The prevalence of dyslipidemia in Indonesia continues to increase. Free radicals are increasing the occurrence of diseases, one of them is dyslipidemia. Previous studies showed that antioxidant compounds have strong potential as dyslipidemia drug. The mechanism action of dyslipidemia treatment is inhibiting cholesterol synthesis through the HMG CoA reductase and cholesterol absorption mediated with lipase. This study aimed to analyze the antioxidant activity along with the inhibition of HMG CoA reductase and lipase in a combination of ethanolic extract of Anredera cordifolia leaf (EB) with ethanolic extract of Curcuma xanthorrhiza rhizome (ET) and its single form. The antioxidant activity test was conducted using DPPH method by making serial dilution of samples and ascorbic acid with adding DPPH and methanol as standard. The inhibitory activity of HMG CoA and lipase was conducted by making a series concentration of sample as well as simvastatin as the comparison. The results showed that the highest antioxidant activity is in ET samples IC50 16.21 ± 1.74 µg/mL, but was less potential compared to ascorbic acid IC50 7,63±0,85 µg/mL. The most potential inhibition of HMG CoA and lipase is in ET samples IC50 8.35 ± 0.02 and 22.35 ± 1.26 µg/mL. The combination of ET-EB (1: 1) is better than EB but lower than ET in antioxidant activity as well as the inhibition of HMG CoA reductase and lipase. The result showed a correlation that the higher antioxidant activity, the higher inhibitory of HMG CoA reductase and lipase respectively.
Gambir (Uncaria gambir Roxb.) is a member of family of Rubiaceae. In Asia including Indonesia, extracts of gambir are empirically used daily to weed out. The high content of catechin flavonoids in gambir has a pharmacological effect in the treatment of hyperlipidemia that potential to be developed into traditional medicine. This literature review aimed to examine the potency of pharmacological effect of gambir as hyperlipidemia treatment therapy based on the results of studies in silico, in vitro, in vivo pharmacological effects and its safety to provide evidence of scientific information to the community. The literatures used for analysis in this study including evidence-based articles on both pharmacology and safety which are available in Pubmed and Google Scholar. The results showed a very strong potency of gambir plants in the treatment of hyperlipidemia with catechin as bioactive compounds. In silico study revealed mechanism action of catechin as antihyperlipidemic using 2 pathways, inhibition of the enzyme HMG-CoA reductase and increase the LDL receptors. In vitro studies of catechin are able to inhibit lipid absorption in the intestine through inhibition of pancreatic lipase activity, lipid hydrolysis and emulsification, micelle cholesterol deposition. Pre-clinical tests on animals showed that the ethyl acetate fraction of gambir leaves was able to reduce the levels of total cholesterol, triglycerides, LDL and increase blood plasma HDL. The long-term use of gambir leaves has been proven to be safe, not mutagenic, no hematological, clinical biochemical abnormalities and no abnormalities in the vital organs of the animal models. Abstrak Gambir (Uncaria gambir Roxb) adalah tumbuhan perdu dari suku Rubiaceae. Di Asia termasuk Indonesia, secara empiris ekstrak gambir digunakan sehari-hari untuk menyirih. Kandungan flavonoid katekin yang tinggi dalam gambir memiliki efek farmakologi dalam pengobatan hiperlipidemia yang berpotensi untuk dikembangkan menjadi obat tradisional. Kajian literatur ini bertujuan untuk mengkaji potensi farmakologi gambir sebagai terapi pengobatan hiperlipidemia berdasarkan hasil studi efek farmakologi in silico, in vitro, in vivo efek farmakologi dan keamanannya, sehingga memberikan bukti informasi ilmiah kepada masyakarat. Literatur yang digunakan dalam proses review meliputi literatur dengan berbasis bukti baik farmakologi maupun keamanan yang tersedia di Pubmed dan Google Scholar. Hasil kajian menunjukkan potensi yang sangat kuat dari tanaman gambir dalam pengobatan hiperlipidemia dengan katekin sebagai senyawa bioaktif utama. Studi in silico menunjukkan mekanisme aksi katekinsebagai antihiperlipidemia menggunakan dua jalur yaitu penghambatan enzim HMG-CoA reduktase dan peningkatan reseptor LDL. Studi in vitro katekin mampu menghambat penyerapan lipid di usus melalui penghambatan aktivitas lipase pankreas, hidrolisis lipid dan emulsifikasi, serta pengendapan kolesterol misel. Studi in vivo menunjukkan fraksi etil asetat daun gambir mampu menurunkan kadar kolesterol total, trigliserida, LDL dan meningkatkan HDL plasma darah. Penggunaan daun gambir dalam jangka panjang terbukti aman, tidak mutagen, tidak ditemukan kelainan hematologi, biokimia klinis dan tidak menyebabkan kelainan organ vital hewan uji.
Abstract Uncaria gambir Roxb., one of native plants of Indonesia contains high levels of catechins. Catechins are very potential to be used for medicinal raw materials because theirs effects are proven to be antibacterial, antiviral, and antidyslipidemic. Derivatization of catechin can be developed to produce drug compounds that are effective as antiviral agents for HIV. Derivatization process needs pure catechin isolate as a starting material in order to obtain maximum result so that the isolation process is one of the important stages. In this study, isolation and purification of catechin isolate from Uncaria gambir Roxb. extract was carried out, which will then be the starting material in the derivatization of catechin. Gambir extract used for catechin isolation was a quality 1 gambir extract obtained from Padang, West Sumatra. Gambier extract is characterized according to the standard method stated in Farmakope Herbal Indonesia. Isolation of catechin from gambir extract was done by percolation method using ethyl acetate solvents. Pure catechin isolate was obtained using a vacuum liquid chromatograpy method with a series of solvent hexane and ethyl acetate gradients. Catechin purification was monitored using Thin Layer Chromatography (TLC) method with eluent chloroform:ethyl acetate:formic acid (5:4:1, then identified using High Performance Liquid Chromatography (HPLC), Nuclear Magnetic Resonance (NMR) Spectroscopy, and Liquid Cromatography- Mass Spectroscopy (LC-MS). The purity of catechin isolate obtained was 99.80%± 0.132. Abstrak Uncaria gambir Roxb., salah satu tanaman asli Indonesia yang mengandung katekin dengan kadar yang tinggi. Katekin sangat potensial digunakan untuk bahan baku obat karena efeknya terbukti sebagai antibakteri, antivirus, dan antidislipidemia. Derivatisasi katekin dapat dikembangkan untuk menghasilkan senyawa obat yang efektif sebagai antivirus untuk HIV. Untuk derivatisasi ini diperlukan isolat katekin murni sebagai starting material agar diperoleh hasil yang maksimal sehingga proses purifikasi isolat merupakan salah satu tahap yang penting. Dalam penelitian ini dilakukan isolasi dan pemurnian isolat katekin dari ekstrak Uncaria gambir Roxb. yang selanjutnya akan menjadi bahan awal dalam derivatisasi katekin. Ekstrak gambir yang digunakan untuk isolasi katekin adalah ekstrak gambir kualitas 1 yang diperoleh dari Padang, Sumatera Barat. Ekstrak gambir dikarakterisasi sesuai dengan metode standar yang tertera dalam Farmakope Herbal Indonesia. Isolasi katekin dari ekstrak gambir dilakukan dengan metode perkolasi menggunakan pelarut etil asetat. Isolat katekin murni diperoleh menggunakan metode kromatografi cair vakum (KCV) dengan serangkaian gradien pelarut heksana dan etil asetat. Pemurnian katekin dimonitor menggunakan metode kromatografi lapis tipis (KLT) dengan eluen kloroform : etil asetat : asam format (5:4:1), kemudian diidentifikasi menggunakan High Performance Liquid Chromatography (HPLC), spektroskopi Nuclear Magnetic Resonance (NMR), dan Liquid Cromatography-Mass Spectroscopy (LC- MS). Kemurnian isolat katekin yang didapatkan 99,80%± 0,132.
Inflammatory is a body defense mechanism due to respond of tissue on undermine influences, either local or the one that go into the body. Inflammatory can cause various physical dysfunctions. Uncaria gambir Roxb, a high catechin content in ethyl acetate fraction, is widely used as wound healing in Indonesian culture, therefore its mechanism of anti-inflammatory action is still unknown. The objective of our study is to investigated the activity of anti-inflammatory ethyl acetate fraction of Uncaria gambir leaves inhibition of edema, COX-2 and iNOS expression using induction method with carrageenan in rats. This study is experimental research which use 25 white Wistar strain rats as animals assay that divided into 5 groups: negative group (water), positive group (sodium diclofenac 50 mg/kg bw), dose I (5 mg/kg bw fraction), II (10 mg/kg bw fraction) and III (20 mg/kg bw fraction) groups. Each of them were given orally 30 min before carrageenan 3% induced. The paw volume was measured every day for seven day after injection carrageenan using plethysmometer. Inhibition COX-2 and iNOS expression were determined by enzyme-linked immunosorbent assay. The results showed that ethyl acetate fraction of Uncaria gambir leaves in all doses had anti-inflammatory effect on white rats through the mechanism of inflammatory inhibition by reducing edema volume. All three fraction doses can also reduce COX-2 and iNOS expression. The fraction had the highest anti-inflammatory potency by the dose of 20 mg/kg body weight. The conclusion that ethyl acetate of three doses had anti-inflammatory activities through a mechanism of edema volume reduction, COX-2 and iNOS expression.
ABSTRAK Daun Sirsak (Annona muricata Linn), Annonaceae telah diketahui memiliki kemampuan meredam radikal bebas yang kuat dan bisa dikembangkan menjadi sediaan farmasi antioksidan. Pembentukan nanopartikel dari ekstrak akan meningkatkan stabilitas, kemampuan mukoadhesif dan penetrasi ekstrak sehingga dapat meningkatkan efektifitasnya. Pembuatan nanopartikel dilakukan dengan melarutkan kitosan dalam larutan asam asetat glasial 1%, dan dicampurkan dengan infus daun sirsak. Suspensi nanopartikel ekstrak daun sirsak dikeringkan dengan menggunakan alat pengering semprot. Hasil evaluasi nanopartikel ekstrak diperoleh ukuran partikel 131,23 ± 1,81%, indeks polidispersitas 0,3-0,4; padatan total 0,47 %, warna coklat muda, bau khas ekstrak, rasa pahit, sifat serbuk halus, higroskopis, kadar air 6.86 ± 0,88%. Pemeriksaan aktivitas antioksidan pada nanopartikel ekstrak daun sirsak dengan menggunakan metode peredaman radikal bebas DPPH menunjukkan aktivitas antioksidan kuat dengan nilai 1C50 sebesar 80,98 bpj. Kata kunci : daun sirsak, Annona muricata Linn., DPPH, antioksidan, nanopartikel, kitosan PENDAHULUAN Berbagai penyakit degeneratif seperti diabetes, kanker, inflamasi jaringan, kelainan imunitas, infark jantung dan penuaan dini disebabkan tingginya kadar radikal bebas dalam tubuh. Radikal bebas yang merusak tubuh ini dapat dinetralisir oleh senyawa antioksidan. Antioksidan merupakan senyawa yang dapat menghambat oksigen reaktif dan radikal bebas dalam tubuh. Senyawa antioksidan ini akan menyerahkan satu atau lebih elektron kepada radikal bebas sehingga menjadi bentuk molekul yang normal kembali dan menghentikan berbagai kerusakan yang ditimbulkan. Dalam studi laboratorium, kehadiran antioksidan eksogen telah terbukti untuk mencegah kerusakan radikal bebas yang telah dikaitkan dengan perkembangan kanker. Tujuan pembuatan nanopartikel adalah sebagai pembawa (carrrier) agar zat berkhasiat dari ekstrak masuk ke dalam sistem peredaran darah tanpa kehilangan material aktif selama proses penghantaran untuk selanjutnya dibawa oleh darah menuju target pengobatan. Nanopartikel mempunyai ukuran di bawah 1 mikrometer sehingga dikenal dapat masuk kedalam sel dan memberikan aktivitas dan menunjukkan reprodisibilitas terapi yang baik. Selain itu, permukaan nanopartikel dapat dimodifikasi untuk sistem penargetan terhadap sel dan organ tertentu sehingga dapat menurunkan dosis dan toksisitasnya. Nanopartikel dpat tinggal di saluran cerna dalam waktu yang cukup lama sehingga dapat meningkatkan
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