Farmasi (S3)

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Browsing Farmasi (S3) by Subject "COX-2"

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    Anti-oral mucosal activity and mechanism of ethanol extract of Kaempferia galanga L. rhizome via inhibition of COX-2 expression
    (2022-04-14) INDAH SUASANI WAHYUNI; Jutti Levita; Irna Sufiawati
    Oral health is an integral part of overall body health. Therefore, oral mucosal inflammation can have an impact on the body`s health. Oral mucosal inflammation can be managed by administering anti-inflammatory drugs, both steroids and non-steroidal, but sometimes cause side effects, especially if used in the long term and in large doses. Research on medicinal plants for alternatives has recently been carried out. One of the plants in Indonesia that is known to have an anti-inflammatory effect is Kaempferia galanga L. The rhizome part of this plant contains a lot of secondary metabolites and this has not been widely explored in plants harvested in the rainy season and dry season, according to Indonesia`s geographical conditions. The difference in harvest time between these two seasons will affect the content of secondary metabolites. One of the anti-inflammatory mechanisms that can be investigated for drug development is through the cyclooxygenase (COX) enzyme inhibition pathway, particularly COX-2. Thus, this study aimed to explore the potential of the Kaempferia galanga L. as an anti-oral mucosal ulcer, which is often used in traditional medicine, has anti-inflammatory effects, and is known to have low toxicity. The research methods used were phytochemical screening/color test method, spectrophotometric analysis, and chromatogram profiles analysis: Thin Layer Chromatography (TLC) and Reversed-Phase High-Performance Liquid Chromatography (RP-HPLC), for identification of secondary metabolites in the ethanolic extract of K. galanga L. (EEKG). Ethyl p-methoxycinnamate (EPMC) levels in the EEKG from plants harvested in the rainy season (EEKG-R) and that of harvested in the dry season (EEKG-D) were determined using validated RP-HPLC method. The in vitro studies were carried out to obtain the IC50 value of the EEKG in inhibiting prostaglandins production catalyzed by COX-2, as well as in vivo studies on acetic acid 70%-induced oral mucosal ulcers in Wistar rats. The effect of EEKG topical application was measured macroscopically, histopathologically, and using the western blot method. The results showed that the secondary metabolites contained in the EEKG were Polyphenols, Flavonoids, Alkaloids, Tannins, Terpenoids, and Saponins; EPMC and flavonoids detected in the EEKG using TLC and spectrophotometric analysis, meanwhile, only EPMC was detected in the EEKG using RP-HPLC. The EPMC level of the EEKG-R was 10 times greater (0.01%) than that of EEKG-D (0.001%). The relative IC50 of EEKG was 39.85 ppm (r = 1) and the IC50 of EEKG was 58.88 ppm (r2 = 0.97/r = 0.99). This in vitro study also revealed that low-dose EEKG (15.625 ppm and 31.25 ppm) showed a statistically significant (p<0.05) effect in inhibiting PGG2 production catalyzed by COX-2. The in vivo study showed that topical application of EEKG 0.5%, macroscopically, achieved the percent recovery of ulcer area (85.24%) more than the negative control (79.82%) and also showed a better percent recovery of inflammation sign scores (76.67%) than the negative control (71.67%). Thus, EEKG doses of 0.5% to 2% reduced the histopathology score, even, the EEKG 1% (p = 0.0348) and 2% (p = 0.0462) reduced the histopathology score significantly compared to the negative control. In vivo study using the Western blot, method revealed that EEKG doses of 0.5% to 2% were able to reduce the expression of COX-2. In conclusion, lower doses of EEKG have exhibited anti-inflammatory activity by inhibiting COX-2 expression, therefore, the rhizome of Kaempferia galanga is prospective to be developed as an alternative topical drug for oral mucosal ulceration.