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Judul Dual anti-inflammatory activities of COX-2/5-LOX driven by kratom alkaloid extracts in lipopolysaccharide-induced RAW 264.7 cells / Siti Irma Rahmawati
Pengarang Siti Irma Rahmawati
Mutia Hardhiyuna
Dwi Wahyu Indriani
Febby Nurdiya Ningsih
A’liyatur Rosyidah
Firdayani Firdayani
Peni Ahmadi
Masteria Yunovilsa Putra
EDISI Scientific Reports, 2024, ? 1
Penerbitan Jawa Barat,Indonesia : National Research and Innovation Agency (BRIN), 2024
Deskripsi Fisik 13 :ill
Subjek MITRAGYNA SPECIOSA
CELLULAR OXIDATIVE STRESS
DUAL INHIBITION COX-2/5-LOX
ANTI-INFLAMMATORY
Abstrak Cyclooxygenase (COX) and lipoxygenase (LOX) enzymes play a pivotal role in producing proinflammatory eicosanoids, including prostaglandins (PGs) and Leukotrienes (LTs), in the inflammation process. Mitragynine is a primary alkaloid contained in the kratom’s leaves and has been reported to show anti-inflammatory activity by suppressing COX-2 mRNA translation to lowering PGs synthesis. In this study, the Kratom’s alkaloid extract Containing ~46% mitragynine was found to exhibit dual inhibition activity towards COX-2/5-LOX enzymes at concentrations below 25 ppm in the LPS-induced RAW 264.7 macrophage cells. At these levels, no cell toxicity was observed while the cells became death (e.g., 10–46% viability at 50–100 ppm) and only COX-2 inhibition activity was observed after exposed with more than 25 ppm of alkaloid extract. In contrast, the methanolic-crude extract of Kratom’s leaf Containing ~ 5% mitragynine showed no inhibition toward COX-2/5-LOX enzymes and did not toxic onto the cells, even after treated at 1
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Lokasi Akses Online DOI: 10.1038/s41598-024-79229-x

 
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245 1 # $a Dual anti-inflammatory activities of COX-2/5-LOX driven by kratom alkaloid extracts in lipopolysaccharide-induced RAW 264.7 cells /$c Siti Irma Rahmawati
250 # # $a Scientific Reports, 2024, ? 1
260 # # $a Jawa Barat,Indonesia :$b National Research and Innovation Agency (BRIN),$c 2024
300 # # $a 13 : $b ill
520 # # $a Cyclooxygenase (COX) and lipoxygenase (LOX) enzymes play a pivotal role in producing proinflammatory eicosanoids, including prostaglandins (PGs) and Leukotrienes (LTs), in the inflammation process. Mitragynine is a primary alkaloid contained in the kratom’s leaves and has been reported to show anti-inflammatory activity by suppressing COX-2 mRNA translation to lowering PGs synthesis. In this study, the Kratom’s alkaloid extract Containing ~46% mitragynine was found to exhibit dual inhibition activity towards COX-2/5-LOX enzymes at concentrations below 25 ppm in the LPS-induced RAW 264.7 macrophage cells. At these levels, no cell toxicity was observed while the cells became death (e.g., 10–46% viability at 50–100 ppm) and only COX-2 inhibition activity was observed after exposed with more than 25 ppm of alkaloid extract. In contrast, the methanolic-crude extract of Kratom’s leaf Containing ~ 5% mitragynine showed no inhibition toward COX-2/5-LOX enzymes and did not toxic onto the cells, even after treated at 100 ppm. The alkaloid extract suppressed Several antiinflammation parameters, including ROS (64% reduction at 25 ppm), NO (30% reduction at 25 ppm), TNF-? (~ 50% reduction at 25 ppm), and IL-6 production (60% reduction at 6.25 ppm). In silico molecular studies indicated strong binding affinity of Kratom alkaloids to COX-2 and 5-LOX active sites, supporting the Kratom’s alkaloids to have great potential dual inhibition activity towards COX2/5-LOX enzymes and to be developed as a safer NSAIDs with fewer side effects.
650 # 4 $a ANTI-INFLAMMATORY
650 # 4 $a CELLULAR OXIDATIVE STRESS
650 # 4 $a DUAL INHIBITION COX-2/5-LOX
650 # 4 $a MITRAGYNA SPECIOSA
700 0 # $a A’liyatur Rosyidah
700 0 # $a Dwi Wahyu Indriani
700 0 # $a Febby Nurdiya Ningsih
700 0 # $a Firdayani Firdayani
700 0 # $a Masteria Yunovilsa Putra
700 0 # $a Mutia Hardhiyuna
700 0 # $a Peni Ahmadi
856 # # $a DOI: 10.1038/s41598-024-79229-x
990 # # $a ARTVET2512
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