Zainul Amiruddin Zakaria

Evaluation of the antinociceptive activity of Ficus deltoidea aqueous extract.

The aqueous extract of Ficus deltoidea leaves was evaluated for possible antinociceptive activity in three models of nociception, namely, acetic acid-induced abdominal writhing, formalin and hot plate test. The results of the present study showed that intraperitoneal administration of the F. deltoidea leaves aqueous extract at the dose of 1, 50 and 100 mg/kg, 30 min prior to pain induction produced significant dose-dependent antinociceptive effect in all the models used, which indicating the presence of both central and peripherally mediated activities. Furthermore, the antinociceptive effect of the extract in the formalin and hot plate test was reversed by the non-selective opioid receptor antagonist naloxone suggesting that the endogenous opioid system is involved in its analgesic mechanism of action. Thus, the present results demonstrated that F. deltoidea leaves aqueous extract contains pharmacologically active constituents which possess antinociceptive activity justifying its popular therapeutic use in treating conditions associated with the painful conditions.

Antinociceptive activity of the essential oil of Zingiber zerumbet.

In the present study, the rhizome essential oil from Zingiber zerumbet (Zingiberaceae) was evaluated for antinociceptive activity using chemical and thermal models of nociception, namely, the acetic acid-induced abdominal writhing test, the hot-plate test and the formalin-induced paw licking test. It was demonstrated that intraperitoneal administration of the essential oil of Z. zerumbet (EOZZ) at the doses of 30, 100 and 300 mg/kg produced significant dose-dependent inhibition of acetic acid-induced abdominal writhing, comparable to that of obtained with acetylsalicylic acid (100 mg/kg). At the same doses, the EOZZ produced significant dose-dependent increases in the latency time in the hot-plate test with respect to controls, and in the formalin-induced paw licking test, the EOZZ also significantly reduced the painful stimulus in both neurogenic and inflammatory phase of the test. In addition, the antinociceptive effect of the EOZZ in the formalin-induced paw licking test as well as hot-plate test was reversed by the nonselective opioid receptor antagonist, naloxone suggesting that the opioid system was involved in its analgesic mechanism of action. On the basis of these data, we concluded that the EOZZ possessed both central and peripheral antinociceptive activities which justifying its popular folkloric use to relieve some pain conditions.

Complementary alternative medicine use among patients with type 2 diabetes mellitus in the primary care setting: a cross-sectional study in Malaysia

BackgroundLimited study on the use of complementary alternative medicine (CAM) among patients with diabetes mellitus (DM), particularly in primary -care settings. This study seeks to understand the prevalence, types, expenditures, attitudes, beliefs, and perceptions of CAM use among patients with DM visiting outpatient primary care clinics.MethodsThis is a descriptive, cross-sectional study of 240 diabetic patients. CAM is defined as a group of diverse medical and healthcare systems, practices, and products that are not generally considered part of conventional Western medicine. Data analysis was done using SPSS v. 19 and multiple logistic regressions were used to identify predictors of CAM use.ResultsThe prevalence of CAM use was 62.5 percent. Female were 1.8 times more likely than male in using CAM. Malays (75%) were the most frequent users, followed Indians (18%) and Chinese (6%). Biological therapy (50.0%) were the most widely used, followed by manipulative-body based systems (9.2%), energy system (8.8%), alternative medicine systems (4.6%) and mind-body system (1.7%). In biological therapy, a total of 30.4 percent, 24.2 percent, 13.3 percent, and 7.9 percent of diabetic patients consumed bitter gourd (Momordica Charantia), followed by Misai Kucing (Orthosiphon Stamineus Benth), garlic (Allium Sativum), and Sabah snake grass (Clinacanthus Nutans Lindau) respectively. The mean of the expenditure on CAM usage was RM 52.8 ± 101.9 (US

Zerumbone-Induced Antinociception: Involvement of the l-Arginine-Nitric Oxide-cGMP -PKC-K+ATP Channel Pathways

16.9 ± 32.5) per month. According to multiple logistic regression analyses, being Muslim (OR 5.258, 95 percent CI 2.952-9.368) had significant positive association with CAM use.ConclusionsThe prevalence of CAM use was high among diabetics. Islam faith is predictor for CAM use among Type 2 DM patients. The most-common herbs used were bitter gourd (Momordica Charantia) and Misai Kucing (Orthosiphon Stamineus, Benth). Further studies on the anti-glycemic activity of the isolated compound may be needed in the future.

Flavonoid combinations cause synergistic inhibition of proinflammatory mediator secretion from lipopolysaccharide-induced RAW 264.7 cells

This study investigated the antinociceptive effects of zerumbone in chemical behavioural models of nociception in mice. Zerumbone given through intraperitoneal route (i.p.) produced dose-related antinociception when assessed on acetic acid-induced abdominal writhing test in mice. In addition, the i.p. administration of zerumbone exhibited significant inhibition of the neurogenic pain induced by intraplantar (i.pl.) injection of capsaicin and bradykinin. Likewise, zerumbone given by i.p. route reduced the nociception produced by i.pl. injection of glutamate and phorbol myristate acetate (PMA). The antinociception caused by zerumbone in the acetic acid test was significantly attenuated by i.p. pre-treatment of mice with l-arginine (nitric oxide precursor) and glibenclamide (ATP-sensitive K(+) channel inhibitor). However, the antinociception of zerumbone was enhanced by methylene blue (non-specific gyanylyl cyclase inhibitor). Together, these results indicate that zerumbone produces pronounced antinociception against chemical models of nociception in mice. It also strongly suggests that the l-arginine-nitric oxide-cGMP-PKC-K(+) ATP channel pathways, the TRPV1 and kinin B2 receptors play an important role in the zerumbone-induced antinociception.

In vitro antiproliferative and antioxidant activities of the extracts of Muntingia calabura leaves.

ObjectivesWe evaluated several flavonoid combinations for synergy in the inhibition of proinflammatory mediator synthesis in the RAW 264.7 cellular model of inflammation.MethodsThe inhibitory effect of chrysin, kaempferol, morin, silibinin, quercetin, diosmin and hesperidin upon nitric oxide (NO), prostaglandin E2 (PGE2) and tumour necrosis factor-α (TNF-α) secretion from the LPS-induced RAW 264.7 monocytic macrophage was assessed and IC50 values obtained. Flavonoids that showed reasonable inhibitory effects in at least two out of the three assays were combined in a series of fixed IC50 ratios and reassessed for inhibition of NO, PGE2 and TNF-α. Dose–response curves were generated and interactions were analysed using isobolographic analysis.ResultsThe experiments showed that only chrysin, kaempferol, morin, and silibinin were potent enough to produce dose–response effects upon at least two out of the three mediators assayed. Combinations of these four flavonoids showed that several combinations afforded highly significant synergistic effects.ConclusionsSome flavonoids are synergistic in their anti-inflammatory effects when combined. In particular chrysin and kaempferol significantly synergised in their inhibitory effect upon NO, PGE2 and TNF-α secretion. These findings open further avenues of research into combinatorial therapeutics of inflammatory-related diseases and the pharmacology of flavonoid synergy.

Preliminary analysis of the antinociceptive activity of zerumbone

The in vitro antiproliferative and antioxidant activities of the aqueous, chloroform and methanol extracts of Muntingia calabura leaves were determined in the present study. Assessed using the 3,(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) (MTT) assay, the aqueous and methanol extracts of M. calabura inhibited the proliferation of MCF-7, HeLa, HT-29, HL-60 and K-562 cancer cells while the chloroform extract only inhibited the proliferation of MCF-7, HeLa, HL-60 and K-562 cancer cells. Interestingly, all extracts of M. calabura, which failed to inhibit the MDA-MB-231 cells proliferation, did not inhibit the proliferation of 3T3 (normal) cells, indicating its safety. All extracts (20, 100 and 500 μg/ml) were found to possess antioxidant activity when tested using the DPPH radical scavenging and superoxide scavenging assays with the methanol, followed by the aqueous and chloroform, extract exhibiting the highest antioxidant activity in both assays. The total phenolic content for the aqueous, methanol and chloroform extracts were 2970.4 ± 6.6, 1279.9 ± 6.1 and 2978.1 ± 4.3 mg/100 g gallic acid, respectively. In conclusion, the M. calabura leaves possess potential antiproliferative and antioxidant activities that could be attributed to its high content of phenolic compounds, and thus, needs to be further explored.

Anti-inflammatory and antinociceptive effects of Mitragyna speciosa Korth methanolic extract.

We have investigated the antinociceptive activity of zerumbone (1), a natural cyclic sesquiterpene isolated from Zingiber zerumbet Smith, in acetic acid-induced abdominal writhing test and hot plate test in mice. 1 given by intraperitoneal route produced significant dose-dependent antinociceptive effect in all the test models used. In addition, the antinociceptive effect of 1 in the hot plate test was reversed by the non-selective opioid receptor antagonist naloxone, suggesting that the opioid system is involved in its analgesic mechanism of action.

Antinociceptive, anti-inflammatory and antipyretic effects of Muntingia calabura aqueous extract in animal models

Objectives: To determine the anti-inflammatory and antinociceptive activities of Mitragyna speciosa Korth methanol extract in rodents. Materials and Methods: Anti-inflammatory activity was evaluated using carrageenan-induced paw edema and cotton pellet-induced granuloma tests in rats. Antinociceptive activity was measured using the writhing test and the hot plate test in mice, and the formalin test in rats. All drugs and extracts were diluted in dH2O and administered through the intraperitoneal route. Results were analyzed using one-way ANOVA followed by Dunnett’s test for multiple comparisons among groups. Results: Results showed that intraperitoneal administration of the extract at doses of 100 and 200 mg/kg produced significant dose-dependent activity in all of the nociceptive models evaluated (p < 0.05). With the formalin test, the antinociceptive activity in mice was inhibited only at the highest dose of the extract (200 mg/kg). The study also showed that intraperitoneal administration of the methanol extract of M. speciosa (100 and 200 mg/kg) significantly and dose-dependently suppressed the development of carrageenan-induced rat paw edema (p < 0.05). In the chronic test, however, significant reduction in granulomatous tissue formation in rats was observed only at the highest dose of the methanol extract of M. speciosa (200 mg/kg, p < 0.05). Conclusion: The present study suggests the presence of potent antinociceptive and anti-inflammatory principles in the extract, supporting its folkloric use for the treatment of these conditions.

The antinociceptive action of aqueous extract from Muntingia calabura leaves: the role of opioid receptors.

The present study was carried out to elucidate the potential of aqueous extract of Muntingia calabura leaves aqueous extract (MCAE) as antinociceptive, anti-inflammatory and antipyretic agents using the formalin-, carrageenan-induced paw edema- and brewer’s yeast-induced pyrexia tests in rats. The extract was prepared by soaking the dried powdered leaves of M. calabura in distilled water (dH2O) overnight. The supernatant obtained, considered as a stock solution (100% concentration/strength), was then diluted to concentrations of 10% and 50% and used together in all experimental models. The MCAE, at concentrations of 10%, 50% and 100%, were found to show significant antinociceptive, anti-inflammatory and antipyretic activities in all tests. However, all of the activities occurred in a concentration-independent manner. The 50% and 100% concentrations of MCAE produced insignificant antinociceptive and antipyretic activities, respectively. Although the 100% concentration of MCAE produced significant (P<0.05) anti-inflammatory activity, the activity was lower than that of the 10% and 50% concentrations of MCAE. Based on the results, we conclude that the M. calabura leaves possessed antinociceptive, anti-inflammatory and antipyretic activities and, thus, justifies the Peruvian folklore claims of its medicinal values.