2020-08-09
Seabra Ferreira, Heloisa Athaydes, Séllos Zorszin, Amanda Louize Rickli, Gouvêa, Isabela Torres, Oda, Caroline Mari Ramos, Duarte, Jaqueline Aparecida, Silva, Juliana de Oliveira, Silva, Izabella Thaís, de Barros, André Luis Branco, Leite, Elaine Amaral
Seabra Ferreira, Heloisa Athaydes ; Séllos Zorszin, Amanda Louize Rickli ; Gouvêa, Isabela Torres ; Oda, Caroline Mari Ramos ; Duarte, Jaqueline Aparecida ; Silva, Juliana De Oliveira ; Silva, Izabella Thaís ; De Barros, André Luis Branco ; Leite, Elaine Amaral ; Paclitaxel (PTX) and cisplatin (CDDP) are potent cytotoxic drugs that target distinct intracellular pathways employed together for breast cancer therapy. While studies indicate enhanced treatment efficacy with drug combinations, the concomitant rise in adverse effects remains a concern. This study assessed the potential of co-administration of these drugs encapsulated into pH-sensitive liposomes (SpHL) against a murine triple-negative breast cancer model. The cytotoxicity studies revealed a concentration-dependent relationship between drug concentration and cell viability for both drugs. The combination effect of free drugs at IC50 and IC50x2 showed an additive effect, while co-treatment with SpHL-PTX:SpHL-CDDP at IC50x4 (1:3 molar ratio) displayed strong synergism (CI = 0.52). Other combinations exhibited antagonism (CI > 2.0). In vivo studies were performed at PTX:CDDP 1:3 molar ratio in two regimen protocols: single or dual dose protocol, resulting in different cumulative doses. Tumor growth was significantly decreased when two doses of free or encapsulated drugs were used compared to single-dose administration. Notably, encapsulated dual-dose treatments demonstrated enhanced antitumor efficacy, diminished systemic toxicity, and zero mortality. In conclusion, our study underscores the promising potential of co-administering encapsulated drugs into SpHL, highlighting their superior efficacy and reduced toxicity in breast cancer treatment compared to free drugs.
2020-08-09
Quecán, Beatriz Ximena Valencia, Lima, Emília Maria França, Almeida, Felipe Alves de, Bueris, Vanessa, Tahrioui, Ali, Pinto, Uelinton Manoel
Quecán, Beatriz Ximena Valencia ; Lima, Emília Maria França ; Almeida, Felipe Alves De ; Bueris, Vanessa ; Tahrioui, Ali ; Pinto, Uelinton Manoel ; Microbial biofilms are ubiquitous and highly successful forms of life. Among them, species found in food industries often include human pathogens like Salmonella spp., a significant concern due to its ability to adapt and survive in diverse environmental stresses. This bacterium is a major global public health issue, causing foodborne illnesses with considerable morbidity and economic costs. Combatting bacteria within biofilms necessitates novel strategies, and recent research highlights natural compounds as promising agents due to their antibiofilm, antivirulence, and antimicrobial properties. Specifically, plant-derived compounds have shown potential to modulate biofilm formation either alone or in combination with other substances. This review provides a comprehensive overview of Salmonella biofilms, encompassing their development, composition, resistance mechanisms, and tolerance mechanisms. It focuses particularly on the inhibition of these biofilms by plant-derived compounds.
2020-08-09
Chen, Chushan, Chen, Haoming, Xie, Juntao, Chen, Yi, Yu, Xin, Fan, Hongxia, Huang, Jiajin, Lu, Huiqin, Zheng, Junxia
Chen, Chushan ; Chen, Haoming ; Xie, Juntao ; Chen, Yi ; Yu, Xin ; Fan, Hongxia ; Huang, Jiajin ; Lu, Huiqin ; Zheng, Junxia ; Inflammation is a condition in which the body’s immune system is compromised. Polysaccharides from Mesona chinensis Benth have been shown to repair the immune system and inhibit inflammation. This study aimed to investigate the activities, network pharmacology, and potential mechanisms of action against inflammation of a homogeneous polysaccharide, MCP-1, from M. chinensis. MCP-1 was isolated and purified using water extraction, alcohol precipitation, the Sevag method, and column chromatography. The molecular weight of MCP-1 was determined to be 70.9kDa. The polysaccharide composition included glucose (39.05%), arabinose (18.31%), galactose (14.80%), galacturonic acid (13.98%), xylose (7.42%), mannose (4.14%), and glucuronic acid (2.30%). MCP-1 showed strong inhibitory effects on the release of NO, IL-6, and TNF-α (30.79 ± 4.13%, 30.51 ± 3.25%, and 37.25 ± 3.57%, respectively). A total of 169 targets were identified based on the monosaccharide structures of MCP-1, with 9 targets associated with inflammation, including TLR4, STAT3, MMP9, COL18A1, TLR9, ABCB1, PPARA, MMP2, and NR1H4. The principal targets for anti-inflammatory therapies were associated with various signaling pathways involved in cancer and immune responses. Molecular docking experiments revealed that MCP-1 exhibited a high binding affinity for MMP2.
2020-08-09
Silva, Taízia Dutra, Ribeiro, Ana Carolina Guimarães, Gonçalves, Raquel Braga Dutra, Resende, Jackson Antonio Lamounier Camargos, Vianna-Soares, Cristina Duarte
Silva, Taízia Dutra ; Ribeiro, Ana Carolina Guimarães ; Gonçalves, Raquel Braga Dutra ; Resende, Jackson Antonio Lamounier Camargos ; Vianna-Soares, Cristina Duarte ; Pulmonary arterial hypertension (PAH) is a severe disease responsible for high mortality in the affected population. Due to the limitations in treatment as severe adverse effects, high cost, we aimed to develop a simple therapeutic option for pulmonary administration, using a vasodilator sildenafil citrate (SILC) in a dry powder inhalation using lactose as carrier. A formulation of micronized SILC was prepared after 30 min wet grinding of the active with the aid of a vibration shear-mill. Solid characterization by laser diffraction and X-ray powder diffraction was assessed for active. Performance tests such as delivered-dose uniformity (DDU) and aerodynamic particle size distribution (APSD), using Dosage Unit Sampling Apparatus and Andersen Cascate Impactor, respectively, were performed. The micronization of SILC resulted in a medium size of 4.54 μm and a 50th percentile of 2.93 μm. For DDU, the total amount delivered ranged from 92.42 to 109.05% of the targeted dose, in agreement with the specified range (75.0-125.0%). For ASPD, a fine particle fraction of 35% was satisfactorily obtained. This formulation is simple and promising therapeutic option for the treatment of PAH with the advantage of being easily produced using less complex carrier matrix or equipment, in a short time.
2020-08-09
Bandeira, Sara Raquel de Moura, Lima, Camila Maria Batista, Reis-Filho, Antônio Carlos dos, Oliveira, Lucas Solyano Almeida de, Gonçalves, Rodrigo Lopes Gomes, Rezende, Diana Carvalho de, Nunes, Daniel Barbosa, Pinheiro Neto, Flaviano Ribeiro, Trindade, Gabriela do Nascimento Caldas, Sousa Neto, Benedito Pereira de, Gomes, Bruno da Silva, Barros, Rômulo Oliveira, Ramos, Ricardo Martins, Medeiros, Maria das Graças Freire de, Almeida, Fernanda Regina de Castro, Lucarini, Massimo, Durazzo, Alessandra, Arcanjo, Daniel Dias Rufino, Oliveira, Francisco de Assis
Bandeira, Sara Raquel De Moura ; Lima, Camila Maria Batista ; Reis-Filho, Antônio Carlos Dos ; Oliveira, Lucas Solyano Almeida De ; Gonçalves, Rodrigo Lopes Gomes ; Rezende, Diana Carvalho De ; Nunes, Daniel Barbosa ; Pinheiro Neto, Flaviano Ribeiro ; Trindade, Gabriela Do Nascimento Caldas ; Sousa Neto, Benedito Pereira De ; Gomes, Bruno Da Silva ; Barros, Rômulo Oliveira ; Ramos, Ricardo Martins ; Medeiros, Maria Das Graças Freire De ; Almeida, Fernanda Regina De Castro ; Lucarini, Massimo ; Durazzo, Alessandra ; Arcanjo, Daniel Dias Rufino ; Oliveira, Francisco De Assis ; Atopic dermatitis is a chronic skin condition characterized by impaired barrier function and underlying inflammation. Monoterpenes, a diverse class of secondary metabolites commonly found in essential oils, have been extensively documented for their potent anti-inflammatory properties. Therefore, this study evaluated the effects of gamma-terpinene (GT) on dinitrochlorobenzene (DNCB)-induced atopic dermatitis in a murine model. Macroscopic and histopathological analyses were conducted to assess skin lesions and ear edema, along with the assessment of serum immunoglobulin E (IgE), lactate dehydrogenase (LDH), and inflammatory cytokines (IL-4, IL-6, IL-1β, and TNF-α) in skin tissues. Histopathological analysis revealed a reduction in skin thickness, spongiosis, inflammatory cell infiltration, along with the presence of blisters and vesicles in both the epidermis and dermis. Additionally, cellular disarrangement and dermal fibrosis were observed. GT significantly decreased ear edema, serum IgE, and LDH levels, along with the expression of tissue IL-4, IL-6, IL-1β, and TNF-α. Therefore, the potential anti-inflammatory response induced by GT in atopic dermatitis suggests its potential for the development of GT-based therapies for chronic inflammatory skin disorders.
2020-08-09
Adebisi, Iyabo Mobolawa, Suleiman, Abdullahi, Ugwah-Oguejiofor, Chinenye Jane, Fajobi, Sunday Joseph, Jega, Amina Yusuf, Umar, Mohammed
Adebisi, Iyabo Mobolawa ; Suleiman, Abdullahi ; Ugwah-Oguejiofor, Chinenye Jane ; Fajobi, Sunday Joseph ; Jega, Amina Yusuf ; Umar, Mohammed ; Peptic ulcer is a common disease in gastroenterology clinics. This study aimed to investigate the chemical composition, antiulcer, and antioxidant activities of methanol extract of Dioscorea praehensilis rhizomes. The rhizomes were extracted by macerating in 80% methanol and subjected to chemical profiling using Gas Chromatography-Mass Spectrometry (GC-MS). The assessment of anti-ulcer activity was done using ethanol and indomethacin-induced gastric ulcer models in rats while the antioxidant studies were conducted using quantitative analysis of phenolic (total phenols and total flavonoid) compounds, 1,1-diphenyl-2-picrylhydrazyl (DPPH), total antioxidant capacity (TAC) and ferric ion reducing antioxidant power (FRAP) assays. D. praehensilis extracts at 125, 250, and 500 mg/kg ‘per os’ (PO) exhibited a significant (p<0.01) dose-dependent decrease in gastric lesions with the percentage inhibition of 65.16, 68.20, and 79.64% respectively in the ethanol model and 81.89, 90.44, and 95.35% in the indomethacin model compared with the control group. D. praehensilis extract contained high phenolic and flavonoid content. The extract also showed considerable antioxidant activity in the DPPH, TAC and FRAP assays. Furthermore, D. praehensilis contains bioactive constituents such as Pentadecanoic acid, 9-Eicosene, n-Hexadecanoic acid, 4-tert-butylphenol and Pentacosane. In conclusion, D. praehensilis possesses antiulcer and antioxidant activity, supporting its traditional use in treating ulcers and dyspepsia.