Study on the Anti-Inflammatory Activity and Mechanism of the Crude Extract and Natural Products Isolated from Fatsia polycarpa

Nurkholis (2012) Study on the Anti-Inflammatory Activity and Mechanism of the Crude Extract and Natural Products Isolated from Fatsia polycarpa. Magister thesis, Universitas Brawijaya.

Abstract

Peradangan kronis adalah penyebab utama berbagai penyakit ganas, termasuk kanker, diabetes, dan penyakit kardiovaskular. Dengan demikian, anti-peradangan dianggap sebagai strategi rapeutik potensial untuk penyakit-penyakit itu. Fatsia Polycarpa, endemik tanaman untuk Taiwan, digunakan sebagai obat herbal dalam mengobati beberapa penyakit yang berhubungan dengan peradangan. Namun, kembali bukan bukti ilmiah tentang fungsi biologisnya. Penelitian ini bertujuan untuk menyelidiki efek anti-inflamasi ekstrak minyak mentah F. Polycarpa, dan mengkarakterisasi konstituen ekstrak yang kemungkinan menstropsi ke bioaktivitasnya. Ditemukan bahwa ekstrak minyak mentah (MCE) daun dan ranting F. Polycarpa kaya akan triterpenoids dan phytosterol, di mana Brassicasterol adalah phytosterol utama dan 3α-hydroxyoleane-11-en-28,13β-olide (Hoeo) adalah salah satu triterpenpenoid utama. Oleh karena itu, efek anti-inflamasi MCE, Brassicasterol, dan Hoeo dikarakterisasi menggunakan tes berbasis sel dan tes hewan. Garis sel makrofag, RAW 264,7, diperlakukan dengan senyawa, dan distimulasi dengan lipopolysaccharide (LPS) untuk menginduksi reaksi inflamasi sel. Produksi mediator pro-inflamasi N yang diperiksa oleh reaksi berantai polimerase transkripsi transkripsi Barat atau semi kuantitatif. MCE dan Hoeo, tetapi bukan brassicasterol, ekspresi dosis yang terhambat dari nitrat oksida yang dapat diinduksi synthase dan cyclooloxygenase-2. Secara konsisten, MCE dan HOEO juga menekan produksi nitrat oksida, prostaglandin E 2, dan ekspresi sitokin pro-inflamasi IL-1β dan IL-6. Bulu Rendah, MCE dan Hoeo ditemukan menenca fosforilasi inhibitor Kappa B (i қ b), dan aktivasi inhibitor kappa b kinase (IKK), sinyal ekstraseluler yang diatur Kinase 1/2 (ERK 1/2) dan C-Jun N -terminal kinase (jnk). Tes hewan mengungkapkan bahwa MCE dapat secara efektif memperbaiki peradangan telinga yang diinduksi TPA pada tikus. Kesimpulannya, MCE dari F. Polycarpa menunjukkan aktivitas anti-inflamasi yang jelas di Vivo dan in vitro, dan mekanisme yang mendasari kemungkinan melibatkan penghambatan jalur IKK / NF-қ B jalur dan MAPK (ERK dan JNK). Ini menunjukkan bahwa F. Polycarpa adalah kandidat potensial untuk dikembangkan sebagai agen pemerutian untuk penyakit yang berhubungan dengan peradangan. Triterpenoids, seperti Hoeo, kemungkinan berkontribusi, setidaknya sebagian, untuk aktivitas anti-inflamasi F. Polycarpa. Dengan demikian, efek dari triterpenoid di MCE F. Polycarpa pantas menjadi bulu yang dieksplorasi.

English Abstract

Chronic inflammation is a primary cause of numerous malignant diseases, including cancer, diabetes, and cardiovascular diseases. Thus, anti-inflammation is considered as a potential rapeutic strategy for those diseases. Fatsia polycarpa, a plant endemic to Taiwan, is used as an herbal medicine in treating several inflammation-related diseases. However, re is no scientific evidence regarding to its biological function. This study aimed to investigate anti-inflammatory effect of crude extract of F. polycarpa, and characterize constituents of extract that likely constribute to its bioactivity. It was found that methanolic crude extract (MCE) of leaves and twigs of F. polycarpa was rich in triterpenoids and phytosterols, in which brassicasterol is a major phytosterol and 3α-hydroxyoleane-11-en-28,13β-olide (HOEO) is one of major triterpenoids. refore, anti-inflammatory effects of MCE, brassicasterol, and HOEO were characterized using cell-based assays and animal tests. A macrophage cell line, RAW 264.7, was treated with compounds, and stimulated with lipopolysaccharide (LPS) to induce inflammatory reactions of cell. production of pro-inflammatory mediators was n examined by Western blotting or semi quantitative reverse transcription polymerase chain reaction. MCE and HOEO, but not brassicasterol, dose-dependently inhibited expression of inducible nitric oxide synthase and cyclooxygenase-2. Consistently, MCE and HOEO also suppressed production of nitric oxide, prostaglandin E 2 , and expression of pro-inflammatory cytokines IL-1β and IL-6. Fur rmore, MCE and HOEO were found to attenuate phosphorylation of inhibitor kappa B (I қ B), and activation of inhibitor kappa B kinase (IKK), extracellular signal regulated kinase 1/2 (ERK 1/2) and c-Jun N-terminal kinase (JNK). Animal tests revealed that MCE could effectively ameliorate TPA-induced ear inflammation in mice. In conclusion, MCE of F. polycarpa exhibited an obvious anti-inflammatory activity in vivo and in vitro , and underlying mechanism likely involves inhibition of IKK/NF- қ B pathway and MAPK (ERK and JNK) pathway. This suggests that F. polycarpa is a potential candidate to be developed as a rapeutic agent for inflammation-related diseases. Triterpenoids, such as HOEO, likely contribute, at least in part, to anti-inflammatory activity of F. polycarpa . Thus, effects of o r triterpenoids in MCE of F. polycarpa deserve to be fur r explored.

Item Type: Thesis (Magister)
Identification Number: TES/615.84/NUR/s/041205997
Subjects: 600 Technology (Applied sciences) > 615 Pharmacology and therapeutics > 615.8 Specific therapies and kinds of therapies
Divisions: S2/S3 > Magister Teknologi Hasil Pertanian, Fakultas Teknologi Pertanian
Depositing User: Endro Setyobudi
Date Deposited: 17 Oct 2013 14:11
Last Modified: 17 Oct 2013 14:11
URI: http://repository.ub.ac.id/id/eprint/158189
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