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1.
Int J Pharm ; 642: 123206, 2023 Jul 25.
Artículo en Inglés | MEDLINE | ID: mdl-37419432

RESUMEN

Improved therapies for inflammatory bowel diseases are sorely needed. Novel therapeutic agents and the development of controlled release systems for targeted tissue delivery are interesting approaches to overcome these barriers. We investigated the activity of trans-chalcone (T) in acetic acid-induced colitis in mice and developed, characterized, and determined the therapeutic effect of pectin/casein polymer microcapsules containing T (MT) in a colitis mouse model. In vitro, compound release was achieved in simulated intestinal fluid but not in the simulated gastric fluid. In vivo, since T at the dose of 3 mg/kg but not 0.3 mg/kg ameliorated colitis, we next tested the effects of MT at 0.3 mg/kg (non-effective dose). MT, but not free T at 0.3 mg/kg, significantly improved colitis outcomes such as neutrophil recruitment, antioxidant capacity, cytokine production, and NF-kB activation. This translated into reduced macro and microscopic damage in the colon. T release from the microcapsules is mediated by a pH-dependent and pectinase-regulated mechanism that provide controlled and prolonged release of T. Moreover, MT lowered the required dose for T therapeutic effect, indicating that could be a suitable pharmaceutical approach to colitis treatment. This is the first demonstration that T or MT is effective at reducing the signs of colitis.


Asunto(s)
Chalcona , Chalconas , Colitis , Ratones , Animales , Caseínas , Chalcona/farmacología , Cápsulas/farmacología , Pectinas , Colitis/inducido químicamente , Colitis/tratamiento farmacológico , Colon , FN-kappa B , Modelos Animales de Enfermedad
2.
Photochem Photobiol Sci ; 20(8): 1033-1051, 2021 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-34297334

RESUMEN

Cordia verbenacea DC (Boraginaceae) is a flowering shrub found along the Brazilian Atlantic Forest, Brazilian coast, and low areas of the Amazon. The crude extract of its leaves is widely used in Brazilian folk medicine as an anti-inflammatory, both topically and orally. The aim of this study is to evaluate the activity of C. verbenacea ethanolic leaves extract (CVE) against UVB-triggered cutaneous inflammation and oxidative damage in hairless mice. CVE treatment recovered cutaneous antioxidant capacity demonstrated by scavenging ABTS+ free radical and iron-reducing antioxidant potential evaluated by FRAP. CVE also controlled the following UV-triggered events in the skin: reduced glutathione (GSH) depletion, catalase activity decrease, and superoxide anion (O⋅-) build-up. Furthermore, mice treated with CVE exhibited less inflammation, shown by the reduction in COX-2 expression, TNF-α, IL-1ß, IL-6, edema, and neutrophil infiltration. CVE also regulated epidermal thickening and sunburn cells, reduced dermal mast cells, and preserved collagen integrity. The best results were obtained using 5% CVE-added emulsion. The present data demonstrate that topical administration of CVE presents photochemoprotective activity in a mouse model of UVB inflammation and oxidative stress. Because of the intricate network linking inflammation, oxidative stress, and skin cancer, these results also indicate the importance of further studies elucidating a possible role of C. verbenacea in the prevention of UVB-induced skin cancer and evaluating a potential synergy between CVE and sunscreens in topical products against UVB damaging effects to the skin.


Asunto(s)
Cordia/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Piel/efectos de los fármacos , Piel/efectos de la radiación , Rayos Ultravioleta/efectos adversos , Administración Tópica , Animales , Emulsiones , Ratones , Estrés Oxidativo/efectos de los fármacos , Extractos Vegetales/administración & dosificación , Hojas de la Planta/química , Piel/metabolismo , Protectores Solares/administración & dosificación , Protectores Solares/química , Protectores Solares/farmacología
3.
J Photochem Photobiol B ; 216: 112151, 2021 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-33581679

RESUMEN

Photochemoprotection of the skin can be achieved by inhibiting inflammation and oxidative stress, which we tested using Cordia verbenacea extract, a medicinal plant known for its rich content of antioxidant molecules and anti-inflammatory activity. In vitro antioxidant evaluation of Cordia verbenacea leaves ethanolic extract (CVE) presented the following results: ferric reducing antioxidant power (886.32 µM equivalent of Trolox/g extract); IC50 of 19.128 µg/ml for scavenging 2,2-diphenyl-1-picrylhydrazyl; IC50 of 12.48 µg/mL for scavenging 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid); decrease of hydroperoxides from linoleic acid (IC50 of 10.20 µg/mL); inhibition of thiobarbituric acid reactive substances (IC50 8.90 µg/mL); iron-chelating ability in bathophenanthroline iron assay (IC50 47.35 µg/mL); chemiluminescence triggered by free radicals in the H2O2/horseradish peroxidase/luminol (IC50 0.286 µg/mL) and xanthine/xanthine oxidase/luminol (IC50 0.42 µg/mL) methods. CVE (10-100 mg per kg, 30 min before and immediately after UVB exposure) treatment was performed by gavage in hairless mice. CVE inhibited skin edema, neutrophil infiltration, and overproduction of MMP-9; reduced levels of TNF-α, IL-1ß, and IL- 6; numbers of skin mast cells, epidermal thickening, number of epidermal apoptotic keratinocytes, and collagen degradation. CVE increased the skin's natural antioxidant defenses as observed by Nrf-2, NAD(P)H quinone oxidoreductase 1, and heme oxygenase 1 mRNA expression enhancement. Furthermore, CVE inhibited lipid peroxidation and superoxide anion production and recovered antioxidant reduced glutathione, catalase activity, and ROS scavenging capacity of the skin. Concluding, CVE downregulates the skin inflammatory and oxidative damages triggered by UVB, demonstrating its potentialities as a therapeutic approach.


Asunto(s)
Antiinflamatorios/química , Antioxidantes/química , Cordia/química , Extractos Vegetales/química , Hojas de la Planta/química , Sustancias Protectoras/química , Animales , Antiinflamatorios/farmacología , Antioxidantes/farmacología , Citocinas/metabolismo , Edema/metabolismo , Femenino , Hemo-Oxigenasa 1/metabolismo , Humanos , Peróxido de Hidrógeno/química , Ácido Linoleico/química , Peroxidación de Lípido , Ratones Pelados , Factor 2 Relacionado con NF-E2/metabolismo , Estrés Oxidativo/efectos de los fármacos , Estrés Oxidativo/efectos de la radiación , Extractos Vegetales/farmacología , Sustancias Protectoras/farmacología , Quinona Reductasas/metabolismo , Piel/efectos de la radiación , Superóxidos/metabolismo , Rayos Ultravioleta
4.
Inflammopharmacology ; 28(6): 1663-1675, 2020 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-32141011

RESUMEN

Evidence demonstrates the pronounced anti-inflammatory activity of a beetroot (Beta vulgaris) dye enriched in betalains obtained using precipitation with ethanol. Herein, we expand upon our previous observations and demonstrate the analgesic and antioxidant effect of betalains. Betalains [10-1000 mg/kg; intraperitoneal route (i.p.)] diminished acetic acid- and PBQ-induced abdominal contortions, and the overt pain-like behaviour induced by complete Freund`s adjuvant (CFA) and formalin (intraplantar; i.pl.) injection. Moreover, betalains (100 mg/kg) administered by various routes [i.p. or subcutaneous (s.c.)] or as a post-treatment reduced carrageenin- or CFA-induced hyperalgesia. Mechanistically, betalains mitigated carrageenin-induced tumour necrosis factor-alpha (TNF-α), interleukin (IL)-1ß, superoxide anion levels, and lipid peroxidation. Betalains also stopped the depletion of reduced glutathione (GSH) levels and ferric reducing ability produced by carrageenin, as well as upregulated Nrf2 and Ho1 transcript expression in the plantar tissue of mice. Furthermore, betalains showed hydroxyl radical, 2,2'-azino-di-(3-ethylbenzthiazoline-6-sulphonic acid) radical (ABTS+), and 2,2-diphenyl-1-picryl-hydrazyl radical (DPPH•) scavenging ability and iron-chelating activity (bathophenantroline assay), and inhibited iron-independent and iron-dependent lipid peroxidation (LPO) in vitro. Finally, betalains-treated bone marrow-derived macrophages exhibited lower levels of cytokines (TNF-α and IL-1ß), and superoxide anion levels and nuclear factor kappa B (NF-κB) activation following lipopolysaccharide (LPS) stimulation. Therefore, this betalain-rich dye extracted using a novel precipitation approach presents prominent analgesic effect in varied models of pain by mechanisms targeting cytokines and oxidative stress.


Asunto(s)
Analgésicos/farmacología , Antiinflamatorios/farmacología , Beta vulgaris/química , Betalaínas/farmacología , Inflamación/tratamiento farmacológico , Animales , Carragenina/farmacología , Citocinas/metabolismo , Modelos Animales de Enfermedad , Hiperalgesia/tratamiento farmacológico , Hiperalgesia/metabolismo , Inflamación/inducido químicamente , Inflamación/metabolismo , Interleucina-1beta/metabolismo , Lipopolisacáridos/farmacología , Macrófagos/efectos de los fármacos , Macrófagos/metabolismo , Masculino , Ratones , Ratones Endogámicos C57BL , Factor 2 Relacionado con NF-E2/metabolismo , FN-kappa B/metabolismo , Estrés Oxidativo/efectos de los fármacos , Dolor/inducido químicamente , Dolor/metabolismo , Superóxidos/metabolismo
5.
Scientifica (Cairo) ; 2016: 8656397, 2016.
Artículo en Inglés | MEDLINE | ID: mdl-27293981

RESUMEN

Tephrosia toxicaria, which is currently known as Tephrosia sinapou (Buc'hoz) A. Chev. (Fabaceae), is a source of compounds such as flavonoids. T. sinapou has been used in Amazonian countries traditional medicine to alleviate pain and inflammation. The purpose of this study was to evaluate the analgesic effects of T. sinapou ethyl acetate extract in overt pain-like behavior models in mice by using writhing response and flinching/licking tests. We demonstrated in this study that T. sinapou extract inhibited, in a dose (1-100 mg/kg) dependent manner, acetic acid- and phenyl-p-benzoquinone- (PBQ-) induced writhing response. Furthermore, it was active via intraperitoneal, subcutaneous, and peroral routes of administration. T. sinapou extract also inhibited formalin- and complete Freund's adjuvant- (CFA-) induced flinching/licking at 100 mg/kg dose. In conclusion, these findings demonstrate that T. sinapou ethyl acetate extract reduces inflammatory pain in the acetic acid, PBQ, formalin, and CFA models of overt pain-like behavior. Therefore, the potential of analgesic activity of T. sinapou indicates that it deserves further investigation.

6.
Arch Pharm Res ; 38(4): 494-504, 2015 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-25173360

RESUMEN

We have recently developed betalain-rich beetroot (Beta vulgaris) dye (betalain) to be used in food products. Betalain (30-300 mg/kg) intraperitoneal (i.p.) treatment diminished carrageenan (100 µg/paw)-induced paw edema and neutrophil migration to the paw skin tissue. Betalain (100 mg/kg) treatment by subcutaneous or per oral routes also inhibited the carrageenan-induced paw edema. Importantly, the post-treatment with betalain (100 mg/kg, i.p.) significantly inhibited carrageenan- and complete Freund's adjuvant (10 µl/paw)-induced paw edema. Betalain (100 mg/kg) also reduced carrageenan (500 µg/cavity)-induced recruitment of total leukocytes, including mononuclear cells and neutrophils, as well as increasing vascular permeability in the peritoneal cavity. Furthermore, betalain significantly reduced carrageenan-induced superoxide anion, tumor necrosis factor-alpha (TNF-α) and interleukin (IL)-1ß levels in the peritoneal fluid, as well as augmenting IL-10 levels. Therefore, this compound presents prominent anti-inflammatory effect on carrageenan-induced paw edema and peritonitis by reducing the production of superoxide anion and the cytokines TNF-α and IL-1ß, in addition to increasing IL-10 levels. These results suggest that betalain shows therapeutic potential that could be utilized in the treatment of inflammation-associated diseases.


Asunto(s)
Antiinflamatorios/uso terapéutico , Betalaínas/uso terapéutico , Citocinas/antagonistas & inhibidores , Edema/tratamiento farmacológico , Leucocitos/efectos de los fármacos , Superóxidos/antagonistas & inhibidores , Animales , Antiinflamatorios/farmacología , Beta vulgaris , Betalaínas/farmacología , Citocinas/biosíntesis , Edema/patología , Leucocitos/metabolismo , Masculino , Ratones , Superóxidos/metabolismo , Resultado del Tratamiento
7.
AAPS PharmSciTech ; 15(1): 86-95, 2014 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-24249253

RESUMEN

Pimenta pseudocaryophyllus is a Brazilian native plant that presents high concentrations of flavonoids and other polyphenolic compounds. Herein, we evaluated: (1) the chemical properties of P. pseudocaryophyllus ethanolic extract (PPE), (2) the in vitro antioxidant activity (AA) of PPE and of two different topical formulations (F1 and F2) containing PPE, (3) physico-chemical and functional stability, (4) in vitro release of PPE, and (5) in vivo capacity of formulations to prevent UV-B irradiation-induced skin damage. Results show that the polyphenol and flavonoid contents in PPE were 199.33 and 28.32 mg/g, respectively, and HPLC results show the presence of eugenol, tannic acid, and rutin. Evaluation of the in vitro AA of PPE demonstrated a dose-dependent effect and an IC50 of 4.75 µg/mL in 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 3.0 µg/mL in 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays. The ferric-reducing antioxidant power (FRAP assay) was 0.046 µmol/L trolox equivalent/µg/mL of extract. Among the AA, only the capacity to scavenge DPPH radical of PPE was maintained in F1 and F2. In addition, both formulations satisfactorily released the extract. The evaluation of the functional stability of F1 and F2 did not demonstrate loss of activity by storage at room temperature and at 4°C/6 months. In irradiated mice, treatment with F1 and F2 added with PPE significantly increased the capacity to scavenge ABTS radical and the FRAP of skin compared to vehicle-treated mice. In conclusion, the present results suggest that formulations containing PPE may be a topical source of antioxidant compounds to decrease oxidative damages of the skin.


Asunto(s)
Antioxidantes/química , Antioxidantes/farmacología , Estrés Oxidativo/efectos de los fármacos , Pimenta/química , Extractos Vegetales/química , Extractos Vegetales/farmacología , Animales , Benzotiazoles/química , Compuestos de Bifenilo/química , Química Farmacéutica/métodos , Etanol/química , Ratones , Ratones Pelados , Fenoles/química , Fenoles/farmacología , Picratos/química , Piel/efectos de los fármacos , Ácidos Sulfónicos/química , Rayos Ultravioleta/efectos adversos
8.
J Photochem Photobiol B ; 127: 153-60, 2013 Oct 05.
Artículo en Inglés | MEDLINE | ID: mdl-24041853

RESUMEN

Plants rich in antioxidant substances may be a promising strategy for preventing UV-induced oxidative and inflammatory damage of the skin. Pimenta pseudocaryophyllus is native to Brazil and presents flavonoids and other polyphenolic compounds in high concentration. Thus, the present study evaluated the possible effects of topical formulations containing P. pseudocaryophyllus ethanolic extract (PPE) at inhibiting UV-B irradiation-induced oxidative stress and inflammation. PPE was administered on the dorsal skin of hairless mice using two formulations: F1 (non-ionic emulsion with high lipid content) and F2 (anionic emulsion with low lipid content) before and after UV-B irradiation. The following parameters were evaluated in skin samples: edema, myeloperoxidase activity, cytokines levels, matrix metalloprotease-9 (MMP-9) secretion/activity, reduced glutathione (GSH), superoxide anion and lipid peroxidation levels, and mRNA expression for glutathione reductase and gp91phox. The UV-B irradiation increased all parameters, except for IL-10 levels and glutathione reductase mRNA expression, which were not altered, and GSH levels, which were reduced by exposure to UV-B light. Treatments with F1 and F2 containing PPE inhibited UV-B-induced edema formation (89% and 86%), myeloperoxidase activity (85% and 81%), IL-1ß production (62% and 82%), MMP-9 activity (71% and 74%), GSH depletion (73% and 85%), superoxide anion (83% and 66%) and TBARS (100% and 100%) levels, increased glutathione reductase (2.54 and 2.55-fold) and reduced gp91phox (67% and 100%) mRNA expression, respectively. F2 containing PPE also increased IL-10 levels. Therefore, this study demonstrates the effectiveness of topical formulations containing PPE in inhibiting UV-B irradiation-induced inflammation and oxidative stress of the skin.


Asunto(s)
Estrés Oxidativo/efectos de los fármacos , Pimenta/química , Extractos Vegetales/farmacología , Rayos Ultravioleta/efectos adversos , Administración Tópica , Animales , Química Farmacéutica , Citocinas/metabolismo , Edema/etiología , Edema/prevención & control , Etanol/química , Femenino , Regulación de la Expresión Génica/efectos de los fármacos , Regulación de la Expresión Génica/efectos de la radiación , Glutatión Reductasa/genética , Inflamación/etiología , Inflamación/prevención & control , Masculino , Metaloproteinasa 9 de la Matriz/metabolismo , Glicoproteínas de Membrana/genética , Ratones , Ratones Pelados , NADPH Oxidasa 2 , NADPH Oxidasas/genética , Estrés Oxidativo/efectos de la radiación , Extractos Vegetales/administración & dosificación , Extractos Vegetales/química , ARN Mensajero/genética , ARN Mensajero/metabolismo , Piel/efectos de los fármacos , Piel/metabolismo
9.
Pharm Biol ; 51(10): 1262-71, 2013 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-23855752

RESUMEN

UNLABELLED: CONTEXT. Tephrosia toxicaria is currently known as Tephrosia sinapou (Buc'hoz) A. Chev. (Fabaceae) and is a source of compounds such as flavonoids that inhibit inflammatory pain. OBJECTIVE: To investigate the analgesic effect and mechanisms of the ethyl acetate extract of T. sinapou in inflammatory pain in mice. MATERIALS AND METHODS: Behavioral responses were evaluated using mechanical (1-24 h) and thermal hyperalgesia (0.5-5 h), writhing response (20 min) and rota-rod (1-5 h) tests. Neutrophil recruitment (myeloperoxidase activity), cytokines (tumor necrosis factor [TNF]α and interleukin [IL]-1ß), aspartate aminotransferase (AST) and alanine aminotransferase (ALT) serum levels were determined by colorimetric assays. Pharmacological treatments were opioid receptor antagonist (naloxone, 0.1-1 mg/kg) and control opioid (morphine, 5 mg/kg). Inflammatory stimuli were carrageenin (100 µg/paw), complete Freund's adjuvant (CFA, 10 µl/paw), prostaglandin E2 (PGE2, 100 ng/paw) and acetic acid (0.8%). RESULTS: The intraperitoneal pre-treatment with extract inhibited in a dose-dependent (30-300 mg/kg) dependent manner the mechanical hyperalgesia induced by carrageenin (up to 93% inhibition). The post-treatment (100 mg/kg) inhibited CFA-induced hyperalgesia (up to 63% inhibition). Naloxone (1 mg/kg) prevented the inhibitory effect of the extract over carrageenin-induced mechanical (100%) and thermal (100%) hyperalgesia, neutrophil recruitment (52%) and TNFα (63%) and IL-1ß (98%) production, thermal threshold in naïve mice (99%), PGE2-induced mechanical hyperalgesia (88%) and acetic acid-induced writhing response (49%). There was no significant alteration in the rota-rod test, and AST and ALT serum levels by extract treatment. Discussion and conclusion. Tephrosia sinapou ethyl acetate extract reduces inflammatory pain by activating an opioid receptor-dependent mechanism.


Asunto(s)
Analgésicos/farmacología , Hiperalgesia/prevención & control , Interleucina-1beta/metabolismo , Dolor/prevención & control , Extractos Vegetales/farmacología , Receptores Opioides/efectos de los fármacos , Tephrosia , Factor de Necrosis Tumoral alfa/metabolismo , Acetatos/química , Analgésicos/química , Analgésicos/aislamiento & purificación , Animales , Conducta Animal/efectos de los fármacos , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Hiperalgesia/inducido químicamente , Hiperalgesia/inmunología , Hiperalgesia/metabolismo , Hiperalgesia/fisiopatología , Masculino , Ratones , Antagonistas de Narcóticos/farmacología , Infiltración Neutrófila/efectos de los fármacos , Dolor/inducido químicamente , Dolor/inmunología , Dolor/metabolismo , Dolor/fisiopatología , Umbral del Dolor/efectos de los fármacos , Fitoterapia , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Raíces de Plantas , Plantas Medicinales , Receptores Opioides/metabolismo , Transducción de Señal/efectos de los fármacos , Solventes/química , Tephrosia/química , Factores de Tiempo
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