Drug development, Brazilian biodiversity and political choices: Where are we heading?

Ferreira, Paulo Michel Pinheiro; Arcanjo, Daniel Dias Rufino; Perón, Ana Paula

doi:10.1080/10937404.2023.2193762

Cited by 44 publications

(7 citation statements)

References 119 publications

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“…The identification of pharmacologically active compounds from plants and other natural sources and the determination of mechanism(s) of action are the main challenges for the development of pharmaceutical chemistry and breaking down pharmacokinetic barriers [14,35,36].…”

Section: Discussionmentioning

confidence: 99%

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Promising Effects of Casearins in Tumor-Bearing Mice and Antinociceptive Action against Oncologic Pain: Molecular Docking and In Vivo Findings

Silva,

Beserra Filho,

Acha

et al. 2024

Pharmaceuticals

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Safer analgesic drugs remain a hard challenge because of cardiovascular and/or gastrointestinal toxicity, mainly. So, this study evaluated in vivo the antiproliferative actions of a fraction with casearins (FC) from Casearia sylvestris leaves against human colorectal carcinomas and antihyperalgesic effects on inflammatory- or opiate-based pain relief and oncologic pain in Sarcoma 180 (S180)-bearing mice. Moreover, docking investigations evaluated the binding among Casearin X and NMDA(N-methyl-D-aspartate)-type glutamate receptors. HCT-116 colorectal carcinoma-xenografted mice were treated with FC for 15 days. Antinociceptive assays included chemically induced algesia and investigated mechanisms by pharmacological blockade. Intraplantar region S180-bearing animals received a single dose of FC and were examined for mechanical allodynia and behavior alterations. AutoDock Vina determined molecular interactions among Cas X and NMDA receptor subunits. FC reduced tumor growth at i.p. (5 and 10 mg/kg) and oral (25 mg/kg/day) doses (31.12–39.27%). FC reduced abdominal pain, as confirmed by formalin and glutamate protocols, whose antinociception activity was blocked by naloxone and L-NAME (neurogenic phase) and naloxone, atropine, and flumazenil (inflammatory phase). Meanwhile, glibenclamide potentiated the FC analgesic effects. FC increased the paw withdrawal threshold without producing changes in exploratory parameters or motor coordination. Cas X generated a more stable complex with active sites of the NMDA receptor GluN2B subunits. FC is a promising antitumor agent against colorectal carcinomas, has peripheral analgesic effects by desensitizing secondary afferent neurons, and inhibits glutamate release from presynaptic neurons and/or their action on cognate receptors. These findings emphasize the use of clerodane diterpenes against cancer-related pain conditions.

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Section: Discussionmentioning

confidence: 99%

“…In this context, natural products have been used as a source of novel anticancer [12][13][14] and antinociceptive [15] agents. Among them, Casearia (Salicaceae) comprises about 180 species distributed in sub-tropical and tropical regions [16] and has promising anticancer effects [17][18][19].…”

Section: Introductionmentioning

confidence: 99%

Promising Effects of Casearins in Tumor-Bearing Mice and Antinociceptive Action against Oncologic Pain: Molecular Docking and In Vivo Findings

Silva,

Beserra Filho,

Acha

et al. 2024

Pharmaceuticals

Self Cite

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“…Fortunately, the reservoir of medicinal flora houses biologically active compounds endowed with therapeutic properties, extensively documented and employed by diverse communities for addressing a spectrum of ailments [ 14 ]. As per the Brazilian Fund for Biodiversity (FUNBIO), the botanical wealth in Brazil encompasses around 55,000 described species, constituting 22% of the global total [ 15 ]. Within arid forests akin to those witnessed in the Cerrado, plant species manifest a profusion of polyphenolic compounds, notably featuring flavonoids, which have been the subject of considerable scientific interest in the fight against neglected diseases [ 16 , 17 , 18 ].…”

Section: Introductionmentioning

confidence: 99%

Design of Liquid Formulation Based on F127-Loaded Natural Dimeric Flavonoids as a New Perspective Treatment for Leishmaniasis

da Costa,

Marques,

do Nascimento

et al. 2024

Pharmaceutics

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Infectious and Parasitic Diseases (IPD) remain a challenge for medicine due to several interconnected reasons, such as antimicrobial resistance (AMR). American tegumentary leishmaniasis (ATL) is an overlooked IPD causing persistent skin ulcers that are challenging to heal, resulting in disfiguring scars. Moreover, it has the potential to extend from the skin to the mucous membranes of the nose, mouth, and throat in both humans and various animals. Given the limited effectiveness and AMR of current drugs, the exploration of new substances has emerged as a promising alternative for ATL treatment. Arrabidaea brachypoda (DC). Bureau is a native Brazilian plant rich in dimeric flavonoids, including Brachydin (BRA), which displays antimicrobial activity, but still little has been explored regarding the development of therapeutic formulations. In this work, we present the design of a low-cost liquid formulation based on the use of Pluronic F127 for encapsulation of high BRA concentration (LF-B500). The characterization techniques revealed that BRA-loaded F127 micelles are well-stabilized in an unusual worm-like form. The in vitro cytotoxicity assay demonstrated that LF-B500 was non-toxic to macrophages but efficient in the inactivation of forms of Leishmania amazonensis promastigotes with IC50 of 16.06 µg/mL. The results demonstrated that LF-B500 opened a new perspective on the use of liquid formulation-based natural products for ATL treatment.

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“…Brazil is home to one of the world’s largest biodiversities, accounting for approximately 15 to 20% of the global biological diversity, and it is at the top among 17 megadiverse countries in the world [ 1 ]. Furthermore, it contains two biodiversity hotspots (the Atlantic Forest and the Cerrado biomes) and is the second country in terms of the richness of endemic species, second only to Indonesia [ 2 ].…”

Section: Introductionmentioning

confidence: 99%

Non-Thermal Supercritical Carbon Dioxide Processing Retains the Quality Parameters and Improves the Kinetic Stability of an Araticum Beverage Enriched with Inulin-Type Dietary Fibers

Arruda

Silva

Pastore

et al. 2023

Foods

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Fruit-based beverages have been considered excellent food vehicles for delivering prebiotics. However, the conventional thermal processes currently used to microbiologically and enzymatically stabilize these products may cause significant losses in their sensory, physicochemical, nutritional, and bioactive characteristics. Thus, in this study, we evaluate the effect of different levels of pressure (8, 15, and 21 MPa) and temperature (35 and 55 °C) on the characteristics of an inulin-enriched araticum beverage processed with non-thermal supercritical carbon dioxide (SC–CO2) technology. The temperature showed a significant effect on total soluble solids, pH, particle size distribution, and kinetic stability. In contrast, pressure affected only the particle size distribution. The interaction between pressure and temperature influenced the total soluble solids, pH, and particle size distribution. Color parameters, ζ-potential, and glucose and fructose contents were not modified after all SC–CO2 treatments. Moreover, the SC–CO2 treatments preserved the inulin molecular structure, thus maintaining its prebiotic functionality. Overall, the SC–CO2 treatment did not alter the sensory, nutritional, and functional quality of the beverage, while improving its physical stability during storage. Therefore, non-thermal SC–CO2 treatment can be an alternative to current conventional processes for stabilizing inulin-enriched fruit-based beverages.

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Drug development, Brazilian biodiversity and political choices: Where are we heading?

Cited by 44 publications

References 119 publications

Promising Effects of Casearins in Tumor-Bearing Mice and Antinociceptive Action against Oncologic Pain: Molecular Docking and In Vivo Findings

Promising Effects of Casearins in Tumor-Bearing Mice and Antinociceptive Action against Oncologic Pain: Molecular Docking and In Vivo Findings

Design of Liquid Formulation Based on F127-Loaded Natural Dimeric Flavonoids as a New Perspective Treatment for Leishmaniasis

Non-Thermal Supercritical Carbon Dioxide Processing Retains the Quality Parameters and Improves the Kinetic Stability of an Araticum Beverage Enriched with Inulin-Type Dietary Fibers

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