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  1. Review on rosmarinic acid extraction, fractionation and its anti-diabetic potential
    Ngo YL, Lau CH, Chua LS
    Food Chem Toxicol, 2018 Nov;121:687-700.
    PMID: 30273632 DOI: 10.1016/j.fct.2018.09.064
    Rosmarinic acid is a bioactive phytochemical that can be found in many herbs as ethnomedicines. It possesses remarkable pharmacological activities, and thus leading to its exploration as a therapeutic drug in diabetes treatment recently. This article reviews the extraction and fractionation techniques for plant-based natural rosmarinic acid and its anti-diabetic potential based on literature data published in journals, books, and patents from 1958 to 2017. Factors affecting the performance of rosmarinic acid extraction and fractionation such as operating temperature, time, solvent to sample ratio and eluent system are compiled and discussed in detail. The inhibitory action of rosmarinic acid against sugar digestive enzymes, and protective action towards pancreatic β-cell dysfunction and glucolipotoxicity mediated oxidative stress are also critically reviewed. The optimal parameters are largely dependent on the applied extraction and fractionation techniques, as well as the nature of plant samples. Previous studies have proven the potent role of rosmarinic acid to control plasma glucose level and increase insulin sensitivity in hyperglycemia. Although rosmarinic acid is readily absorbed by human body, its mechanism after consumption is remained unclear. Intensive studies should be well planned to determine the dosage and toxicity level of rosmarinic acid for efficacy and safe consumption.
    Matched MeSH terms: Cinnamates/pharmacology*; Hypoglycemic Agents/pharmacology*; Plant Extracts/pharmacology*; Depsides/pharmacology*
  2. Fulltext Antioxidant and Neuroprotective Effects Induced by Cannabidiol and Cannabigerol in Rat CTX-TNA2 Astrocytes and Isolated Cortexes
    di Giacomo V, Chiavaroli A, Recinella L, Orlando G, Cataldi A, Rapino M, et al.
    Int J Mol Sci, 2020 05 18;21(10).
    PMID: 32443623 DOI: 10.3390/ijms21103575
    Cannabidiol (CBD) and cannabigerol (CBG) are Cannabis sativa terpenophenols. Although CBD's effectiveness against neurological diseases has already been demonstrated, nothing is known about CBG. Therefore, a comparison of the effects of these compounds was performed in two experimental models mimicking the oxidative stress and neurotoxicity occurring in neurological diseases. Rat astrocytes were exposed to hydrogen peroxide and cell viability, reactive oxygen species production and apoptosis occurrence were investigated. Cortexes were exposed to K+ 60 mM depolarizing stimulus and serotonin (5-HT) turnover, 3-hydroxykinurenine and kynurenic acid levels were measured. A proteomic analysis and bioinformatics and docking studies were performed. Both compounds exerted antioxidant effects in astrocytes and restored the cortex level of 5-HT depleted by neurotoxic stimuli, whereas sole CBD restored the basal levels of 3-hydroxykinurenine and kynurenic acid. CBG was less effective than CBD in restoring the levels of proteins involved in neurotransmitter exocytosis. Docking analyses predicted the inhibitory effects of these compounds towards the neurokinin B receptor. Conclusion: The results in the in vitro system suggest brain non-neuronal cells as a target in the treatment of oxidative conditions, whereas findings in the ex vivo system and docking analyses imply the potential roles of CBD and CBG as neuroprotective agents.
    Matched MeSH terms: Antioxidants/pharmacology*; Cannabidiol/pharmacology*; Cannabinoids/pharmacology*; Neuroprotective Agents/pharmacology*
  3. Fulltext Anti-neoplastic Potential of Flavonoids and Polysaccharide Phytochemicals in Glioblastoma
    Atiq A, Parhar I
    Molecules, 2020 Oct 23;25(21).
    PMID: 33113890 DOI: 10.3390/molecules25214895
    Clinically, gliomas are classified into four grades, with grade IV glioblastoma multiforme being the most malignant and deadly, which accounts for 50% of all gliomas. Characteristically, glioblastoma involves the aggressive proliferation of cells and invasion of normal brain tissue, outcomes as poor patient prognosis. With the current standard therapy of glioblastoma; surgical resection and radiotherapy followed by adjuvant chemotherapy with temozolomide, it remains fatal, because of the development of drug resistance, tumor recurrence, and metastasis. Therefore, the need for the effective therapeutic option for glioblastoma remains elusive. Previous studies have demonstrated the chemopreventive role of naturally occurring pharmacological agents through preventing or reversing the initiation phase of carcinogenesis or arresting the cancer progression phase. In this review, we discuss the role of natural phytochemicals in the amelioration of glioblastoma, with the aim to improve therapeutic outcomes, and minimize the adverse side effects to improve patient's prognosis and enhancing their quality of life.
    Matched MeSH terms: Antineoplastic Agents/pharmacology*; Flavonoids/pharmacology*; Polysaccharides/pharmacology*; Phytochemicals/pharmacology*
  4. Fulltext Residual analysis of chitosan-based agronanofungicides as a sustainable alternative in oil palm disease management
    Maluin FN, Hussein MZ, Yusof NA, Fakurazi S, Maznah Z, Idris AS, et al.
    Sci Rep, 2020 12 18;10(1):22323.
    PMID: 33339951 DOI: 10.1038/s41598-020-79335-6
    The nanoformulations of pesticides have shown great interest from many parties due to their slow release capability and site-specific delivery. Hence, in this work, a new nanoformulation of a fungicide, namely chitosan-hexaconazole nanoparticles with a mean diameter size of 18 nm was subjected to the residual analysis on oil palm tissue, leaf and palm oil (crude palm oil and crude palm kernel oil) using a quick, easy, cheap, effective, rugged and safe (QuEChERS) method coupled with the gas chromatography-micro electron capture detector (GC-µECD). The chitosan-hexaconazole nanoparticles were applied using the trunk injection method at 4.5 g a.i./palm (standard single dose) and 9.0 g a.i./palm (double dose). The fungicide residue was analyzed at 0 (6 h after application), 1, 3, 7, 14, 30, 60, 90, and 120 days after treatment. The palm oil matrices; the crude palm oil (CPO) and crude palm kernel oil (CPKO) were found to be residue-free. However, it was observed that high accumulation of the fungicide in the stem tissue and leaf after the treatment using the chitosan-hexaconazole nanoparticles, which is good for better bioavailability for the treatment of the fungi, Ganoderma boninense. The dissipation kinetic at double dose treatment in the tissue and leaf was found to govern by the second-order kinetic with half-lives (t1/2) of 383 and 515 days, respectively.
    Matched MeSH terms: Fungicides, Industrial/pharmacology*; Pesticides/pharmacology*; Triazoles/pharmacology; Chitosan/pharmacology*
  5. Antioxidative, tyrosinase inhibiting and antibacterial activities of leaf extracts from medicinal ferns
    Lai HY, Lim YY, Tan SP
    Biosci Biotechnol Biochem, 2009 Jun;73(6):1362-6.
    PMID: 19502733
    Leaf extracts of five medicinal ferns, Acrostichum aureum L. (Pteridaceae), Asplenium nidus L. (Aspleniaceae), Blechnum orientale L. (Blechnaceae), Cibotium barometz (L.) J. Sm. (Cyatheaceae) and Dicranopteris linearis (Burm.) underwood var. linearis (Gleicheniaceae), were investigated for their total phenolic content (TPC), and antioxidative, tyrosinase inhibiting and antibacterial activities. The antioxidative activity was measured by assays for radical scavenging against 1,1-diphenyl-2-picrylhydrazyl (DPPH), ferric ion reducing power (FRP), beta-carotene bleaching (BCB) and ferrous ion chelating (FIC). The results revealed B. orientale to possess the highest amount of total polyphenols and strongest potential as a natural antioxidative, tyrosinase inhibiting and antibacterial agent as demonstrated by its strong activities in all related bioassays. The other ferns with antioxidative potential were C. barometz and D. linearis. Except for A. aureum, all ferns showed antibacterial activity which may justify their usage in traditional medicines.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology*; Antioxidants/pharmacology*; Enzyme Inhibitors/pharmacology*; Plant Extracts/pharmacology*
  6. Plant Polyphenols as Neuroprotective Agents in Parkinson's Disease Targeting Oxidative Stress
    Hor SL, Teoh SL, Lim WL
    Curr Drug Targets, 2020;21(5):458-476.
    PMID: 31625473 DOI: 10.2174/1389450120666191017120505
    Parkinson's disease (PD) is the second most prevalent progressive neurodegenerative disorder characterized by the degeneration of dopaminergic neurons in the human midbrain. Various ongoing research studies are competing to understand the pathology of PD and elucidate the mechanisms underlying neurodegeneration. Current pharmacological treatments primarily focused on improving dopamine metabolism in PD patients, despite the side effects of long-term usage. In recent years, it is recognized that oxidative stress-mediated pathways lead to neurodegeneration in the brain, which is associated with the pathophysiology of PD. The importance of oxidative stress is often less emphasized when developing potential therapeutic approaches. Natural plant antioxidants have been shown to mediate the oxidative stress-induced effects in PD, which has gained considerable attention in both in vitro and in vivo studies. Yet, clinical trials on natural polyphenol compounds are limited, restricting the potential use of these compounds as an alternative treatment for PD. Therefore, this review provides an understanding of the oxidative stress-induced effects in PD by elucidating the underlying events contributing to oxidative stress and explore the potential use of polyphenols in improving the oxidative status in PD. Preclinical findings have supported the potential of polyphenols in providing neuroprotection against oxidative stress-induced toxicity in PD. However, limiting factors, such as safety and bioavailability of polyphenols, warrant further investigations so as to make them the potential target for clinical applications in the treatment and management of PD.
    Matched MeSH terms: Antioxidants/pharmacology*; Neuroprotective Agents/pharmacology*; Polyphenols/pharmacology*; Phytochemicals/pharmacology*
  7. Inhibitory activity of cyclohexenyl chalcone derivatives and flavonoids of fingerroot, Boesenbergia rotunda (L.), towards dengue-2 virus NS3 protease
    Kiat TS, Pippen R, Yusof R, Ibrahim H, Khalid N, Rahman NA
    Bioorg Med Chem Lett, 2006 Jun 15;16(12):3337-40.
    PMID: 16621533
    Boesenbergia rotunda (L.) cyclohexenyl chalcone derivatives, 4-hydroxypanduratin A and panduratin A, showed good competitive inhibitory activities towards dengue 2 virus NS3 protease with the Ki values of 21 and 25 microM, respectively, whilst those of pinostrobin and cardamonin were observed to be non-competitive. NMR and GCMS spectroscopic data formed the basis of assignment of structures of the six compounds isolated.
    Matched MeSH terms: Chalcone/pharmacology*; Cyclohexanes/pharmacology*; Flavonoids/pharmacology*; Protease Inhibitors/pharmacology*
  8. Reversal of multidrug resistance (MDR) by aspidofractinine-type indole alkaloids
    Kam TS, Subramaniam G, Sim KM, Yoganathan K, Koyano T, Toyoshima M, et al.
    Bioorg Med Chem Lett, 1998 Oct 06;8(19):2769-72.
    PMID: 9873619
    A series of indole alkaloids of the aspidofractinine-type was assessed for their potential in reversing MDR in vincristine-resistant KB cells. Of the compounds tested, kopsiflorine, kopsamine, pleiocarpine, 11-methoxykopsilongine, lahadinine A and N-methoxycarbonyl-11,12-methylenedioxy-delta 16,17-kopsinine were found to show appreciable activity.
    Matched MeSH terms: Alkaloids/pharmacology*; Antineoplastic Agents, Phytogenic/pharmacology*; Indoles/pharmacology*; Vincristine/pharmacology
  9. Synthesis, characterization and antimicrobial activity of norfloxacin based acetohydrazides
    Walayat K, Ahmad M, Rasul A, Aslam S, Anjum MN, Sultan S, et al.
    Pak J Pharm Sci, 2020 Mar;33(2(Supplementary)):855-860.
    PMID: 32863262
    The drug resistance phenomenon in microbes is resulting in the ineffectiveness of available drugs to treat the infections. Thus, there is a continued need to discover new molecules to combat the drug resistance phenomenon. Norfloxacin is a fluoroquinolone antibiotic that is used for the treatment of urinary tract infections. In this research work, norfloxacin is structurally modified by hybridizing with a range of substituted acetohydrazidic moieties through a multistep reaction. The first step involves the coupling of norfloxacin 1 with methyl chloroacetate followed by the treatment with hydrazine hydrate to result in corresponding acetohydrazide 3. A range of substituted benzaldehydes were reacted with the acetohydrazide to form the targeted series of norfloxacin derivatives 4a-i. The final compounds were screened for antimicrobial activity. Among the tested compounds, 4c, 4d, 4e and 4f displayed better antifungal activity against F.avenaceum, while compound 4c and 4e were active against F. bubigeum.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology*; Antifungal Agents/pharmacology; Hydrazines/pharmacology*; Norfloxacin/pharmacology*
  10. Synthesis, characterization, antibacterial, hemolytic and thrombolytic activity evaluation of 5-(3-chlorophenyl)-2-((N-(substituted)-2-acetamoyl)sulfanyl)-1,3,4-oxadiazole derivatives
    Aziz-Ur-Rehman -, Khan SG, Bokhari TH, Anjum F, Akhter N, Rasool S, et al.
    Pak J Pharm Sci, 2020 Mar;33(2(Supplementary)):871-876.
    PMID: 32863264
    A novel series of 5-(3-Chlorophenyl)-2-((N-(substituted)-2-acetamoyl)sulfanyl)-1,3,4-oxadiazole derivatives was efficiently synthesized and screened for antibacterial, hemolytic and thrombolytic activities. The molecule 7c remained the best inhibitor of all selected bacterial strains and furthermore possessed very low toxicity, 8.52±0.31. Compound 7a 7b and 7f showed very good thrombolytic activity relative to Streptokinase employed as reference drug. In addition to low toxicity and moderately good thrombolytic activity, the synthesized compounds possessed excellent to moderate antibacterial activity, relative to ciprofloxacin. All compounds especially 7b and 7f can be consider for further clinical studies and might be helpful in synthesis of new drugs for treatment of cardiovascular diseases.
    Matched MeSH terms: Anti-Bacterial Agents/pharmacology*; Ciprofloxacin/pharmacology; Fibrinolytic Agents/pharmacology*; Oxadiazoles/pharmacology*
  11. Chemical composition and anticholinesterase inhibitory activity of the essential oil of Pseuduvaria macrophylla (Oliv.) Merr. from Malaysia
    Salleh WMNHW, Khamis S, Nafiah MA, Abed SA
    Nat Prod Res, 2021 Jun;35(11):1887-1892.
    PMID: 31293176 DOI: 10.1080/14786419.2019.1639183
    This study was designed to examine the chemical composition and anticholinesterase inhibitory activity of the essential oil of Pseuduvaria macrophylla (Oliv.) Merr. (Annonaceae) from Malaysia. The essential oil was obtained by hydrodistillation and fully analyzed by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). The analysis led to the identification of thirty-four chemical components that represented 87.7 ± 0.5% of the total oil. The essential oil was found to be rich in germacrene D (21.1 ± 0.4%), bicyclogermacrene (10.5 ± 0.5%), δ-cadinene (5.6 ± 0.2%), α-copaene (5.1 ± 0.3%), and α-cadinol (5.0 ± 0.3%). Anticholinesterase activity was evaluated using Ellman method. The essential oil showed weak inhibitory activity against acetylcholinesterase (I%: 32.5%) and butyrylcholinesterase (I%: 35.4%) assays. Our findings demonstrate that the essential oil could be very useful for the characterization, pharmaceutical and therapeutic applications of the essential oil from Pseuduvaria macrophylla.
    Matched MeSH terms: Cholinesterase Inhibitors/pharmacology*; Oils, Volatile/pharmacology*; Sesquiterpenes/pharmacology; Sesquiterpenes, Germacrane/pharmacology
  12. Synergistic Effect of Polyalthia longifolia Leaf and Antibiotics against Clinical Isolates of Methicillin-Resistant Staphylococcus aureus (MRSA) by Microscopic Technique
    Kirubakari B, Chen Y, Sasidharan S
    Antiinflamm Antiallergy Agents Med Chem, 2020;19(3):323-334.
    PMID: 31113347 DOI: 10.2174/1871523018666190522112902
    BACKGROUND: Polyalthia longifolia is a popular medicinal plant and has been widely used as a traditional remedy for centuries in curing of various ailments. The purpose of this study was conducted to determine the in situ antimicrobial synergistic effects between Polyalthia longifolia leaf ethyl acetate fraction (PLEAF) and ampicillin against MRSA local isolate by using modern microscopy technique.

    METHODS: Hence, the evaluation of the synergistic activity of PLEAF and ampicillin against MRSA local isolate was conducted with scanning electron microscopy (SEM).

    RESULTS: The combinational effect of PLEAF fraction and ampicillin exhibited significant antibacterial activity against MRSA. Bacterial cells observations showed invagination, impaired cell division, extensive wrinkles, cell shrinkage, the appearance of a rougher cell with fibrous matrix and clustered cells which confirmed the synergistic effect of PLEAF and ampicillin against MRSA local isolate by SEM.

    CONCLUSION: Conclusively, the in situ SEM observation proved the synergistic antimicrobial activity between PLEAF fraction and ampicillin to destroy the MRSA resistance bacteria which is an important aspect of PLEAF fraction to be used in the future combinational therapy.

    Matched MeSH terms: Acetates/pharmacology; Ampicillin/pharmacology*; Anti-Infective Agents/pharmacology; Plant Extracts/pharmacology
  13. Fulltext Antioxidant and cytotoxicity effect of rice bran phytic acid as an anticancer agent on ovarian, breast and liver cancer cell lines
    Norhaizan ME, Ng SK, Norashareena MS, Abdah MA
    Malays J Nutr, 2011 Dec;17(3):367-75.
    PMID: 22655458 MyJurnal
    Phytic acid (PA) has been shown to have positive nutritional benefits. There are also claims that it is able to prevent cancer through its antioxidant capability. This study investigated antioxidant activity and cytotoxic effect of PA extracted from rice bran against selected cancer cell lines (i.e. ovarian, breast and liver cancer).
    Matched MeSH terms: Antineoplastic Agents/pharmacology*; Antioxidants/pharmacology*; Phytic Acid/pharmacology*; Plant Extracts/pharmacology
  14. Fulltext Laboratory evaluation of three commercial coil products for protection efficacy against Anopheles gambiae from southern Ghana: a preliminary study
    Avicor SW, Wajidi M FF, Jaal Z
    Trop Biomed, 2015 Jun;32(2):386-9.
    PMID: 26691267 MyJurnal
    Residents in irrigated urban agricultural sites face numerous mosquito problems such as increased mosquito populations and reduced insecticides susceptibility due to the creation of mosquito breeding sites and agricultural use of insecticides and hence require effective protective products against them. In this study, the protection effectiveness of three pyrethroid formulated mosquito coils of Malaysian origin against Anopheles gambiae sensu lato from an irrigated urban agricultural site in Ghana were evaluated for their potential use. Sucrose fed An. gambiae s.l. were exposed to insecticide-containing coils in a 70 cm x 70 cm x 70 cm glass chamber to assess the insecticidal effect of the coils. The 0.005% metofluthrin coil caused the most rapid knockdown of 50% of the test mosquitoes. The mean lethal effect of the coils on An. gambiae s.l. were as follows; 0.005% metofluthrin (86%), 0.3% d-allethrin (74.33%), 0.15% d-trans allethrin (72%) and the 0.25% d-allethrin reference coil (69%). The 0.005% metofluthrin coil achieved the highest insecticidal effect on An. gambiae s.l. compared to the other coils and hence performed better than the others as an anti-mosquito product. All the three test coils were effective against An. gambaie s.l. from the irrigated agricultural site compared to the reference coil.
    Matched MeSH terms: Allethrin/pharmacology; Cyclopropanes/pharmacology; Fluorobenzenes/pharmacology; Insecticides/pharmacology*
  15. Fulltext In vitro activity of fluconazole and voriconazole against clinical isolates of Candida spp. by E-test method
    Madhavan P, Jamal F, Chong PP, Ng KP
    Trop Biomed, 2010 Aug;27(2):200-7.
    PMID: 20962716 MyJurnal
    The in vitro susceptibility of clinical Candida isolates towards fluconazole and voriconazole was determined using the E-test method. A total of 41 clinical isolates recovered from patients since 2004 until 2009 from two local hospitals in Kuala Lumpur, Malaysia were used. These comprised Candida tropicalis, Candida albicans, Candida krusei, Candida parapsilosis, Candida rugosa, Candida dubliniensis and Candida glabrata. Strains from American Type Culture Collection were used as quality control. Lawn cultures of the isolates on RPMI-1640 agar medium supplemented with 2% glucose were incubated with the E-test strips at 35ºC for 48 h. Our results show that 71% were susceptible to fluconazole and 90% were susceptible to voriconazole. All strains of C. krusei were resistant to fluconazole and 50% were susceptible in a dose-dependent manner to voriconazole. There were 66% and 33% of C. glabrata that were resistant to fluconazole and voriconazole. Our study revealed that majority of the clinical Candida isolates was susceptible to fluconazole and voriconazole with a small percentage being resistant to both the drugs.
    Matched MeSH terms: Antifungal Agents/pharmacology*; Pyrimidines/pharmacology*; Triazoles/pharmacology*; Fluconazole/pharmacology*
  16. Fulltext Insecticide resistance development in Culex quinquefasciatus (Say), Aedes aegypti (L.) and Aedes albopictus (Skuse) larvae against malathion, permethrin and temephos
    Hamdan H, Sofian-Azirun M, Nazni W, Lee HL
    Trop Biomed, 2005 Jun;22(1):45-52.
    PMID: 16880753
    Laboratory-bred females of Culex quinquefasciatus, Aedes aegypti and Aedes albopictus from the insectarium, Unit of Medical Entomology, Institute for Medical Research were used in the experiment. The late third stage of the F0 larvae which survived the high selection pressure of malathion, permethrin and temephos were reared and colonies were established from adults that emerged. Cx. quinquefasciatus larvae were subjected to selection by malathion and permethrin for 40 generations, Ae. aegypti larvae to malathion, permethrin and temephos for 32 generations and Ae. albopictus larvae were selected against malathion and permethrin for 32 generations and 20 generations against temephos. The rate of resistance development was measured by LC50 value. Cx. quinquefasciatus larvae developed higher resistance to malathion and permethrin compared to Ae. aegypti and Ae. albopictus. On the whole, permethrin resistance developed at a faster rate than malathion and temephos.
    Matched MeSH terms: Temefos/pharmacology; Insecticides/pharmacology*; Malathion/pharmacology; Permethrin/pharmacology
  17. Fulltext Resistance development and insecticide susceptibility in Culex quinquefasciatus against selection pressure of malathion and permethrin and its relationship to cross-resistance towards propoxur
    Selvi S, Endah MA, Nazni WA, Lee HL, Azahari AH
    Trop Biomed, 2005 Dec;22(2):103-13.
    PMID: 16883275
    To determine resistance level and characterize malathion and permethrin resistance in Culex quinquefasciatus, two methods were used namely: WHO procedures of larval bioassay to determine the susceptibility of lethal concentration (LC) and adult bioassay to determine the lethal time (LT) which are resistant to malathion and permethrin. These mosquito strains were bred in the Insectarium, Division of Medical Entomology, IMR. Thousands of late fourth instar larvae which survived the selection pressure to yield 50% mortality of malathion and permethrin were reared and colonies were established from adults that emerged. Larvae from these colonies were then subjected to the subsequent 10 generations in the test undertaken for malathion resistant strain (F61 - F70) and permethrin resistant strain (F54 - F63). Selection pressure at 50% - 70% mortality level was applied to the larvae of each successive generation. The rate of resistance development and resistance ratio (RR) were calculated by LC5 0 for larval bioassay and LT50 value for adult bioassay. The lab bred Cx. quinquefasciatus was used as a susceptible strain for comparison purpose. The adult bioassay test was carried out by using diagnostic dosages of malathion 5.0%, permethrin 0.75% and with propoxur 0.1%. All bioassay results were subjected to probit analysis. The results showed that LC5 0 for both malathion (F61 - F70) and permethrin (F54 - F63) resistant Cx. quinquefasciatus increased steadily to the subsequent 10 generations indicating a marked development of resistance. The adult female malathion resistant strain have developed high resistance level to malathion diagnostic dosage with resistance ratio 9.3 to 9.6 folds of resistance. Permethrin resistance ratio remained as 1.0 folds of resistance at every generation. It was obvious that malathion resistance developing at a higher rate in adult females compared to permethrin. Female adults exposed to 2 hours of exposure period for propoxur 0.1% showed presence of cross-resistance among the both strains of mosquitoes towards propoxur and it was indicated by 70%-100% mortality at 24 hours post-recovery period.
    Matched MeSH terms: Propoxur/pharmacology; Insecticides/pharmacology*; Malathion/pharmacology*; Permethrin/pharmacology*
  18. Current progress in antimalarial pharmacotherapy and multi-target drug discovery
    Tibon NS, Ng CH, Cheong SL
    Eur J Med Chem, 2020 Feb 15;188:111983.
    PMID: 31911292 DOI: 10.1016/j.ejmech.2019.111983
    Discovery and development of antimalarial drugs have long been dominated by single-target therapy. Continuous effort has been made to explore and identify different targets in malaria parasite crucial for the malaria treatment. The single-target drug therapy was initially successful, but it was later supplanted by combination therapy with multiple drugs to overcome drug resistance. Emergence of resistant strains even against the combination therapy has warranted a review of current antimalarial pharmacotherapy. This has led to the development of the new concept of covalent biotherapy, in which two or more pharmacophores are chemically bound to produce hybrid antimalarial drugs with multi-target functionalities. Herein, the review initially details the current pharmacotherapy for malaria as well as the conventional and novel targets of importance identified in the malaria parasite. Then, the rationale of multi-targeted therapy for malaria, approaches taken to develop the multi-target antimalarial hybrids, and the examples of hybrid molecules are comprehensively enumerated and discussed.
    Matched MeSH terms: Antimalarials/pharmacology*; Quinolines/pharmacology*; Paclitaxel/pharmacology*; Artemisinins/pharmacology*
  19. Fulltext Lack of insecticidal effect of mosquito coils containing either metofluthrin or esbiothrin on Anopheles gambiae sensu lato mosquitoes
    Lukwa N, Chiwade T
    Trop Biomed, 2008 Dec;25(3):191-5.
    PMID: 19287356
    Use of mosquito coils for personal protection against malaria and mosquito nuisance is advocated under mosquito and malaria control programmes. We performed field studies of mosquito coils containing either metofluthrin or esbiothrin in experimental huts situated in Kamhororo village, Gokwe district, Zimbabwe. All tests were performed on 3-5 day old reared female Anopheles gambiae sensu lato mosquitoes. The burning times were 9hr 20min for mosquito coils containing metofluthrin and 8 hr for those containing esbiothrin and the results were significantly different (p = <0.001). The mean knock down rate for mosquito coils containing metofluthrin was 90% and that for esbiothrin was 73.3% and the results were significantly different (p = 0.00). Mosquito coils containing metofluthrin had a mean repellence of 92.7% as compared to 85.4% for esbiothrin and the results were not significantly different (p=0.27). The protection time as required by EPA (1999) was 6 hr for mosquito coils containing metofluthrin and 5 hr for those containing esbiothrin. The mean insecticidal effect of mosquito coils containing metofluthrin was 84% as compared to 83% for those containing esbiothrin and the results were not significantly different (p = 0.56). Both mosquito formulations could not be classified as having insecticidal effect since none of them met the 95% mortality rate criteria.
    Matched MeSH terms: Allethrin/pharmacology; Cyclopropanes/pharmacology*; Fluorobenzenes/pharmacology*; Insecticides/pharmacology*
  20. Probing the effects of fish oil on the delivery and inflammation-inducing potential of imiquimod
    Rehman K, Aluwi MF, Rullah K, Wai LK, Mohd Amin MC, Zulfakar MH
    Int J Pharm, 2015 Jul 25;490(1-2):131-41.
    PMID: 26003416 DOI: 10.1016/j.ijpharm.2015.05.045
    Imiquimod is a chemotherapeutic agent for many skin-associated diseases, but it has also been associated with inflammatory side effects. The aim of this study was to prevent the inflammatory effect of commercial imiquimod (Aldara(®)) by controlled release of imiquimod through a hydrogel/oleogel colloidal mixture (CA bigel) containing fish oil as an anti-inflammatory agent. Imiquimod permeability from Aldara® cream and bigel through mice skin was evaluated, and the drug content residing in the skin via the tape stripping technique was quantified. The fish oil fatty acid content in skin along with its lipophilic environment was also determined. An inflammation study was conducted using animal models, and Aldara(®) cream was found to potentially cause psoriasis-like inflammation, which could be owing to prolonged application and excessive drug permeation. Controlled release of imiquimod along with fish oil through CA bigel may have caused reduced imiquimod inflammation. NMR studies and computerized molecular modeling were also conducted to observe whether the fish oil and imiquimod formed a complex that was responsible for improving imiquimod transport and reducing its side effects. NMR spectra showed dose-dependent chemical shifts and molecular modeling revealed π-σ interaction between EPA and imiquimod, which could help reduce imiquimod inflammation.
    Matched MeSH terms: Aminoquinolines/pharmacology*; Anti-Inflammatory Agents/pharmacology; Delayed-Action Preparations/pharmacology; Fish Oils/pharmacology*
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