Lucindo José Quintans Júnior

Plants with anticonvulsant properties: a review

Seizures are resistant to treatment with currently available anticonvulsant drugs in about 1 out of 3 patients with epilepsy. Thus, there is a need for new, more effective anticonvulsant drugs for intractable epilepsy. However, nature is a rich source of biological and chemical diversity and a number of plants in the world have been used in traditional medicine remedies, i.e., anticonvulsant, anxiolytic, analgesic, antidepressant. This work constitutes a literature review on medicinal plants showing anticonvulsant properties. The review refers to 16 Brazilian plants and a total 355 species, their families, geographical distribution, the utilized parts, method and references. Some aspects of research on medicinal plants and a brief review of the most common animal models to discover antiepileptic drugs are discussed. For this purpose over 170 references were consulted.

Borneol, a Bicyclic Monoterpene Alcohol, Reduces Nociceptive Behavior and Inflammatory Response in Mice

Borneol, a bicyclic monoterpene, has been evaluated for antinociceptive and anti-inflammatory activities. Antinociceptive and anti-inflammatory activities were studied by measuring nociception by acetic acid, formalin, hot plate, and grip strength tests, while inflammation was prompted by carrageenan-induced peritonitis. The rotarod test was used to evaluate motor coordination. Borneol produced a significant (P < 0.01) reduction of the nociceptive behavior at the early and late phases of paw licking and reduced the writhing reflex in mice (formalin and writhing tests, resp.). When the hot plate test was conducted, borneol (in higher dose) produced an inhibition (P < 0.05) of the nociceptive behavior. Such results were unlikely to be provoked by motor abnormality. Additionally, borneol-treated mice reduced the carrageenan-induced leukocytes migration to the peritoneal cavity. Together, our results suggest that borneol possess significant central and peripheral antinociceptive activity; it has also anti-inflammatory activity. In addition, borneol did not impair motor coordination.

Encapsulation of carvacrol, a monoterpene present in the essential oil of oregano, with β-cyclodextrin, improves the pharmacological response on cancer pain experimental protocols

Cancer pain is a major public health problem worldwide due to the strong impact on the quality of life of patients and side effects of the existing therapeutic options. Monoterpenes, as carvacrol (CARV), have been extensively studied about their therapeutic properties, especially their importance in the control of painful conditions and inflammation, which can be improved through the use of inclusion complexes of β-cyclodextrin (β-CD). We evaluated the effect of encapsulation of CARV in β-CD (CARV/β-CD) on the nociception induced by tumor cells (Sarcoma 180) in rodents. Inclusion complexes were prepared in two different procedures and characterized through thermal analysis and scanning electron microscopy. CARV/β-CD complex was administered (50 mg/kg, p.o.) in mice with tumor on the hind paw and was able to reduce the hyperalgesia (von Frey) during 24 h, unlike the free CARV (100 mg/kg, p.o.), which promoted effects until 9 h. Administration on alternate days of complex of CARV/β-CD (12.5-50 mg/kg, p.o.) reduced hyperalgesia, as well as spontaneous and palpation-induced nociception. However, pure CARV (50 mg/kg) did not cause significant changes in nociceptive responses. Together, these results produced evidence that the encapsulation of carvacrol in β-cyclodextrin can be useful for the development of new options for pain management.

Evidence for the involvement of descending pain-inhibitory mechanisms in the attenuation of cancer pain by carvacrol aided through a docking study

AIMS The present study evaluated the carvacrol (CARV) effect on hyperalgesia and nociception induced by sarcoma 180 (S180) in mice. MAIN METHODS Carvacrol treatment (12.5-50mg/kgs.c.) once daily for 15days was started 24h after injection of the sarcoma cells in the hind paw (s.c.). Mice were evaluated for mechanical sensitivity (von Frey), spontaneous and palpation-induced nociception, limb use and tumor growth on alternate days. CARV effects on the central nervous system were evaluated through immunofluorescence for Fos protein. Molecular docking studies also were performed to evaluate intermolecular interactions of the carvacrol and muscimol, as ligands of interleukin-10 and GABAA receptors. KEY FINDINGS CARV was able to significantly reduce mechanical hyperalgesia and spontaneous and palpation-induced nociception, improve use paw, decrease the number of positively marked neurons in lumbar spinal cord and activate periaqueductal gray, nucleus raphe magnus and locus coeruleus. CARV also caused significant decreased tumor growth. Docking studies showed favorable interaction overlay of the CARV with IL-10 and GABAA. SIGNIFICANCE Together, these results demonstrated that CARV may be an interesting option for the development of new analgesic drugs for the management of cancer pain.

Biological Oxidations and Antioxidant Activity of Natural Products

Oxygen is the most prevalent element in the earth’s crust. It exists in air as a diatomic molecule, O2. Except for a small number of anaerobic bacteria, all living organisms use O2 for energy production and it is essential for life as we know it. Energy production by organisms from food material requires “oxidation”, which implies the loss of electrons. However the potential of O2 to oxidize also makes it toxic. Oxidation can inactivate important enzymes, and anaerobes that do not have antioxidant mechanisms do not survive in an O2 environment (Magder, 2006).

Orofacial antinociceptive effect and antioxidant properties of the hydroethanol extract of Hyptis fruticosa salmz ex Benth.

ETHNOPHARMACOLOGICAL RELEVANCE Hyptis fruticosa is a plant native to Brazil with antinociceptive and antiinflamatory properties. This study evaluated the antinociceptive activity of the hydroethanol extract of the plant leaves (CHEE) against orofacial pain as well as its in vitro effect against lipid peroxidation. MATERIALS AND METHODS The antinociceptive activity was investigated in mice orally treated with different doses of the CHEE (50, 100, and 200 mg/kg) and morphine (5 mg/kg) using formalin, glutamate, and capsaicin orofacial pain models using. Lipoperoxidation was induced in egg yolk by AAPH and FeSO4 in the absence and presence of the CHEE (5, 50, 100, and 150 μg/mL). RESULTS CHEE (200 mg/kg) significantly reduced (ρ<0.001) the pain response in the first (69.6%) and second (81.8%) phases of the formalin test, while the nociception caused by capsaicin was significantly (ρ<0.001) reduced by up to 62% at 200 mg/kg of extract. When glutamate was used as algogen, a significant (ρ<0.001) nociception reduction of up to 85% at 200 mg/kg extract was observed. CHEE showed a higher protection against lipoperoxidation caused by FeSO4 (82.3% TBARS inhibition) than AAPH (35.7% TBARS inhibition) at 150 μg/mL. CONCLUSION Hyptis fruticosa leaf CHEE is of pharmacological interest because it was able to inhibit the peripheral and central transmission of orofacial pain, while reducing the spreading of the inflammatory processes by neutralizing reactive oxygen species, which are by-products in the biosynthesis of pain mediators.

Antinociceptive and anti-inflammatory effects of Costus spicatus in experimental animals.

Context: Costus spicatus Swartz (Costaceae), commonly called “cana-do-brejo’” in Brazil’s northeast, is a medicinal plant found in wet coastal forests. In folk medicine an infusion of the aerial parts is taken to treat inflammation and pain. Objective: The methanol extract obtained from the leaves of Costus spicatus (MECs) was evaluated for antinociceptive and anti-inflammatory activities. Methods: Analgesic and anti-inflammatory activities were studied by measuring nociception through acetic acid, formalin, and hot-plate tests, while inflammation was induced by carrageenan. All experiments were conducted with experimental animals. Results and discussion: Following oral administration, MECs (100, 200, and 400 mg/kg) significantly reduced the number of writhes (52.8, 43.1, and 55.3%, respectively) in the writhing test and the number of paw licks during phase 1 (61.9, 54.1, and 92.1%) and phase 2 (62.5, 82.9, and 98.1%, all doses) during the formalin test when compared to the control group animals. The reaction time during the hot-plate test was increased significantly and was dose-dependent, whereas pretreatment with naloxone rigorously reduced the analgesic potential of MECs, which suggested participation of the opioid system in the modulation of pain induced by MECs. Such results were unlikely to be provoked by motor abnormality, as MECs-treated mice did not exhibit any performance alteration during the Rota-rod test. The administration of 200 and 400 mg/ kg (i.p.) of MECs exhibited an anti-inflammatory effect during the carrageenan test, which was based on interference with inflammatory mediator synthesis. Conclusion: We conclude that MECs has antinociceptive and anti-inflammatory activities in rodents.

Effects of luteolin and quercetin 3-β-d-glucoside identified from Passiflora subpeltata leaves against acetaminophen induced hepatotoxicity in rats

Passiflora subpeltata has many beneficial effects in the treatment of various diseases including inflammation, pain and fever. This study was aimed to analyze the phytochemical compounds present in acetone extract of P. subpeltata leaves and to evaluate their performance against paracetamol induced hepatotoxicity activity. HPLC-DAD method was used to identify and quantify the phytochemical compounds. Hepatoprotective activity of acetone extract in the treatment of rat liver functions was monitored by the measurement of blood parameters and serum biochemical parameters such as SGOT, SGPT, ALP and in vivo antioxidant parameters viz. SOD, CAT and LPO. Further, liver tissues were also subjected to histopathological analysis. The HPLC-DAD results showed the luteolin and quercetin 3-β-d-glucoside as newly identified compounds in P. subpeltata species. Pre-treatment with acetone extract of P. subpeltata leaves at 200 and 400mg/kg doses significantly elevated the WBC, RBC and HB counts and retained the serum biochemical and enzymatic antioxidants levels to normal level. Based on this detailed study we conclude that acetone extract of P. subpeltata leaves offered better protection against hepatotoxicity induced by the acetaminophen.

Avaliação dos sintomas de ansiedade e depressão em fibromiálgicos

Se objetivo identificar la frecuencia de sintomas de ansiedad y depresion y verificar la asociacion entre ansiedad-rasgo y sintomas actuales de depresion y ansiedad en fibromialgicos. Fueron entrevistados 60 sujetos con diagnostico de fibromialgia en Ambulatorio de Reumatologia de Universidad Federal de Sergipe, de agosto 2007 a marzo 2008. Se aplicaron dos cuestionarios: Escala Hospitalaria de Ansiedad y Depresion (EHAD) e Inventario de Ansiedad Rasgo-Estado (IDATE-T). La frecuencia de sintomas depresivos y ansiosos fue, respectivamente, 50% y 86% para los fibromialgicos y el promedio de puntaje del rasgo ansioso fue de 59,38. Se observo asociacion entre ansiedad-rasgo y estado. La ansiedad y la depresion fueron sintomas frecuentes en pacientes con fibromialgia. Entretanto, la ansiedad fue un sintoma secundario mas frecuente que la depresion y se presento de forma mas grave, resultando una comorbilidad que necesita ser mas valorizada y estudiada.The objective of this study was to identify the frequency of anxiety and depression symptoms by verifying the association between anxiety traits, current depression and anxiety symptoms in fibromyalgia patients. Interviews were performed with 60 subjects diagnosed with fibromyalgia at the Rheumatology Outpatient Clinic at Universidade Federal de Sergipe between August 2007 and March 2008, in which two questionnaires were administered: the Hospital Anxiety and Depression Scale (HADS) and the State-Trait Anxiety Inventory (STAI). The frequency of anxiety and depression symptoms was, respectively, 50% and 86% for individuals with fibromyalgia, and the mean trait-anxiety score was 59.38. An association was observed between trait and state anxiety. Anxiety and depression were frequent symptoms among patients with fibromyalgia. However, anxiety appeared as a secondary symptom to depression, appearing in a more severe form, and, therefore, this comorbidity should be more valued and studied.

Side Effects of the Therapy With Peginterferon and Ribavirin in Chronic Hepatitis C: A Small Audit

This study sought to decribe, quantify, and classify any adverse reactions occurring in patients with chronic hepatitis C treated with peginterferon and ribavirin, as well as verify the occurrence of potential medication interactions. The most prevalent reactions were fatigue (84.8%), fever (83%), weight loss (80%), irritability (74%), and body pain (72%). Most of the reactions were classified as mild (95%), whereas 4.5% were classified as moderate and 0.4% as severe. Adverse reactions led to the rearrangement of therapy for 9 patients (20%), where there was a reduction in dose for 7 (15%), temporary interruption of treatment for 5 (11%), and permanent discontinuation for 3 patients (7%). A total of 11 potential medication interactions were identified in 9 patients (20%), with the most frequent between peginterferon-α2a and captopril (45%). Given the above, it is observed that the treatment of chronic hepatitis C is marked by several adverse reactions of varying severity, which can interfere with the patient’s quality of life or in treatment compliance, and that can be aggravated by potential drug–drug interactions.