Antinociceptive and antispasmodic effects of the essential oil of Ocimum micranthum: potential anti-inflammatory properties.

The antinociceptive and antispasmodic properties of the essential oil of OCIMUM micranthum (EOOM) were characterized. In mice, EOOM (15-100 mg · kg (-1), p. o.) reduced both the writhing responses induced by acetic acid and the licking-time induced by formalin, being inert on the hot plate test. In rat trachea, EOOM relaxed sustained contractions induced by KCl or carbachol (CCh). Its constituents, ( E)- [( E)-MC] and ( Z)-methyl cinnamate [( Z)-MC], reproduced several effects of EOOM. Inhaled as aerosol, EOOM prevented tracheal hyperresponsiveness to KCl or CCh in ovalbumin-sensitized animals after antigen challenge. Thus, EOOM exerts peripheral analgesia in nociception of inflammatory origin and has antispasmodic actions on rat airways under an inflammatory environment. Its effects are mainly due to ( E)-MC, which makes this substance potentially interesting for studies involving conjunctly smooth muscle cells, nociception, and inflammation. Other EOOM constituents also appear to be involved in its pharmacological actions.

In vitro antiplasmodial activity and identification, using tandem LC-MS, of alkaloids from Aspidosperma excelsum, a plant used to treat malaria in Amazonia.

ETHNOPHARMACOLOGICAL RELEVANCE: Aspidosperma excelsum Benth. (Apocynaceae), a native tree in the Brazilian Amazonia, is traditionally used to treat various diseases, including malaria. AIM OF STUDY: To investigate the chemical constitution, antiplasmodial activity and cytotoxicity of samples obtained from A. excelsum trunk bark by different procedures aiming to evaluate their potential as an antimalarial phytomedicine. MATERIALS AND METHODS: A hydroethanolic extract and alkaloid extracts were prepared and assayed for antiplasmodial activity and cytotoxicity against chloroquine-resistant Plasmodium falciparum (W2 strain) and HepG2 cells, respectively. Taking into account the known occurrence and antimalarial activity of Aspidosperma monoterpene indole alkaloids (MIA), acid-base extractions were carried out and the fractions were assayed for antiplasmodial activity and cytotoxicity. All the samples were analysed by hyphenated chromatographic techniques, such as UPLC-DAD-ESI-MS/MS and HRMS (HPLC-MS MicroTOF), comparing their chemical composition to the literature data. RESULTS: The hydroethanolic extract disclosed a moderate in vitro activity against chloroquine-resistant Plasmodium falciparum (W2 strain) with IC50 23.68 ± 3.08 µg/mL), low cytotoxicity to HepG2 cells (> 250 µg/mL) and good SI (> 10.56). A total of 20 known monoterpene indole alkaloids were identified, seven of which are here firstly described for A. excelsum. Known highly active alkaloids, namely demethylaspidospermine, aspidocarpine, and ochrolifuanine are present in active alkaloid fractions and might contribute to their observed antiplasmodial effect. An alkaloid fraction (Ae-Alk2), obtained directly from trunk bark by extraction with dil. aqueous HCl, pointed out for its activity (IC50 8.75±2.26 µg/mL, CC50 185.14±1.97 µg/mL, SI 21.16) and should be highlighted as the most promising out of the assayed samples. CONCLUSION: The present results represent a preliminary support to the alleged antimalarial use of A. excelsum trunk bark and allowed to highlight alkaloid fractions as promising phytomedicines.

Salicytamide: a New Anti-inflammatory Designed Drug Candidate.

Salicytamide is a new drug developed through molecular modelling and rational drug design by the molecular association of paracetamol and salicylic acid. This study was conducted to assess the acute oral toxicity, antinociceptive, and antioedematogenic properties of salicytamide. Acute toxicity was based on the OECD 423 guidelines. Antinociceptive properties were investigated using the writhing, hot plate and formalin tests in Swiss mice. Antioedematogenic properties were evaluated using the carrageenan-induced paw oedema model and croton oil-induced dermatitis in Wistar rats. Salicytamide did not promote behavioural changes or animal deaths during acute oral toxicity evaluation. Furthermore, salicytamide exhibited peripheral antinociceptive activity as evidenced by the reduction in writhing behaviour (ED50 = 4.95 mg/kg) and licking time in the formalin test's inflammatory phase. Also, salicytamide elicited central antinociceptive activity on both hot plate test and formalin test's neurogenic phase. Additionally, salicytamide was effective in reducing carrageenan or croton oil-induced oedema formation. Overall, we have shown that salicytamide, proposed here as a new NSAID candidate, did not induce oral acute toxicity and elicited both peripheral antinociceptive effects (about 10-25 times more potent than its precursors in the writhing test) and antioedematogenic properties. Salicytamide also presented central antinociceptive activity, which seems to be mediated through opioid-independent mechanisms. These findings reveal salicytamide as a promising antinociceptive/antioedematogenic drug candidate.

Antifungal Activity of Hydroalcoholic Extract of Chrysobalanus icaco Against Oral Clinical Isolates of Candida Species.

BACKGROUND: Chrysobalanus icaco is a medicinal plant commonly used to treat fungal infections in Brazilian Amazonian region. OBJECTIVE: This work aimed to evaluate the antifungal activity of the hydroalcoholic extract of C. icaco (HECi) against oral clinical isolates of Candida spp. and to determine the pharmacognostic parameters of the herbal drug and the phytochemical characteristics of HECi. MATERIALS AND METHODS: The pharmacognostic characterization was performed using pharmacopoeial techniques. Phytochemical screening, total flavonoid content, and high-performance liquid chromatography (HPLC) analysis were used to investigate the chemical composition of the HECi. A broth microdilution method was used to determine the antifungal activity of the extract against 11 oral clinical isolates of Candida spp. RESULTS: Herbal drug presented parameters which were within the limits set forth in current Brazilian legislation. A high amount of flavonoid content (132,959.33 ± 12,598.23 µg quercetin equivalent/g of extract) was found in HECi. Flavonoids such as myricetin and rutin were detected in the extract by HPLC analyses. HECi showed antifungal activity against oral isolates of Candida albicans and Candida parapsilosis (minimum inhibitory concentrations [MIC] 3.12 and 6.25 mg/mL, respectively), and C. albicans American American Type Culture Collection (MIC <1.56 mg/mL). CONCLUSION: HECi was shown to possess antifungal activity against Candida species with clinical importance in the development of oral candidiasis, and these activities may be related to its chemical composition. The antifungal activity detected for C. icaco against Candida species with clinical importance in the development of oral candidiasis can be attributed to the presence of flavonoids in HECi, characterized by chromatographic and spectroscopic techniques. SUMMARY: Chrysobalanus icaco presents a high amount of flavonoids in its constitutionLC analysis was able to identify the flavonoids myricetin and rutin in C. icaco hydroalcoholic extractThe C. icaco hydroalcoholic extract inhibits the growth of oral clinical isolates of Candida spp. and Candida albicans American Type Culture Collection. Abbreviations Used: HECi: Hydroalcoholic extract of C. icaco; HPLC: High performance liquid chromatography; AlCl3: Aluminum chloride; DMSO: Dimethyl sulfoxide; CH3NOONa: Sodium acetate; MTT: 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; ATCC: American Type Culture Collection; EMBRAPA: Brazilian Agricultural Research Corporation - Eastern Amazon; v/v: Volume per volume; SD: Standard deviation; TFC: Total flavonoid content; w/v: Weight per volume; ELSD: Evaporative light scattering detector; DAD: Diode-arrange detector; UFPA: Federal University of Pará; IEC: Evandro Chagas Institute; INCQS-FIOCRUZ: National Institute of Quality Control in Health - Fundação Oswaldo Cruz; SDA: Sabouraud Dextrose Agar; CFU: Colony-forming units; MIC: Minimum inhibitory concentrations; MFC: Minimum fungicidal concentrations.

Avaliação fitoquímica e potencial cicatrizante do extrato etanólico dos frutos de Jucá (Libidibia ferrea) em ratos Wistar / Phytochemical evaluation and wound healing potential of the fruit extract ethanolic of Jucá (Libidibia ferrea) in Wistar rats

Libidibia ferrea é uma planta muito utilizada popularmente para fins terapêuticos, inclusive para acelerar processos de cicatrização de feridas cutâneas. O presente trabalho pesquisou a composição química e avaliou o potencial cicatrizante do extrato etanólico dos frutos de L. ferrea (Mart. ex Tul.) em ratos. Foram utilizados 24 ratos Wistar divididos em quatro grupos. De todos os animais, foi retirado um fragmento de pele do dorso e cada grupo recebeu um tratamento diferente: solução de NaCl 0,9%, digliconato de clorexidina 1%, extrato etanólico dos frutos de Libidibia ferrea 12,5% e 50%. O processo de cicatrização foi avaliado macro e microscopicamente. Para a cicatrização de pele em ratos o extrato etanólico dos frutos de L. ferrea a 12,5% é significativamente mais eficiente do que a 50%. Saponinas, ácidos orgânicos, açúcares redutores, fenóis e taninos, sesquiterpenolactonas e outras lactonas, e antraquinonas foram encontrados no extrato.

Libidibia ferrea is a plant popularly used for therapeutic purposes, including processes to accelerate wound healing. The present investigation analyzed the chemical composition and the healing potential of ethanolic extract of the fruits of L. ferrea (Mart. ex Tul.) in rats. This study used 24 Wistar rats divided into four groups. In all animals a piece of skin on the back was removed and each group received a different treatment: NaCl 0.9%, Chlorhexidine digluconate 1%, ethanol extract of the fruits of Libidibia ferrea 12.5% and 50%. The healing process was evaluated macroscopically and microscopically. The ethanolic extract of the fruits of L. ferrea 12.5% was significantly more efficient than the 50% healing in rat skin.