A bioassay-guided investigation of Melicope ptelefolia Champ ex Benth (Rutaceae) resulted in the identification of an acyphloroglucinol, 2,4,6-trihydroxy-3-geranylacetophenone or tHGA, as the active principle inhibiting soybean 15-LOX. The anti-inflammatory action was also demonstrated on human leukocytes, where the compound showed prominent inhibitory activity against human PBML 5-LOX, with an IC(50) value of 0.42 μM, very close to the effect produced by the commonly used standard, NDGA. The compound concentration-dependently inhibited 5-LOX product synthesis, specifically inhibiting cysteinyl leukotriene LTC(4) with an IC(50) value of 1.80 μM, and showed no cell toxicity effects. The anti-inflammatory action does not seem to proceed via redox or metal chelating mechanism since the compound tested negative for these bioactivities. Further tests on cyclooxygenases indicated that the compound acts via a dual LOX/COX inhibitory mechanism, with greater selectivity for 5-LOX and COX-2 (IC(50) value of 0.40 μM). The molecular features that govern the 5-LOX inhibitory activity was thus explored using in silico docking experiments. The residues Ile 553 and Hie 252 were the most important residues in the interaction, each contributing significant energy values of -13.45 (electrostatic) and -5.40 kcal/mol (electrostatic and Van der Waals), respectively. The hydroxyl group of the phloroglucinol core of the compound forms a 2.56Å hydrogen bond with the side chain of the carboxylate group of Ile 553. Both Ile 553 and Hie 252 are crucial amino acid residues which chelate with the metal ion in the active site. Distorting the geometry of these ligands could be the reason for the inhibition activity shown by tHGA. The molecular simulation studies supported the bioassay results and served as a good model for understanding the way tHGA binds in the active site of human 5-LOX enzyme.
Aceclofenac is a new generation non-steroidal anti-inflammatory drug showing effective anti-inflammatory and analgesic properties. It is available in the form of tablets of 100 mg. Importance of aceclofenac as a NSAID has inspired development of topical dosage forms. This mode of administration may help avoid typical side effects associated with oral administration of NSAIDs, which have led to its withdrawal. Furthermore, aceclofenac topical dosage forms can be used as a supplement to oral therapy for better treatment of conditions such as arthritis. Ointments, creams, and gels containing 1% (m/m) aceclofenac have been prepared. They were tested for physical appearance, pH, spreadability, extrudability, drug content uniformity, in vitro diffusion and in vitro permeation. Gels prepared using Carbopol 940 (AF2, AF3) and macrogol bases (AF7) were selected after the analysis of the results. They were evaluated for acute skin irritancy, anti-inflammatory and analgesic effects using the carrageenan-induced thermal hyperalgesia and paw edema method. AF2 was shown to be significantly (p < 0.05) more effective in inhibiting hyperalgesia associated with inflammation, compared to AF3 and AF7. Hence, AF2 may be suggested as an alternative to oral preparations.
Ketoprofen is a potent non-steroidal anti-inflammatory drug has been used in the treatment of various kinds of pains, inflammation and arthritis. However, oral administration of ketoprofen produces serious gastrointestinal adverse effects. One of the promising methods to overcome these adverse effects is to administer the drug through the skin. The aim of the present work is to evaluate the anti-inflammatory and analgesic effects from topically applied ketoprofen entrapped palm oil esters (POEs) based nanoemulsion and to compare with market ketoprofen product, Fastum(®) gel. The novelty of this study is, use of POEs for the oil phase of nanoemulsion. The anti-inflammatory and analgesic studies were performed on rats by carrageenan-induced rat hind paw edema test and carrageenan-induced hyperalgesia pain threshold test to compare the ketoprofen entrapped POEs based nanoemulsion formulation and market formulation. Results indicated that there are no significant different between ketoprofen entrapped POEs nanoemulsion and market formulation in carrageenan-induced rat hind paw edema study and carrageenan-induced hyperalgesia pain threshold study. However, it shows a significant different between POEs nanoemulsion formulation and control group in these studies at p<0.05. From these results it was concluded that the developed nanoemulsion have great potential for topical application of ketoprofen.
The ethanolic extract of Alpinia conchigera Griff. leaves (EACL) was evaluated for its antinociceptive and anti-inflammatory activities in several in vivo experimental models. Antinociceptive activity was determined using the acetic acid-induced abdominal writhing test, the hot plate test and the formalin test. Anti-inflammatory activity was determined using the carrageenan-induced paw edema test. The extract (30, 100 and 300 mg/kg i.p.) was found to possess significant, dose-dependent inhibitory activity in all test models. In addition, the antinociceptive effect of the extract in the acetic acid-induced writhing and hot plate tests was reversed by naloxone, suggesting that this activity is mediated through activation of the opioid system. These findings suggest that EACL presents notable analgesic and anti-inflammatory activities, which support its folkloric use for painful and inflammatory conditions.
Micro-emulsions and sometimes nano-emulsions are well known candidates to deliver drugs locally. However, the poor rheological properties are marginally affecting their acceptance pharmaceutically. This work aimed to modify the poor flow properties of a nano-scaled emulsion comprising palm olein esters as the oil phase and ibuprofen as the active ingredient for topical delivery. Three Carbopol ® resins: 934, 940 and Ultrez 10, were utilized in various concentrations to achieve these goals. Moreover, phosphate buffer and triethanolamine solutions pH 7.4 were used as neutralizing agents to assess their effects on the gel-forming and swelling properties of Carbopol ® 940. The addition of these polymers caused the produced nano-scaled emulsion to show a dramatic droplets enlargement of the dispersed globules, increased intrinsic viscosity, consistent zeta potential and transparent-to-opaque change in appearance. These changes were relatively influenced by the type and the concentration of the resin used. Carbopol ® 940 and triethanolamine appeared to be superior in achieving the proposed tasks compared to other materials. The higher the pH of triethanolamine solution, the stronger the flow-modifying properties of Carbopol ® 940. Transmission electron microscopy confirmed the formation of a well-arranged gel network of Carbopol ® 940, which was the major cause for all realized changes. Later in vitro permeation studies showed a significant decrease in the drug penetration, thus further modification using 10% w/w menthol or limonene as permeation promoters was performed. This resulted in in vitro and in vivo pharmacodynamics properties that are comparably higher than the reference chosen for this study.
Chemical investigation of the stem bark of Bauhinia rufescens resulted in the isolation of a new cyanoglucoside and menisdaurin from methanol extract and oxepin from petroleum ether extract. The isolated compounds were tested for their anti-inflammatory potentials based on the cyclooxygenase-2 enzyme (COX-2) model. Cyanoglucoside exhibited the highest activity among the compounds with an inhibition activity of 49.34 % at 100 µM (IC50 0.46 µM) compared to the positive control, indomethacin (79.20 %, IC50 0.24 µM).
Adamantyl-based compounds are commercially important in the treatments for neurological conditions and type-2 diabetes, aside from their anti-viral abilities. Their values in drug design are chronicled as multi-dimensional. In the present study, a series of 2-(adamantan-1-yl)-2-oxoethyl benzoates, 2(a-q), and 2-(adamantan-1-yl)-2-oxoethyl 2-pyridinecarboxylate, 2r, were synthesized by reacting 1-adamantyl bromomethyl ketone with various carboxylic acids using potassium carbonate in dimethylformamide medium at room temperature. Three-dimensional structures studied using X-ray diffraction suggest that the adamantyl moiety can serve as an efficient building block to synthesize 2-oxopropyl benzoate derivatives with synclinal conformation with a looser-packed crystal packing system. Compounds 2a, 2b, 2f, 2g, 2i, 2j, 2m, 2n, 2o, 2q and 2r exhibit strong antioxidant activities in the hydrogen peroxide radical scavenging test. Furthermore, three compounds, 2p, 2q and 2r, show good anti-inflammatory activities in the evaluation of albumin denaturation.
Gynura procumbens (Lour.) Merr. (Family Asteraceae) is a medicinal plant commonly found in tropical Asia countries such as China, Thailand, Indonesia, Malaysia, and Vietnam. Traditionally, it is widely used in many different countries for the treatment of a wide variety of health ailments such as kidney discomfort, rheumatism, diabetes mellitus, constipation, and hypertension. Based on the traditional uses of G. procumbens, it seems to possess high therapeutic potential for treatment of various diseases making it a target for pharmacological studies aiming to validate and provide scientific evidence for the traditional claims of its efficacy. Although there has been considerable progress in the research on G. procumbens, to date there is no review paper gathering the reported biological activities of G. procumbens. Hence, this review aims to provide an overview of the biological activities of G. procumbens based on reported in vitro and in vivo studies. In brief, G. procumbens has been reported to exhibit antihypertensive, cardioprotective, antihyperglycemic, fertility enhancement, anticancer, antimicrobial, antioxidant, organ protective, and antiinflammatory activity. The commercial applications of G. procumbens have also been summarized in this paper based on existing patents. The data compiled illustrate that G. procumbens is a potential natural source of compounds with various pharmacological actions which can be utilized for the development of novel therapeutic agents.
Annona muricata is a member of the Annonaceae family and is a fruit tree with a long history of traditional use. A. muricata, also known as soursop, graviola and guanabana, is an evergreen plant that is mostly distributed in tropical and subtropical regions of the world. The fruits of A. muricata are extensively used to prepare syrups, candies, beverages, ice creams and shakes. A wide array of ethnomedicinal activities is contributed to different parts of A. muricata, and indigenous communities in Africa and South America extensively use this plant in their folk medicine. Numerous investigations have substantiated these activities, including anticancer, anticonvulsant, anti-arthritic, antiparasitic, antimalarial, hepatoprotective and antidiabetic activities. Phytochemical studies reveal that annonaceous acetogenins are the major constituents of A. muricata. More than 100 annonaceous acetogenins have been isolated from leaves, barks, seeds, roots and fruits of A. muricata. In view of the immense studies on A. muricata, this review strives to unite available information regarding its phytochemistry, traditional uses and biological activities.
Statins are known to prevent heart failure (HF). However, it is unclear whether statins as class or type (lipophilic or hydrophilic) improve outcomes of established HF.
Introduction: The impact of irrational use of drug is reduction in the quality of drug therapy leading to increased morbidity and mortality. The main objective was to obtain baseline information regarding the prescribing pattern for non-steroidal anti-inflammatory drugs (NSAIDs) by physicians in the outpatient departments (OPDs) of two selected polyclinics in Kota Kinabalu, Sabah. Methods: Four hundred (200 from each polyclinic) prescriptions containing NSAIDs were collected, photocopied and later analyzed. Two hundred selected patients (100 from each polyclinic) attending the OPDs were interviewed using a questionnaire. Results: Educated and higher income group of patients mostly attended in private polyclinic (PPC) whereas comparatively less educated and lower income group of patients generally attended government UMS polyclinic (UPC). Analgesics with no or minimal anti-inflammatory effects were the most commonly prescribed NSAIDs in the OPD of UPC. On the contrary, analgesics with potent anti-inflam-matory effects were the most commonly prescribed NSAIDs in PPC. Due to the nature of potent drugs, socioeco-nomically advantaged patients attending PPC is more likely to develop adverse effects. Therefore, the prescribers in PPC had to prescribe additional drugs to counter the adverse effects of NSAIDs, hence increasing the cost of drugs prescribed compared to UPC. The patients taking NSAIDs before coming to hospital were influenced by pharmacists, friends and doctor’s advice given previously. Conclusions: The overall prescribing pattern of NSAIDs among two polyclinics is satisfactory, although there may be scopes for improvement. Educational intervention can be designed for rational prescribing to improve the quality of health care.
Ipomea aquatica, locally known as water spinach, is one of the most common vegetable consumed by
Malaysian. Based on previous studies, crude extract and phenolic compounds of I. aquatica exhibited
several biological activities including antioxidant, anti-microbial and anti-proliferative. The presence
of phenolic compounds in I. aquatica may contributed to their ability to inhibit enzymes, chelate
metals and scavenge free radicals. Currently, no study reported on anti-inflammatory activity of I.
aquatica with respect to lipoxygenase, hyaluronidase and xanthine oxidase enzymes. The present
study aims to enhance current knowledge on biological properties of I. aquatica crude extract
particularly on anti-inflammatory activity. Three enzymes that involve in inflammatory pathway were
selected in this study including lipoxygenase, hyaluronidase and xanthine oxidase. I. aquatica was
extracted in methanol and tested for lipoxygenase, hyaluronidase and xanthine oxidase at different
concentrations using direct enzyme inhibition assay. Lipoxygenase, hyaluronidase and xanthine
oxidase inhibitory activities of the methanol crude extract increased with increasing
concentration. Highest inhibition activity against lipoxygenase, hyaluronidase and xanthine oxidase
were observed at a concentration of 1000 µg/ml with inhibition of 87.18%, 95.36% and 78.38%,
respectively. Our finding in this study indicates potential anti-inflammatory activity of I. aquatica
crude extract through inhibition of lipoxygenase, hyaluronidase and xanthine oxidase.
Aim: In this study, curcumin was encapsulated in niosomes (Nio-Curc) to increase its effectiveness for the treatment of asthma. Materials & methods: The formulation underwent various physicochemical characterization experiments, an in vitro release study, molecular simulations and was evaluated for in vitro anti-inflammatory activity. Results: Results showed that Nio-Curc had a mean particle size of 284.93 ± 14.27 nm, zeta potential of -46.93 and encapsulation efficacy of 99.62%, which demonstrates optimized physicochemical characteristics. Curcumin release in vitro could be sustained for up to 24 h. Additionally, Nio-Curc effectively reduced mRNA transcript expression of pro-inflammatory markers; IL-6, IL-8, IL-1β and TNF-α in immortalized human airway basal cell line (BCi-NS1.1). Conclusion: In this study, we have demonstrated that Nio-Curc mitigated the mRNA expression of pro-inflammatory markers in an in vitro study, which could be applied to treatment of asthma with further studies.
Medicinal plants have healing properties and are able to synthesize various chemical compounds. These chemicals (also known as phytochemical compounds) play vital roles in determining the pharmacological properties existing in certain plants. The phytochemical compounds present in plants are associated with primary and secondary constituents. Most of the time, the secondary constituents exhibit the bioactivities in plants such as antimicrobial, antioxidant, antidiabetic, antibacterial and anti-inflammatory properties. Some common medicinal plants that have been used in curing various diseases by traditional practitioners in Malaysia are Ficus deltoidea Jack, Andrographis paniculata, Curcuma longa, Clinacanthus nutans and Eurycoma longifolia Jack. This review discusses the morphology, phytochemical compounds and phytochemical properties of selected medicinal plants in Malaysia. The plants of focus have been found to possess anti-cancer and anti-diabetic effects. This review, it is hoped will enable Malaysian researchers to explore further on the potential of these plants in investigating new and novel drugs in the future.
Aloe vera which is also known as Aloe barbadensis Miller,is a plant that is commonly used for medicinal purposes and as treatments for various health issues. It produces two substances; gel and latex, which are used for commercial household products, halal food and cosmetics. Aloe gel is the clear, jelly-like substance found in the inner part of the Aloe leaf while Aloe’s yellow latex comes from the peel. Aloe vera is able to provide therapeutic effects such as wound healing, anti-inflammatory, antioxidant, laxative and antimicrobial properties. The objective of this study was to
investigate the extracts via spectrophotometry (λ = 200 – 400 nm) and liquid chromatography. After 21 days, the ultraviolet spectra showed the evidence of the water molecules interactions and the hydroxyl groups in hydroalcoholic extracts. Significant peaks were also observed in the chromatograms. Further studies evaluating the stability of A. vera extracts should be carried out.
Sinensetin, a plant-derived polymethoxylated flavonoid found in Orthosiphon aristatus var. aristatus and several citrus fruits, has been found to possess strong anticancer activities and a variety of other pharmacological benefits and promising potency in intended activities with minimal toxicity. This review aims to compile an up-to-date reports of published scientific information on sinensetin pharmacological activities, mechanisms of action and toxicity. The present findings about the compound are critically analyzed and its prospect as a lead molecule for drug discovery is highlighted. The databases employed for data collection are mainly through Google Scholar, PubMed, Scopus and Science Direct. In-vitro and in-vivo studies showed that sinensetin possessed strong anticancer activities and a wide range of pharmacological activities such as anti-inflammatory, antioxidant, antimicrobial, anti-obesity, anti-dementia and vasorelaxant activities. The studies provided some insights on its several mechanisms of action in cancer and other disease states. However, more detail mechanistic studies are needed to understand its pharmacological effects. More in vivo studies in various animal models including toxicity, pharmacokinetic, pharmacodynamic and bioavailability studies are required to assess its efficacy and safety before submission to clinical studies. In this review, an insight on sinensetin pharmacological activities and mechanisms of action serves as a useful resource for a more thorough and comprehensive understanding of sinensetin as a potential lead candidate for drug discovery.
Gallic acid (GA) is a phenolic compound found in almost all plants and has been reported to possess powerful health benefits such as anti-oxidant, anti-inflammatory, anti-cancer, and anti-diabetic properties. However, GA suffers a short half-life when administered in vivo. Recent studies have employed graphene oxide (GO), a biocompatible and cost-effective graphene derivative, as a nanocarrier for GA. However, the toxicity effect of this formulated nano-compound has not been fully studied. Thus, the present study aims to evaluate the toxicity and teratogenicity of GA loaded GO (GAGO) against zebrafish embryogenesis to further advance the development of GA as a therapeutic agent. GAGO was exposed to zebrafish embryos (n ≥ 10; 24hr post fertilization (hpf)) at different concentrations (0-500 μg/ml). The development of zebrafish was observed and recorded twice daily for four days. The toxicity of pure GO and GA was also observed at similar concentrations. Distilled water was used as control throughout the experiment. A significantly high mortality rate, delayed hatching rate and low heartbeat were recorded in embryos exposed to GO at concentrations of ≥ 150 μg/ml at 48 hr (p
The growing demand for high value aromatic herb Polygonum minus-based products have increased in recent years, for its antioxidant, anticancer, antimicrobial, and anti-inflammatory potentials. Although few reports have indicated the chemical profiles and antioxidative effects of Polygonum minus, no study has been conducted to assess the benefits of micro-environmental manipulation (different shading levels) on the growth, leaf gas exchange and secondary metabolites in Polygonum minus. Therefore, two shading levels (50%:T2 and 70%:T3) and one absolute control (0%:T1) were studied under eight weeks and 16 weeks of exposures on Polygonum minus after two weeks. It was found that P. minus under T2 obtained the highest photosynthesis rate (14.892 µmol CO2 m-2 s-1), followed by T3 = T1. The increase in photosynthesis rate was contributed by the enhancement of the leaf pigments content (chlorophyll a and chlorophyll b). This was shown by the positive significant correlations observed between photosynthesis rate with chlorophyll a (r2 = 0.536; p ≤ 0.05) and chlorophyll b (r2 = 0.540; p ≤ 0.05). As the shading levels and time interval increased, the production of total anthocyanin content (TAC) and antioxidant properties of Ferric Reducing Antioxidant Power (FRAP) and 2,2-Diphenyl-1-picrylhydrazyl (DPPH) also increased. The total phenolic content (TPC) and total flavonoid content (TFC) were also significantly enhanced under T2 and T3. The current study suggested that P.minus induce the production of more leaf pigments and secondary metabolites as their special adaptation mechanism under low light condition. Although the biomass was affected under low light, the purpose of conducting the study to boost the bioactive properties in Polygonum minus has been fulfilled by 50% shading under 16 weeks' exposure.
Gynura procumbens, commonly known as ‘sambung nyawa’ in Malaysia has been used
traditionally as remedies for anti-inflammatory, anti-hyperlipidimic and anti-hyperglycemic. The
purpose of the present study was to qualitatively evaluate the antimicrobial effects of Gynura procumbens extracts. effects of the sample were determined by disc diffusion method against two bacteria and two fungi namely E. coli, S. aureus, C. albicans and S. cerevisiae. The results showed that the acidic extract of G. procumbens has positive reactions towards E. coli, S. aureus and C. albicans with the presence of zone of inhibition at the concentration of 150 mg/mL. Following the positive reaction, the minimum inhibitory concentration (MIC) of the acidic extract was then evaluated by broth dilution method. The MIC of E. coli and S. aureus were determined at concentration 37.5 mg/mL and 75 mg/mL for C. albicans. It indicated that acidic extracts at lower concentration could inhibit the bacteria, but high concentration of extracts was required in the inhibition of the fungi. It can be concluded that, the present study proves that there is potential of antimicrobial effects in Gynura procumbens leaves extracts.
Erythroxylum cuneatum (E. cuneatum) which belongs to Erythroxylaceae family is a tropical flowering plant from the genus of Erythroxylum. It is used in Malaysia and Thailand's traditional medicines, yet there is limited scientific reports on its medicinal value. This study aimed at exploring the antioxidative and anti-inflammatory properties of E. cuneatum alkaloid leaf extract. The alkaloid extract was obtained through Soxhlet heat extraction method, while the antioxidantive properties were assessed via 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging, ferric reducing antioxidant power (FRAP) and xanthine oxidase inhibition (XOI) assays. Further, anti-inflammatory property of the extract was evaluated on rat's model of carrageenan induced paw model of edema via physical measurements and histology. The extract exhibited antioxidant activity with an EC50 value of 1482 μg/ml in the DPPH radical scavenging assay, an EC1 value of 2191 μg/ml in the FRAP assay and 10.15 ± 6.20% in the XOI assay. Rats pretreated with the extract have shown dose dependent decrease in paw edema when compared to non-treated group of rats. The highest dose (50 mg/kg) of extract exhibited similar effects to aspirin in terms of reducing paw thickness, leucocytes infiltration and disruption of collagen. In conclusion, the E. cuneatum alkaloid leaf extract possesses both antioxidative and anti-inflammatory properties suggesting its potentials for future development of antioxidant and anti-inflammatory drugs.