Antipyretic and Anticonvulsant Activity of Polygonatum verticillatum: Comparison of Rhizomes and Aerial Parts

The current study was undertaken to explore the antipyretic and anticonvulsant profile of the Polygonatum verticillatum in established pharmacological paradigms. The crude methanol extract of rhizomes (PR) and aerial parts (PA) of the plant were tested in Brewer's‐yeast‐induced pyrexia and pentylenetetrazole‐induced convulsion test. PR and PA both evoked prominent antipyretic activity (p < 0.01) in a dose‐dependent manner during all assessment times at the dose of 50, 100, and 200 mg/kg intraperitoneally. The protection elicited by PR (82.20%) at 200 mg/kg was comparable with aspirin (88.48%) as a standard drug at 100 mg/kg. However, PA was less potent, and maximum protection was 64% at 200 mg/kg. Both PR and PA were devoid of any anticonvulsant activity. Our results demonstrated prominent evidence of antipyretic activity of P. verticillatum that is consistent with the folk uses of the plant. In addition from a biodiversity point of view, PA of the plant can also be used as an alternate of PR. Copyright © 2012 John Wiley & Sons, Ltd.     

The Prokinetic,Laxative, and Antidiarrheal Effects of Morus nigra: Possible Muscarinic,Ca2+ Channel Blocking,and Antimuscarinic Mechanisms

Morus nigra Linn. (black mulberry) is used in gastrointestinal ailments. This study demonstrates gut modulatory properties of M. nigra. The prokinetic, laxative, and antidiarrheal activities of M. nigra were assessed in mice, while isolated rabbit jejunum and guinea‐pig ileum were used to explore insight into mechanism(s). At 30 and 70 mg/kg, the crude extract of M. nigra (Mn.Cr) exhibited atropine‐sensitive prokinetic and laxative effects, similar to carbachol (CCh). While at higher doses (100, 300, and 500 mg/kg), Mn.Cr offered protection against castor oil‐induced diarrhea. In rabbit jejunum, Mn.Cr and its chloroform fraction inhibited CCh‐induced contractions more potently compared with high K⁺ (80 mm ). Conversely, petroleum fraction was more potent against high‐K⁺‐induced contractions. At 0.01 mg/mL, Mn.Cr caused a parallel shift in acetylcholine concentration–response curves (CRCs) followed by a non‐parallel shift at 0.03 mg/mL, similar to dicyclomine. At further tested concentrations, Mn.Cr (0.1 and 0.3 mg/mL) and petroleum fraction suppressed Ca²⁺ CRCs, similar to verapamil. In guinea‐pig ileum, Mn.Cr, its aqueous and ethyl acetate fractions exhibited atropine‐sensitive gut stimulant activity along with additional uncharacterized excitatory response in the aqueous fraction only. These results suggest that black mulberry possesses prokinetic, laxative, and antidiarrheal effects, putatively mediated through cholinomimetic, antimuscarinic, and Ca²⁺ antagonist mechanisms, respectively. Copyright © 2016 John Wiley & Sons, Ltd.     

Triple-component nanocomposite films prepared using a casting method: Its potential in drug delivery

The purpose of this study was to fabricate a triple-component nanocomposite system consisting of chitosan, polyethylene glycol (PEG), and drug for assessing the application of chitosan–PEG nanocomposites in drug delivery and also to assess the effect of different molecular weights of PEG on nanocomposite characteristics. The casting/solvent evaporation method was used to prepare chitosan–PEG nanocomposite films incorporating piroxicam-β-cyclodextrin. In order to characterize the morphology and structure of nanocomposites, X-ray diffraction technique, scanning electron microscopy, thermogravimetric analysis, and Fourier transmission infrared spectroscopy were used. Drug content uniformity test, swelling studies, water content, erosion studies, dissolution studies, and anti-inflammatory activity were also performed. The permeation studies across rat skin were also performed on nanocomposite films using Franz diffusion cell. The release behavior of films was found to be sensitive to pH and ionic strength of release medium. The maximum swelling ratio and water content was found in HCl buffer pH 1.2 as compared to acetate buffer of pH 4.5 and phosphate buffer pH 7.4. The release rate constants obtained from kinetic modeling and flux values of ex vivo permeation studies showed that release of piroxicam-β-cyclodextrin increased with an increase in concentration of PEG. The formulation F10 containing 75% concentration of PEG showed the highest swelling ratio (3.42 ± 0.02) in HCl buffer pH 1.2, water content (47.89 ± 1.53%) in HCl buffer pH 1.2, maximum cumulative drug permeation through rat skin (2405.15 ± 10.97 μg/cm²) in phosphate buffer pH 7.4, and in vitro drug release (35.51 ± 0.26%) in sequential pH change mediums, and showed a significantly (p < 0.0001) higher anti-inflammatory effect (0.4 cm). It can be concluded from the results that film composition had a particular impact on drug release properties. The different molecular weights of PEG have a strong influence on swelling, drug release, and permeation rate. The developed films can act as successful drug delivery approach for localized drug delivery through the skin.     

Therapeutic Potential of Turmeric in Alzheimer's Disease: Curcumin or Curcuminoids?

Alzheimer's disease (AD) is the most common form of dementia. There is limited choice in modern therapeutics, and drugs available have limited success with multiple side effects in addition to high cost. Hence, newer and alternate treatment options are being explored for effective and safer therapeutic targets to address AD. Turmeric possesses multiple medicinal uses including treatment for AD. Curcuminoids, a mixture of curcumin, demethoxycurcumin, and bisdemethoxycurcumin, are vital constituents of turmeric. It is generally believed that curcumin is the most important constituent of the curcuminoid mixture that contributes to the pharmacological profile of parent curcuminoid mixture or turmeric. A careful literature study reveals that the other two constituents of the curcuminoid mixture also contribute significantly to the effectiveness of curcuminoids in AD. Therefore, it is emphasized in this review that each component of the curcuminoid mixture plays a distinct role in making curcuminoid mixture useful in AD, and hence, the curcuminoid mixture represents turmeric in its medicinal value better than curcumin alone. The progress in understanding the disease etiology demands a multiple‐site‐targeted therapy, and the curcuminoid mixture of all components, each with different merits, makes this mixture more promising in combating the challenging disease. Copyright © 2013 John Wiley & Sons, Ltd.     

Effects of folate, vitamin B-12 and vitamin B-6 supplementation on methionine-induced hyperhomocysteinemia in rats

An excessive intake of dietary methionine increases plasma total homocysteine (tHcy, an independent risk factor for premature cardiovascular disease) by enhancing the synthesis of homocysteine. Information on the influence of excess dietary vitamins involved in homocysteine metabolism on the methionine-induced hyperhomocysteinemia is, however, limited. Thus, a six-week study was conducted to determine the influence of excess folic acid, vitamin B-12 and vitamin B-6 on the methionine-induced hyperhomocysteinemia in rats. Supplementation of the casein control diet with 10 and 20 g/kg L-Met increased plasma tHcy to 2.0 and 8.0 times control, respectively. The hyperhomocysteinemia caused by the addition of 10 g/kg L-Met to the control diet, was completely counteracted by extra folic acid or three vitamins combined (folic acid, 2 mg/kg; vitamin B-12, 25 μg/kg; plus vitamin B-6, 6 mg/kg) but the addition of extra vitamin B-12 or vitamin B-6 alone had no effect on plasma tHcy. Similarly, extra dietary folic acid or the three vitamins combined caused substantial reduction in plasma tHcy of rats fed the control diet supplemented with 20 g/kg L-Met but addition of vitamin B-12 or vitamin B-6 alone exacerbated plasma tHcy.     

Knowledge and attitudes of physicians in Iran with regard to chronic cancer pain.

BACKGROUND AND AIM: The knowledge and attitudes of health care professionals with regard to pain and its impact on the patient are among identified barriers that prevent health care professionals from providing effective treatment for pain. The purpose of the present study was to evaluate knowledge about and attitudes towards cancer pain and its management in Iranian physicians with patient care responsibilities. METHODS: We surveyed 122 physicians in six university hospitals in Tehran. Fifty-five (45.1%) questionnaires were completed. RESULTS: The majority of physicians (76%) recognized the importance of pain management priority and about one half of the physicians acknowledged the problem of inadequate pain management in their settings. Most cited inability to access professionals who practice specialized methods in this field, and inadequate staff knowledge of pain management as barriers to good pain management. A large majority of them expressed dissatisfaction with their training for pain management in medical school and in residency. Furthermore a considerable widespread knowledge deficit among all medical subspecialties and all levels of experience was noted which was significantly more profound in the non-oncologists group and only correlated poorly with number of total treated patients in past 6 months. CONCLUSION: The most significant barrier to the effective management of pain in cancer patients in Iran is deficit in knowledge as identified in this survey. A combination of an active continuing education program on both the international guidelines with routine professional education and dissemination of guidelines is needed to bring about significant improvement in cancer pain control.     

Pharmacokinetics and renal excretion of sulfamethoxazole in sheep

Pharmacokinetics and urinary excretion of sulfamethoxazole were investigated in healthy sheep. From the plasma disappearance curves after intravenous bolus injection (50 mg/kg), the half-life and volume of distribution were found to be 76±14 min and 0.41±0.18 lit/kg respectively. Body clearance was 4.06±1.03 ml/kg/min. Very low Concentration of drug was present in plasma after 3 hours of administration and plasma level at 6 hour was only 4.4±2.0 μg/ml. The renal clearance of sulfamethoxazole (22±2.17 ml/min/10 kg) exceeded the creatinine clearance (9.78±1.57 ml/min/10 kg) which may be due to involvement of active tubular secretion and pH dependent back diffusion. Half of the dose of sulfamethoxazole was excreted as unchanged free drug while acetylated amine comprised of 20 percent within the first 6 hours of drug administration.     

Psychological benefits of prostate cancer screening: the role of reassurance

Objectives The role of reassurance in decision‐making about screening for health problems is largely unknown. We examined the reassurance value of prostate cancer screening in primary care patients. Setting and participants One hundred and sixty eight men, aged 45–70 years, who had no history of prostate cancer, from three family medicine practices in southeast Texas. Methods A hypothetical scenario was developed where men were asked to assume they did not have prostate cancer, and then to rank three predefined screening states with regard to reassurance value: (A) unknown (no screening), (B) normal by screening [a prostate‐specific antigen (PSA) test and a digital rectal examination (DRE)] and (C) normal by biopsy (abnormal PSA test and DRE results but a negative ultrasound‐guided prostate biopsy). Results Most of the men (96.8%) associated some reassurance value with screening, considering health state A to be the worst possible health state. Results from a multivariate analysis showed that preference for screening state C was associated with a family history of prostate cancer and perceived greater risk for prostate cancer compared with other men. Conclusion These findings suggest that prostate cancer screening may have some reassurance value for men, and that increased risk status may explain why some men prefer the added reassurance afforded by screening.     

Presence of acetylcholine-like substance(s) inSesamum indicum

Alcoholic extract of seeds ofSesamum indicum (SI, 1–30 mg/kg) caused hypotensive action in anesthetized rats. Heart rate was also decreased at slightly higher doses (10–30 mg/kg). Pretreatment with atropine (2 mg/kg) abolished these cardiovascular responses. In isolated spontaneously beating atria from guinea-pigs, SI caused decrease in force and rate of atrial contractions. In isolated guinea-pig ileum and rat uterus, SI (100–1000 ug/ml) produced contractile responses. All these actions of SI were abolished in the presence of atropine (1 μM). These results indicate that alcoholic extract of seeds ofSesamum indicum contains acetylcholine-like constituents(s) which explains some of the folkloric uses of plant.