Pharmacological activities of a novel phthalic acid ester and iridoid glycoside isolated from the root bark of Anthocleista vogelii Planch.

In this study, a novel phthalic acid ester (1) and a known iridoid glycoside (2) were isolated from the root bark of Anthocleista vogelii. The structures of the novel compound and iridoid glycoside were elucidated on the basis of their chemical and spectral data (UV, FT-IR, EI-MS, 1D and 2D NMR) and found to be phthalic acid ester, 4-ethyl-6-propyl-4,5,6,7-tetrahydro3H-2,8-benzodioxacycloundecine-1,9-dione (1) and sweroside (2). The compounds were evaluated for their in vitro inhibitory activities against pancreatic lipase, α-amylase and αglucosidase, and in vivo laxative activity in rats. The metabolite phthalic acid ester (1) exhibited moderate inhibitory activity against pancreatic lipase (IC50 = 24.43 ± 0.096 µg/mL) and relatively good activity against α-glucosidase (IC50 = 10.28 ± 0.015 µg/mL). Sweroside (2) displayed weak activity against α-glucosidase (IC50 = 40.28 ± 0.063 µg/mL) but significantly (p<0.05) increased the feacal output of the treated animals compared to the normal and sodium picosulfate controls.

Pharmacological activities of a novel phthalic acid ester and iridoid glycoside isolated from the root bark of Anthocleista vogelii Planch

@#In this study, a novel phthalic acid ester (1) and a known iridoid glycoside (2) were isolated from the root bark of Anthocleista vogelii. The structures of the novel compound and iridoid glycoside were elucidated on the basis of their chemical and spectral data (UV, FT-IR, EI-MS, 1D and 2D NMR) and found to be phthalic acid ester, 4-ethyl-6-propyl-4,5,6,7-tetrahydro- 3H-2,8-benzodioxacycloundecine-1,9-dione (1) and sweroside (2). The compounds were evaluated for their in vitro inhibitory activities against pancreatic lipase, α-amylase and α- glucosidase, and in vivo laxative activity in rats. The metabolite phthalic acid ester (1) exhibited moderate inhibitory activity against pancreatic lipase (IC50 = 24.43 ± 0.096 μg/mL) and relatively good activity against α-glucosidase (IC50 = 10.28 ± 0.015 μg/mL). Sweroside (2) displayed weak activity against α-glucosidase (IC50 = 40.28 ± 0.063 μg/mL) but significantly (p<0.05) increased the feacal output of the treated animals compared to the normal and sodium picosulfate controls.

[Effectiveness of School-based Interventions for the Prevention and/or Reduction of Psychosocial Problems among Children and Adolescents: A Review of Reviews]. / Wirksamkeit von schulbasierten Interventionen zur Prävention und/oder Reduktion psychosozialer Probleme bei Kindern und Jugendlichen: Ein Review von Reviews.

Objective: To summarize the current evidence on the effectiveness of school-based interventions for the maintenance of mental health and the prevention of psychosocial problems among pupils. Methods: A systematic literature search of reviews published between 2007 and 2015 was carried out. Databases searched included Medline, PsycINFO, Campbell Library, Cochrane Library, NICE, ERIC, and Web of Science. Study selection, data extraction, and quality assessment (using AMSTAR criteria) were performed by 2 independent reviewers. Results: 6 reviews covering 331 primary studies were included in this review of reviews. Findings of three reviews with a focus on the maintenance and/or promotion of mental health and general well-being suggested that interventions aimed at changes in the social and the school environment were more effective than those that only targeted individual behavior change among pupils. Interventions for the reduction of mobbing/bullying were most effective if they comprised organizational changes at schools, such as playground and schoolyard supervision, and disciplinary measures. One review suggested strong evidence for the effectiveness of classroom management to reduce violent behavior among pupils. Conclusions: Participation in interventions promoting changes in the school environment, in addition to individual behavior change, appears to be associated with improved mental health among pupils and reductions in mobbing/bullying and violent behavior at schools.

Intra-articular Hyaluronic Acid (HA) and Platelet Rich Plasma (PRP) injection versus Hyaluronic acid (HA) injection alone in Patients with Grade III and IV Knee Osteoarthritis (OA): A Retrospective Study on Functional Outcome.

Introduction: Intra-articular hyaluronic acid (HA) is widely utilized in the treatment of knee osteoarthritis whereas platelet rich plasma (PRP) enhances the regeneration of articular cartilage. This study analyses the efficacy of HA and PRP in grade III and IV knee osteoarthritis. Methodology: This is a cross sectional study with retrospective review of 64 patients (101 knees) which includes 56 knees injected with HA+ PRP, and 45 knees with HA only. Results: During the post six months International Knee Documentation Committee (IKDC) evaluation, HA+PRP group showed marked improvement of 24.33 compared to 12.15 in HA group. Decrement in visual analogue score (VAS) in HA+PRP was 1.9 compared to 0.8 in HA group. Conclusion: We propose intra-articular HA and PRP injections as an optional treatment modality in Grade III and IV knee osteoarthritis in terms of functional outcome and pain control for up to six months when arthroplasty is not an option.

Preclinical profile of bacopasides from Bacopa monnieri (BM) as an emerging class of therapeutics for management of chronic pains.

Chronic pains management costs billions of dollars in medical exchequer to the world population. Additionally, 77% of people with chronic pains also have a degree of medically treatable depression. Opioids have a narrower safety index due to their side effects associated with its tolerance, hyperalgesia and subsequent dependence. Likewise, non steroidal anti-inflammatory drugs and anticonvulsants, also have limited safety and tolerability profile in the management of chronic pains. Bacopa monnieri, a renowned ayurvedic medicine has a strong antidepressant effect and significant antinociceptive effect, which is comparable to the effect of morphine via adenosinergic, opioidergic, and adrenergic mechanisms. BM has been also reported to be effective in neuropathic pains. Additionally, it has a strong anti-inflammatory effect mediated via COX-2 inhibitory mechanism. Apart from its effect of augmenting morphine analgesia, BM also inhibits opioid-withdrawal induced hyperalgesia, and acquisition and expression of morphine tolerance. BM is reported to have a strong protective effect against toxic effects of opiates on major organs like brain, kidneys and heart. BM is well documented to be safe and well tolerated herbal therapy in multiple clinical trials including various age groups. This minireview evaluated the preclinical data that highlights potential of BM as a future candidate for clinical management of chronic pains.

Remifentanil infusion in association with fentanyl-propofol anaesthesia in patients undergoing cardiac surgery: effects on morphine requirement and postoperative analgesia.

BACKGROUND: We have prospectively assessed the effects of remifentanil on morphine requirement in the first hour after emerging from general anaesthesia after elective coronary artery bypass surgery and in the first 12 h postoperatively, and pain and agitation scores in the first hour after emerging from general anaesthesia. METHODS: Twenty patients undergoing off-pump coronary artery bypass surgery, receiving standardized propofol-fentanyl-based anaesthesia, randomly received infusions of either remifentanil 0.1 microg kg(-1) min(-1) (Group R, n=10) or saline (Group S, n=10), each infused at 0.12 ml kg(-1) h(-1). Propofol and trial drug infusion were continued into the postoperative period until the patients were ready to be woken up. Postoperative analgesia was provided with morphine infusion commenced immediately after operation, and was additionally nurse controlled on the basis of a visual analogue scale (VAS) score (0-10). Agitation score was recorded using a VAS of 0-3. RESULTS: In the first hour after discontinuing propofol and trial infusion, morphine requirements were significantly higher in the remifentanil group (8.15 (sd 3.59) mg) compared with the saline group (3.29 (2.36) mg) (P<0.01). There was no difference in the total morphine given during the period after stopping propofol or in the total requirement in the first 12 h postoperatively. There was no significant difference in either pain scores or agitation scores between the two groups. CONCLUSION: Use of remifentanil is associated with increased opioid requirement in the first hour after it has been discontinued.

Inhibition of capsaicin-induced cough by the gamma-aminobutyric acid agonist baclofen.

Gamma-aminobutyric acid (GABA) is a central inhibitory neurotransmitter that also exists in the lungs. The GABA-agonist baclofen has been shown to have antitussive activity via a central mechanism in animals. Recently it was demonstrated that a 14-day course of baclofen given three times daily significantly inhibits the cough reflex in healthy volunteers. Because of the prolonged antitussive effect of baclofen that has been previously observed, the present study was conducted to evaluate the antitussive effect of low-dose, oral baclofen given once daily. Forty-one healthy volunteers were randomly assigned in a double-blind manner to receive a 28-day course of baclofen, either 10 mg or 20 mg once daily, or placebo. Subjects underwent cough challenge testing with inhaled capsaicin to establish baseline cough reflex sensitivity, and subsequently after 14 and 28 days of therapy. Subjects receiving baclofen 20 mg daily demonstrated significant inhibition of cough sensitivity after 14 days and after 28 days of therapy compared with baseline. Neither placebo nor baclofen 10 mg daily had a significant effect on cough sensitivity. No serious side effects were experienced by any study participant. These results confirm the recent observation that baclofen has significant antitussive activity in humans. Further, once-daily administration of a relatively low dose of baclofen is sufficient to achieve significant cough inhibition, although at least 14 to 28 days of therapy may be required to attain maximal antitussive effect. These results support further investigation of baclofen or other GABA-agonists as potential therapeutic agents for chronic, nonproductive cough.

The influence of gender on cough reflex sensitivity.

BACKGROUND: The more common occurrence in women of cough due to angiotensin-converting enzyme inhibitors raises the possibility of gender-related differences in the sensitivity of the cough reflex. Of two recent studies that evaluated cough response to inhaled capsaicin in normal subjects, one demonstrated heightened sensitivity of the cough reflex in women compared with men, while the other revealed no gender-related differences. To further investigate this question, we reviewed our experience with cough challenge testing in normal volunteers. STUDY OBJECTIVE: To compare cough reflex sensitivity in healthy adult female and male subjects. DESIGN: Retrospective data analysis. SETTING: Academic medical center. PARTICIPANTS: One hundred healthy volunteers (50 male, 50 female). INTERVENTIONS: Subjects inhaled capsaicin in ascending, doubling concentrations until the concentration inducing five or more coughs (C5) was reached. In addition, the concentration inducing two or more coughs (C2; cough threshold) was measured. RESULTS: Mean log C5 was significantly lower in women than in men: 1.02+/-0.09 (SEM) microM vs 1.41+/-0.08 microM, respectively (p=0.002). Log C2 (cough threshold) was also significantly lower in female subjects: 0.534+/-0.068 microM vs 0.870+/-0.065 microM in male subjects (p=0.00058). CONCLUSION: Healthy women have a more sensitive cough reflex than do healthy men. The reasons for this significant gender difference remain to be elucidated, but may involve a heightened sensitivity, in women, of the sensory receptors within the respiratory tract that mediate cough.

Treatment of chronic, refractory cough with baclofen.

Chronic, nonproductive cough may result from enhanced sensitivity of the cough reflex. Often, this debilitating symptom is refractory to standard antitussive therapy. Baclofen, an agonist of gamma-aminobutyric acid (GABA), has been shown, in animals, to have antitussive activity via a central mechanism. Recently, in normal subjects, we have demonstrated the ability of baclofen to inhibit capsaicin-induced cough, as well as cough due to angiotensin-converting enzyme (ACE) inhibitors. Herein, we describe two patients with chronic, refractory cough who obtained symptomatic improvement after a 14-day course of low-dose, oral baclofen, administered in a double-blind, placebo-controlled manner. In addition, both subjects demonstrated significant increases in cough threshold to inhaled capsaicin after treatment with baclofen.

The Coventry thermal injury study.

Two hundred and fifty-six consecutive new patients seen in the weekly burns outpatient clinic were questioned, concerning details of their injury and first aid measures taken, and the information was recorded on a questionnaire. Following computer analysis, an interesting pattern of incidence, susceptible age groups, 'danger zones', and first aid given in the community emerged. Conclusions regarding burn prevention and first aid have been drawn.