Mefenamic acid (MEF) is a non-steroidal anti-inflammatory drug (NSAID) characterized by low bioavailability with relative high toxicity. Despite the efforts which have been paid to enhance its bioavailability, its inherent toxicity remains the limiting factor for its medical uses. Designing MFE as a prodrug of ester derivatives can attenuate gastrointestinal (GI) toxicity, but shows no advantages in term of therapeutic efficacy. Liposomes have a dual action and would be a promising tool to enhance MFE bioavailability and reduce its gastric and systemic adverse reactions. This review covers the pharmacological and toxicological aspects of MFE and provides substantial trend to enhance its clinical therapy.
The aqueous and ethanolic extracts from four medicinal plants namely Acanthus ilicifolius, Aquilaria
malaccensis, Goniothalamus tapis, and Maesa ramentacea, were tested in vitro against Trypanosoma evansi, a hemoprotozoan parasite causing surra in a vast variety of domesticated and wild animals. The antitrypanosomal activity was evaluated by calculating median inhibitory concentration (IC50), the concentration that gives half maximal growth of the trypanosomes, of the plant extracts. Goniothalamus tapis ethanolic extract showed the most potent antitrypanosomal activity with an IC50 value of 7.6 ± 1.6 μg ml-1. The other extracts scored IC50 values ranging from 36.2 ± 1.3 μg ml-1 to 314.1 ± 37.1 μg ml-1.
Candida albicans, Candida tropicalis and Candida krusei frequently cause many infections in immunodeficient humans. The infection invariably becomes invasive and disseminate to other body sites. Tests of antifungal effect of Azadirachta indica (Neem), Peperomia pellucida (“ketumpang air”) and Allium sativum (Garlic) extracts on the three Candida species through paper disc diffusion method showed that all the three Candida species were resistant to A. indica and P. pellucida, but susceptible to A. sativum extract. Subsequently, the effect of different concentrations of garlic extract on the growth of C. albicans was evaluated to determine the IC50 and LD50. The effect of garlic extract suggests that sublethal doses can reduce the colonization of Candida species in the oral cavity of humans by suppressing the virulent hyphal growth form.
Obesity and overweight are major public health problems. Various factors, such as daily nutritional habits, physical inactivity, and genetic, are related to the prevalence of obesity. Recently, it was revealed that the gut microflora may also play an important role in weight management. Thus, this study aimed to determine the anti-obesity effects of Lactobacillus casei strain Shirota (LcS) compared with those of orlistat in an animal model fed a high-fat diet (HFD).Thirty-two male Sprague-Dawley rats were assigned to four groups fed various diets as follows: a standard diet group, HFD group, HFD supplemented with LcS (108109 colony-forming units (HFD-LcS) group, and HFD group treated with Orlistat (10 mg/kg body weight)). After 15 weeks, the weights of organs, body weight, body fat mass and serological biomarkers were measured. In addition, histological analysis of the liver and adipose tissue was performed.Body weight, body mass index, fat mass, leptin and glucose levels were lower, and high-density lipoprotein and adiponectin levels were higher in the HFD-LcS and HFD-orlistat groups than in the HFD group. In addition a significant difference in body fat mass was observed between HFD-LcS group with HFD-orlistat group (19.19±5.76 g vs. 30.19±7.98 g). Although the interleukin-6 level was significantly decreased in the HFD-LcS and HFD-orlistat groups compared with the HFD group, no significant change was observed in other inflammatory biomarkers.The results of the present study show that LcS supplementation improves body weight management and the levels of some related biomarkers. In addition, LcS supplementation showed a better result in fat mass and alanine aminotransferase reduction than Orlistat. Further studies are needed to elucidate the anti-obesity effects of LcS, with a longer period of supplementation.
The in vitro cytotoxicity tests on the extracts of Mesua beccariana , M. ferrea , and M. congestiflora against Raji, SNU-1, HeLa, LS-174T, NCI-H23, SK-MEL-28, Hep-G2, IMR-32, and K562 were achieved using MTT assay. The methanol extracts of Mesua beccariana showed its potency towards the proliferation of B-lymphoma cell (Raji). In addition, only the nonpolar to semipolar extracts (hexane to ethyl acetate) of the three Mesua species indicated cytotoxic effects on the tested panel of human cancer cell lines. Antioxidant assays were evaluated using DPPH scavenging radical assay and Folin-Ciocalteu method. The methanol extracts of M. beccariana and M. ferrea showed high antioxidant activities with low EC 50 values of 12.70 and 9.77 μ g/mL, respectively, which are comparable to that of ascorbic acid (EC 50 = 5.62 μ g/mL). Antibacterial tests were carried out using four Gram positive and four Gram negative bacteria on Mesua beccariana extracts. All the extracts showed negative results in the inhibition of Gram negative bacteria. Nevertheless, methanol extracts showed some activities against Gram positive bacteria which are Bacillus cereus , methicillin-sensitive Staphylococcus aureus (MSSA), and methicillin-resistant Staphylococcus aureus (MRSA), while the hexane extract also contributed some activities towards Bacillus cereus .
Cosmos caudatus or Ulam Raja in Malay originated from Latin America and transferred to Europe, Africa, and tropical Asia. It has been known for many traditional practices worldwide such as to rigidify bones and tone up blood circulation. The aim of this review is to summarize and discuss the association between phytochemical and pharmacological reports of C. caudatus and their traditional uses via ethnopharmacological approaches. Cosmos caudatus is a traditional medicinal plant used widely for culinary and therapeutic purposes. Phytochemical studies indicated the presence of Phenolic acids, flavonoids, tannins, sesquiterpene lactones, carbohydrates, minerals and vitamins in leaves while phenylpropanoids were in roots. Pharmacological data have been compiled for diverse activities for fresh leaves and extracts such as antihypertensive, antihyperlipidemic, antidiabetic, antimicrobial, antioxidant and antiosteoporotic. These activities experimented by in vitro and in vivo studies. Multiple C. caudatus constituents propose many potential actions in different fields such as neuroprotection, antidepression, and gastroprotection.
Purpose: To determine the effect of aqueous extract of Channa striatus on plasma lipids concentrations, pro-inflammatory cytokines levels, adhesion molecules and arterial plaque formation in cholesterol-fed rabbits. Methods: New Zealand rabbits (n = 30, females) were divided into five groups of six rabbits each as follows: cholesterol control group (0.5 % cholesterol); normal control group (normal diet), positive control group (0.5 % cholesterol + 5 mg/kg atorvastatin); and treatment groups (0.5% cholesterol + 250 mg/kg or 500 mg/kg C. striatus extracts, respectively) for 6 weeks. Blood was taken every 2 weeks and analyzed for total cholesterol (TC), low-density lipoprotein cholesterol (LDL), high-density lipoprotein cholesterol (HDL), triglyceride (TG), tumor necrosis factor-alpha (TNF-α) and interleukin-1 beta (IL-1β). Atherogenic index (AI) was calculated based on LDL:HDL ratio. Results: Cholesterol feeding for 6 weeks resulted in significantly increased TC, LDL, HDL, AI, TG, TNFα and IL-1β when compared to C. striatus-fed rabbits. Serum LDL was 26.34 ± 1.43 mmol/L in C. striatus group to 30.52 ± 0.82 mmol/L in cholesterol group (p < 0.05). C. striatus extract (250 mg/kg) increased HDL by approximately 400 % (6.23 ± 1.76 mmol/L from 0.72 ± 0.18 mmol/L), decreased AI value (4.6 in C. striatus group to 10.4 in cholesterol group). Also, IL-1β and TNF-α concentration also significantly (p < 0.05) reduced with C. striatus administration. Interestingly, down-regulation of ICAM-1 and VCAM-1 expression and reduced plaque formation were observed with C. striatus feeding. Conclusion: Channa striatus extract is effective in reducing atherogenesis. This could be due to the high HDL level produced in 250 mg/kg dose group, and strongly suggests the significance of HDL in preventing atherogenesis even if other lipid profiles remain unchanged
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