effects of flavonoid intake against mild cognitive impairment and dementia

Spectroscopic and photochemical properties of some annulated boldine derivatives

The aim of this study was to determine the influence of the substituent groups on the photostability of eight boldine derivatives, including some oxazole and oxazinone derivatives, in order to increase the sunscreen protection properties previously demonstrated for boldine. Such derivatives showed bands similar to those of boldine in the absorption and emission spectrum. The spectroscopic properties are pH dependent. The photostability of the derivative compounds was higher than that of boldine, in accordance with the low value of the photoconsumption quantum yield determined. The low fluorescence quantum yield values observed for boldine 1 and 4 as both base and hydrochloride derivative compounds led us to postulate that these compounds are deactivated by a mechanism different to the fluorescence pathway, probably due to the electron-withdrawing inductive effect of NO for boldine 1, and to the increase of the aromatic framework for boldine 4. © 2010 Sociedade Brasileira de Química