Evaluation of anti-inflammatory activity of kaurenol: Experimental evaluation and mechanistic insights.

BACKGROUND: Kaurenol, a diterpene alcohol found in Copaifera langsdorffii Desf. (known as "copaiba"), is historically used in traditional medicine for inflammatory conditions. OBJECTIVES: This study aims to comprehensively assess the potential anti-inflammatory and antinociceptive properties of kaurenol. METHODS: To this end, the following experiments were conducted to evaluated toxicity: locomotor performance and acute toxicity; nociception: acetic acid-induced writhing and formalin-induced antinociception; and anti-inflammatory activity: carrageenan and dextran-induced paw edema at 10, 20, and 40 mg/kg, and measurement of nitric oxide (NO), tumor necrosis factor alpha (TNF-α), interleukin-6 (IL-6), and interleukin-10 (IL-10) in macrophages at 1, 3, and 9 µg/ml. RESULTS: Kaurenol did not show significant locomotor changes, acute toxicity, and central analgesic activity in the first phase of formalin test at dosages tested. Kaurenol showed 53%, 64%, 64%, and 58% of inhibition in the acetic acid-induced writhing, second phase of formalin test, carrageenan and dextran-induced paw edema, respectively. CONCLUSION: The anti-inflammatory activity was associated with the regulation of NO release and probably with the regulation of mediators, such as serotonin and prostaglandin in vascular permeability, as well as by being associated with the regulation of IL-6 and IL-10. Kaurenol display anti-inflammatory activity but has no analgesic activity.

Ingenol mebutate in the treatment of actinic keratoses: clearance rate and adverse effects.

BACKGROUND: Actinic keratoses are benign intraepithelial skin neoplasms that develop in photoexposed areas and can progress to invasive carcinoma. They are seen frequently in dermatological practice, occurring in 5.1% of consultations. Ingenol mebutate (IM) was recently approved in Brazil as a topical therapy for field cancerization in actinic keratosis. OBJECTIVE: To evaluate the clearance rate and adverse events in the treatment of actinic keratoses with ingenol mebutate. METHODS: A longitudinal, prospective, non-randomized, interventional, open, single-center study was conducted. Patients with actinic keratoses applied ingenol mebutate on a 25cm2 area of the face and/or scalp for three consecutive days (0.015%) or on the forearm for two days (0.05%). RESULTS: 27 patients completed the protocol, of whom 13 on the face and/or scalp and 14 on the forearm. Complete clearance occurred in 53.8% in the first group and 42.8% in the second. Partial response was observed in 15.4% and 35.7%, respectively. The most common side effects were erythema, edema, desquamation, pruritus, and local erosion. STUDY LIMITATIONS: The study had a small sample and was not randomized, double-blind, placebo-controlled, or vehicle-controlled. CONCLUSION: Ingenol mebutate is well-tolerated for the treatment of actinic keratosis, with good patient adherence thanks to the short treatment period.

Ingenol mebutate in the treatment of actinic keratoses: clearance rate and adverse effects

Abstract: Background: Actinic keratoses are benign intraepithelial skin neoplasms that develop in photoexposed areas and can progress to invasive carcinoma. They are seen frequently in dermatological practice, occurring in 5.1% of consultations. Ingenol mebutate (IM) was recently approved in Brazil as a topical therapy for field cancerization in actinic keratosis. Objective: To evaluate the clearance rate and adverse events in the treatment of actinic keratoses with ingenol mebutate. Methods: A longitudinal, prospective, non-randomized, interventional, open, single-center study was conducted. Patients with actinic keratoses applied ingenol mebutate on a 25cm2 area of the face and/or scalp for three consecutive days (0.015%) or on the forearm for two days (0.05%). Results: 27 patients completed the protocol, of whom 13 on the face and/or scalp and 14 on the forearm. Complete clearance occurred in 53.8% in the first group and 42.8% in the second. Partial response was observed in 15.4% and 35.7%, respectively. The most common side effects were erythema, edema, desquamation, pruritus, and local erosion. Study limitations: The study had a small sample and was not randomized, double-blind, placebo-controlled, or vehicle-controlled. Conclusion: Ingenol mebutate is well-tolerated for the treatment of actinic keratosis, with good patient adherence thanks to the short treatment period.

Seco-taondiol, an unusual meroterpenoid from the Chilean seaweed Stypopodium flabelliforme and its gastroprotective effect in mouse model.

Ten known meroterpenoids and the new meroterpenoid 7 were isolated from the Chilean seaweed Stypopodium flabelliforme as their acetylated derivatives. Furthermore, the known metabolite taondiol has been isolated for the first time from this species. The molecular structure of the new metabolite was determined by spectroscopic methods based on 1D- and 2D-NMR. Isolation of 7 represents a key step toward a better understanding of the biogenesis of this class of meroterpenoids. Among the meroditerpenoids isolated, stypodiol, isoepitaondiol, epitaondiol and sargaol exhibited gastroprotective activity on the HCl/Ethanol-induced gastric lesions model in mice. Regarding the mode of gastroprotective action, the activity of epitaondiol was reversed significantly when animals were pretreated with indomethacin, N-ethylmaleimide and N-nitro-l-arginine methyl ester (L-NAME) suggesting that prostaglandins, sulfhydryl groups and nitric oxide are involved in their mode of gastroprotective action. In the case of sargaol the gastroprotective activity was attenuated with indomethacin and N-ethylmaleimide, which suggests that prostaglandins and sulfhydryl groups are also involved in the mode of action using this model.

O consumo de café e sua relação com a hiperhomocisteinemia: revisão / Coffee intake and the relation with hyperhomocisteinemia: a review

Coffee is one of the most worldwide consumed beverages, and Brazil is its major source. Coffee plants belong to the Rubiacea e family, and there are many species, although only C. arabica and C. canephora (Robusta) have commercial value. The chemical composition of green coffee depends on the species, climatic conditions, processing and storage. Recently, coffee intake has been related to increased plasma homocysteine levels ­ this non-proteica minoacid is one of the risk factors for occlusive cardiovascular diseases,one of the main causes of death in industrialized countries. This finding points out to the relevance of analysis of coffee constituents involved inincreased homocysteine plasma levels. Caffeine, chlorogenic acid and diterpenes (caffestol and caveol) are important substances present in coffee,which exert physiological effects

El café es una de las bebidas mas consumidas en el mundo, siendo Brasil el mayor produto rmundial. El café pertenece a la família Rubiáceas, y existen numerosas especies, pero solamente la C. arabica y la C. canéfora (Robusta) tienen valor comercial. La composición química del café verde depende dela especie, condiciones climáticas, de procesamiento y de almacenamiento. Recientemente, el consumo de café ha sido relacionado al aumento de los niveles de homocisteína plasmática ­ este aminoácido no proteico es uno de los factores de riesgo para las enfermedades cardiovasculares oclusivas, las cuales responden por las principales causas de muerte en países industrializados ­ esto es relevante para la investigación que busca los componentes del café, responsables por el aumento de los niveles de homocisteínaplasmática. La cafeína, el acido clorogénico, diterpenos (cafestol y cahweol) son importantes substancias presentes en el café que ejercen efectos fisiológicos en el organismo

A bebida de café é uma das bebidas mais consumidas no mundo, sendo o Brasil o seu maior produtor. As plantas de café pertencem à família Rubiaceae, e possuem inúmeras espécies, mas somente a C. arábica e C. canéfora (Robusta) têm valor comercial. A composição química do café verde depende da espécie, condições climáticas, processamento e estocagem. Recentemente, o consumo de café tem sido relacionado ao aumento dos níveis de homocisteína plasmática - esse aminoácido não protéico é um dos fatores de risco para a ocorrência de doenças cardiovasculares oclusivas, uma das principais causas de morte em países industrializados - tal fato torna relevante a investigação sobre os componentes do café, envolvidos no incremento dos níveis de homocisteína plasmática. A cafeína, o ácido clorogênico e os diterpenos (cafestol e caveol) são importantes substâncias presentes no café, exercendo efeitos fisiológicos no organismo