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1.
Chem Biodivers ; 17(1): e1900419, 2020 Jan.
Article in English | MEDLINE | ID: mdl-31721431

ABSTRACT

This work investigated the polar (PC: protein, amino acid and metabolite) and non-polar (NPC: fatty acid) compounds and bioactivity characteristics of the EBN harvested from the state of Johor in Malaysia. The electrophoretic gels exhibited 15 protein bands (16-173 kD) with unique protein profile. Amino acids analysis by AccQ⋅Tag method revealed 18 types of amino acids in EBN. Metabolite profiling was performed using High-Performance Liquid Chromatography coupled with Quadrupole Time-of-Flight Mass Spectrometer (HPLC-QTOF/MS) technique and a total of 54 compounds belonging to different groups were detected and identified. These findings help to uncover the relation of therapeutic activity of EBN. The EBN was further extracted with AcOEt and BuOH. The AcOEt extract was fractionated into three fractions (F1 -F3 ), and the high triglyceride content in F2 was verified by gC-FID. The three groups of fatty acids discovered in EBN are 48.43 % of poly-unsaturated (PUFA), 25.35 % of saturated fatty acids (SFA) and 24.74 % of mono-unsaturated fat (MUFA). This is the first time to report results ofEBN, BuOH, and AcOEt extracts and of fraction F2 (TEBN) on their analysis for their antioxidant activities by DPPH, ABTS and catalase assay and for their paraoxonase and anti-tyrosinase activities. The results showed that TEBN exhibited the significant bioactivity in all assays. These findings suggest that TEBN is a good source for natural bioactive compounds in promoting body vigor. Current work widened the content of EBN especially on the triglyceride and also marked the content of specific location (Johor, Malaysia) of EBN origin.


Subject(s)
Amino Acids/analysis , Biological Products/analysis , Biological Products/chemistry , Birds , Fatty Acids/analysis , Food Analysis , Nesting Behavior , Proteins/analysis , Amino Acids/chemistry , Animals , Chromatography, High Pressure Liquid , Fatty Acids/chemistry , Malaysia , Nutritive Value , Proteins/chemistry
2.
Fitoterapia ; 112: 116-31, 2016 Jul.
Article in English | MEDLINE | ID: mdl-27259370

ABSTRACT

The last few decades have seen an alarming rise in fungal infections, which currently represent a global health threat. Despite extensive research towards the development of new antifungal agents, only a limited number of antifungal drugs are available in the market. The routinely used polyene agents and many azole antifungals are associated with some common side effects such as severe hepatotoxicity and nephrotoxicity. Also, antifungal resistance continues to grow and evolve and complicate patient management, despite the introduction of new antifungal agents. This suitation requires continuous attention. Cinnamaldehyde has been reported to inhibit bacteria, yeasts, and filamentous molds via the inhibition of ATPases, cell wall biosynthesis, and alteration of membrane structure and integrity. In this regard, several novel cinnamaldehyde derivatives were synthesized with the claim of potential antifungal activities. The present article describes antifungal properties of cinnamaldehyde and its derivatives against diverse classes of pathogenic fungi. This review will provide an overview of what is currently known about the primary mode of action of cinnamaldehyde. Synergistic approaches for boosting the effectiveness of cinnamaldehyde and its derivatives have been highlighted. Also, a keen analysis of the pharmacologically active systems derived from cinnamaldehyde has been discussed. Finally, efforts were made to outline the future perspectives of cinnamaldehyde-based antifungal agents. The purpose of this review is to provide an overview of current knowledge about the antifungal properties and antifungal mode of action of cinnamaldehyde and its derivatives and to identify research avenues that can facilitate implementation of cinnamaldehyde as a natural antifungal.


Subject(s)
Acrolein/analogs & derivatives , Antifungal Agents/pharmacology , Acrolein/chemistry , Acrolein/pharmacology , Animals , Antifungal Agents/chemistry , Drug Synergism , Fungi/drug effects , Humans , Molecular Structure , Yeasts/drug effects
3.
Eur J Med Chem ; 101: 534-51, 2015 Aug 28.
Article in English | MEDLINE | ID: mdl-26188909

ABSTRACT

Malaria has been teasing human populations from a long time. Presently, several classes of antimalarial drugs are available in market, but the issues of toxicity, lower efficacy and the resistance by malarial parasites have decreased their overall therapeutic indices. Thus, the search for new promising antimalarials continues, however, the battle against malaria is far from over. Ferroquine is a derivative of chloroquine with antimalarial properties. It is the most successful of the chloroquine derivatives. Not only ferroquine, but also its derivatives have shown promising potential as antimalarials of clinical interest. Presently, much research is dedicated to the development of ferroquine derivatives as safe alternatives to antimalarial chemotherapy. The present article describes the structural, chemical and biological features of ferroquine. Several classes of ferroquine derivatives including hydroxyferroquines, trioxaferroquines, chloroquine-bridged ferrocenophanes, thiosemicarbazone derivatives, ferrocene dual conjugates, 4-N-substituted derivatives, and others have been discussed. Besides, the mechanism of action of ferroquine has been discussed. A careful observation has been made into pharmacologically significant ferroquine derivatives with better or equal therapeutic effects to that of chloroquine and ferroquine. A brief discussion of the toxicities of ferroquine derivatives has been made. Finally, efforts have been made to discuss the current challenges and future perspectives of ferroquine-based antimalarial drug development.


Subject(s)
Aminoquinolines/pharmacology , Antimalarials/pharmacology , Ferrous Compounds/pharmacology , Malaria/drug therapy , Plasmodium/drug effects , Aminoquinolines/chemical synthesis , Aminoquinolines/chemistry , Animals , Antimalarials/chemical synthesis , Antimalarials/chemistry , Dose-Response Relationship, Drug , Ferrous Compounds/chemical synthesis , Ferrous Compounds/chemistry , Humans , Metallocenes , Molecular Structure , Parasitic Sensitivity Tests , Structure-Activity Relationship
4.
BMC Complement Altern Med ; 11: 94, 2011 Oct 12.
Article in English | MEDLINE | ID: mdl-21992551

ABSTRACT

BACKGROUND: There has been no effective treatment or agent that is available for corneal injury in promoting corneal wound healing. Previous studies on edible bird's nest extract (EBN) had reported the presence of hormone-like substance; avian epidermal growth factor that could stimulate cell division and enhance regeneration. This study aimed to investigate the effects of EBN on corneal keratocytes proliferative capacity and phenotypical changes. METHODS: Corneal keratocytes from six New Zealand White Rabbits were isolated and cultured until Passage 1. The proliferative effects of EBN on corneal keratocytes were determined by MTT assay in serum-containing medium (FDS) and serum-free medium (FD). Keratocytes phenotypical changes were morphologically assessed and gene expression of aldehyde dehydrogenase (ALDH), collagen type 1 and lumican were determined through RT-PCR. RESULTS: The highest cell proliferation was observed when both media were supplemented with 0.05% and 0.1% EBN. Cell proliferation was also consistently higher in FDS compared to FD. Both phase contrast micrographs and gene expression analysis confirmed the corneal keratocytes retained their phenotypes with the addition of EBN. CONCLUSIONS: These results suggested that low concentration of EBN could synergistically induce cell proliferation, especially in serum-containing medium. This could be a novel breakthrough as both cell proliferation and functional maintenance are important during corneal wound healing. The in vitro test is considered as a crucial first step for nutri-pharmaceutical formation of EBN-based eye drops before in vivo application.


Subject(s)
Biological Factors/pharmacology , Birds , Cornea/cytology , Corneal Diseases/drug therapy , Corneal Keratocytes/drug effects , Saliva/chemistry , Animals , Biological Factors/metabolism , Birds/metabolism , Cell Proliferation/drug effects , Cells, Cultured , Cornea/drug effects , Corneal Diseases/physiopathology , Corneal Injuries , Corneal Keratocytes/cytology , Humans , Medicine, Chinese Traditional , Rabbits , Saliva/metabolism
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