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"Naftokuinon dan turunannya dilaporkan mempunyai aktivitas multipotensi. Hasil skrining aktivitas sitotoksik 5 senyawa turunan naftokuinon terhadap sel kanker payudara MCF7 dan sel kanker hati HEPG2, menunjukkan bahwa senyawa 1,4 naftokuinon (N) dan senyawa 2-hidroksi-1,4-naftokuinon(2HN) mempunyai aktivitas sitotoksik yang kuat. Sebagai upaya optimisasi aktivitas sitotoksik selektif terhadap kedua senyawa tersebut dilakukan rancangan modifikasi strukturnya sehingga diperoleh 30 senyawa turunan. Senyawa turunan tersebut selanjutnya dilakukan skrining secara virtual terhadap reseptor target Polo like kinase 1 (Plk-1) dengan perangkat lunak Molegro Virtual Docker. PLk-1 adalah target potensial generasi terbaru dalam terapi kanker, proteinnya terekspresikan secra bermakna dalam beberapa jenis kanker. Hasil skrining virtual menunjukan bahwa senyawa hasil rancangan mempunyai afinitas pengikatan lebih tinggi dibandingkan senyawa induk, ligan acuan benzolaktam serta doxorubicin. Senyawa yang mempunyai nilai afinitas lebih baik dari senyawa induk dan nilai clogp<5 disintesis. Hasil modifikasi senyawa N diperoleh 3 senyawa yaitu senyawa 4-oksim-naftalen-1-on (NO-1); senyawa 4-((benzoiloksi)imino)naftalen-1(4h)-on (NO-2) dan senyawa (E)-4-(asetoxiimino) naftalen-1(4H)-on (NO-6). Sedangkan modifikasi senyawa 2HN diperoleh 4 senyawa yaitu 1,4-diokso-1,4-dihidronaftalen-2il-benzoat (2HN-13), 1,4-diokso-1,4-dihidronaftalen-2-il 4- metilbenzoat (2HN-14); 1,4-diokso-1,4-dihidronaftalen-2il-3-metilbenzoat (2HN-15), dan 1,4-diokso1,4-dihidro-naftalen-2-il 2-metilbenzoat (2HN-16). Struktur senyawa hasil modifikasi dikonfirmasi dengan FTIR, LCMS, 1H-NMR dan 13C-NMR serta aktivitas sitotoksik selektif terhadap sel kanker payudara MCF7, sel kanker hati HEPG2 dan sel normal CHO menggunakan metode MTT. Senyawa yang paling poten dilakukan analisis siklus sel dengan flowcytometry. Hasil penelitian menunjukkan senyawa N, NO-1, NO-2 dan NO-6 mampu menginhibisi proliferasi sel kanker payudara MCF7 dengan masing-masing nilai IC50 20,63 μM, 11,23; 48,18 μM.μM dan 3,24 μM. Senyawa NO-1 dan NO-6 mempunyai aktivitas sitotoksik selektif terhadap sel kanker MCF7 dan tidak selektif sitotoksik terhadap sel kanker hati HepG2. Mekanisme penghambatan proliferasi sel kanker MCF7 oleh senyawa NO-1 dan NO-2 diduga kuat melalui penghambatan plk-1 yang selanjutnya menginduksi apoptosis dan menekan mitosis sel. Hasil analisa HKSA menunjukkan bahwa efek hidrofobik khususnya log p senyawa turunan 1,4 naftokuinon menunjang aktivitas sitotoksik terhadap sel kanker payudara MCF7, namun tidak demikian terhadap sel kanker hati HEPG2. Sedangkan efek sterik dan elektronik tidak memberikan pengaruh yang signifikan.

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Naphthoquinone and its derivatives have been reported to have multipotent activity. Results from cytotoxic screening against breast carcinoma cell line (MCF7) and hepatocarcinoma cell line (HepG2) showed that 1.4-naphthoquinone and 2-hydroxy-1.4-naphthoquinone compounds had the highest cytotoxic activity. In this study, the selective cytotoxic activity was optimized, 30-naphthoquinone derivatives from 1,4-naphthoquinone and 2-hydroxy-1,4-naphthoquinone were designed and virtually screened using Molegro Virtual Docker software. Those compounds were adhered to targeted receptor, which is Polo-like kinase 1 (Plk-1). Plk 1 is one of the potential targets for cancer therapy because it is expressed on several types of cancer cells. Result of the study demonstrated that naphthoquinone derivatives had more potent bonding activity compared to ligand references, i.e. benzolactam and doxorubicin. Modification of 1.4-naftokuinon to oxyme structure had been performed and resulted in NO-1 (4-oxime-naphtalene-1-on), NO-6 ((E)-4-(acetoxyimino) naphtalen-1(4H)-on) and NO-2 (4-((benzoyloxy)imino)naftalen-1(4h)-on). Furthermore, 2-hydroxy-1,4-naphtho- quinone had been modified and the synthesized compounds were 1,4-dioxo-1,4-dihydronaphtalen-2yl-benzoate (2HN-13), 1,4-dioxo-1,4-dihydronaphthalen-2-yl 4-methylbenzoate (2HN-14) 1,4-dioxo-1,4-dihydronaphtalen-2yl-3-metilbenzoate (2HN-15), and 1,4-dioxo-1,4-dihydronaphthalen-2-yl 2-methylbenzoate (2HN-16). Modified compounds had been confirmed using FTIR, LCMS, 1H-NMR and 13C-NMR. MTT assay was performed to study the selective cytotoxic activity. Flow cytometry was also being used to observe the cell cycles of cell after treated with the potent compounds. In this present study, it was observed that the compound N, NO-1, NO 2 and NO-6 inhibited the proliferation of MCF7 breast carcinoma cell line with IC50 20.63 μM, 11.23.μM, 48.18 μM and 3.24 μM respectively. NO-1 and NO-6 had selective cytotoxic activity against breast carcinoma cell line, MCF7 and had no selective cytotoxic activity against hepatocarcinoma cell line, HepG2. Mechanism of proliferation inhibited breast carcinoma cell line (MCF7) of NO-1 and NO-6 compounds were estimated by Plk-1 inhibition which further induced apoptotic and suppressed mitotic. QSAR analysis presented the hydrophobic effect of oxyme derivatives, particularly log p, played a role to breast carcinoma cell line (MCF7) on cytotoxic effect, but not to hepatocarcinoma cell line (HEPG2). However, the steric and electronic effects did not significantly contribute to the activity."

"Turunan naftokuinon dilaporkan memiliki berbagai aktivitas farmakologis yang baik seperti antioksidan, antibakteri, antikanker dan antiinflamasi. Pada penelitian ini senyawa turunan naftokuinon telah berhasil disintesis melalui metode multikomponen melalui reaksi Mannich dengan bantuan nanokatalis . Nanokatalis telah berhasil disintesis dengan metode menggunakan ekstrak daun murbei. Senyawa metabolit sekunder yang terkandung dalam daun murbei seperti alkaloid berperan sebagai agen penghidrolisis (sumber basa lemah) dan saponin sebagai agen penstabil untuk mencegah aglomerasi. Katalis dikarakterisasi dengan spektroskopi FT-IR, XRD, PSA, SEM-EDX, TEM dan VSM. Hasil XRD menunjukkan bahwa nanopartikel memiliki struktur spinel. Nanopartikel memiliki bentuk dengan ukuran rata-rata 33,63 nm. Sifat magnetik dari nanopartikel ditinjau dari nilai koersivitas (Hc), remanensi (Mr), dan magnetisasi saturasi (Ms) yaitu masing-masing sebesar 175,44 Oe; 1,63 emu/g dan 14,10 emu/g. Senyawa turunan naftokuinon dilakukan pada kondisi optimum yaitu menggunakan pelarut etanol:air (1:1) selama 8 jam pada suhu ruang dengan jumlah katalis 10% mol. Senyawa tersebut disintesis dengan mereaksikan lawson, benzaldehida dan variasi amina aromatik (anilin, 4-kloroanilin dan 4-nitroanilin). Senyawa yang telah terbentuk dikonfirmasi dengan uji titik leleh, kromatografi lapis tipis, spektroskopi FT-IR, spektrofotometer UV-Vis dan GC-MS. Senyawa 1 (2-hidroksi-3-(fenil(fenilamino)metil)naftalena-1,4-dion) berhasil disintesis dengan massa produk campuran sebesar 0,3127 gram dengan kemurnian sebesar 6,78%. Senyawa 2 (2-(((4-klorofenil)amino)(fenil)metil)-3-hidroksinaftalen-1,4-dion) dan senyawa 3 (2-hidroksi-3-(((4-nitrofenil)amino)(fenil)metil)naftalen-1,4-dion) belum berhasil terbentuk dengan massa campuran masing-masing sebesar 0,3014 gram dan 0,2599 gram. Aktivitas farmakologis antioksidan diuji dengan menggunakan metode DPPH. Uji aktivitas antioksidan senyawa 1, 2 dan 3 memiliki IC masing-masing yaitu 5,95; 7,21 dan 14,41 ppm. Naphthoquinone derivatives reported have a variety of good pharmacological activities such as antioxidants, antibacterial, anticancer and anti-inflammatory. In this research, the naphthoquinone derivatives have been successfully synthesized through Mannich reaction using nanocatalyst. nanocatalyst has been successfully synthesized by green synthesis method using mulberry leaf extract. Secondary metabolite compounds contained in mulberry leaves such as alkaloids as hydrolyzing agents (weak base sources) and saponins as stabilizing agents to prevent agglomeration. The catalyst was characterized by FT-IR spectroscopy, XRD, PSA, SEM-EDX, TEM and VSM nanoparticles have a spherical shape with an average size of 33.63 nm. The magnetic properties of CuFe nanoparticles such as coercivity (Hc), remanence (Mr), and saturation magnetization (Ms) values were respectively 175.44 Oe; 1.63 emu/g and 14.10 emu/g. Naphthoquinone derivative was carried out under optimal conditions using ethanol : water (1:1) solvent for 8 hours at room temperature with a catalyst amount of 10% mol. The compound was synthesized by reacting lawsone, benzaldehyde and aromatic amine variations (aniline, 4-chloroaniline and 4-nitroaniline). The compounds were confirmed by melting point test, thin layer chromatography, FT-IR spectroscopy, UV-Vis spectrophotometer and GC-MS. Compound 1 (2-hydroxy-3-(phenyl(phenylamino)methyl)naphthalene-1,4-dione) was successfully synthesized with mixed mass 0.3127 gram and purity 6.78%, compound 2 (2-(((4-chlorophenyl)amino)(phenyl)methyl)-3-hydroxynaphthalene-1,4-dione) and compound 3 (2-hydroxy-3-(((4-nitrophenyl)amino)(phenyl)methyl)naphthalene-1,4-dione) have not been successfully formed with mixed mass 0.3014 gram and 0.2599 gram, respectively. In naphthoquinone derivatives, the results of synthesis were tested by antioxidant activity using DPPH method. The antioxidant activity test of compound 1, 2 and 3 have IC 5.95; 7.21 and 14.41 ppm, respectively."

"Bawang dayak mengandung naphtoquinon sedangkan herba ceplukan mengandung quersetin dan physalin yang memiliki efek antihipertensi. Penelitian ini bertujuan untuk menguji efektivitas antihipertensi kombinasi ekstrak bawang dayak dan herba ceplukan. Deksametason 0,02mg dan larutan NaCl 2,5% digunakan sebagai penginduksi hipertensi. Kelompok normal: akuades, kontrol negatif: CMC-Na 1%, kontrol positif: kaptopril 0,45mg, ekstrak bawang dayak 121,5mg, ekstrak herba ceplukan 232,5mg, dosis kombinasi 1 (BD 40.5mg + HC 77,5mg), dosis kombinasi 2 (BD 81mg + HC 155mg), dan  dosis kombinasi 3 (BD 121,5 mg + HC 232,5mg). Tekanan darah dan berat badan diukur setiap minggu selama 49 hari. Hasil uji antihipertensi menunjukan bahwa, dosis kombinasi 1, 2, dan 3 efektif menurunkan hipertensi dengan p<0,05 dibandingkan dengan tekanan darah pada hari 28. Dosis kombinasi 1 menurunkan tekanan sistolik 32 mmHg (27%), diastolik 29 mmHg (37%), dan MAP 30 mmHg (33%). Dosis kombinasi 1 sudah  cukup untuk menurunkan tekanan darah, kadar angiotensin 2, malondialdehid, VEGF, dan kaveolin-1 dalam plasma serta mengurangi penebalan dinding aorta. 

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Dayak onions contain naphtoquinone while herba ceplukan  contain quercetin and physalin which have antihypertensive effects. This study aimed to test the antihypertensive effectiveness of a combination of dayak onion extract and herba ceplukan. Dexamethasone 0.02mg and 2.5% NaCl solution are used as inducers of hypertension. Normal group: aquades, negative control: CMC-Na 1%, positive control: captopril 0.45mg, dayak onion extract 121.5 mg, herba ceplukan  extract 232.5 mg, combination dose 1 (BD 40.5mg + HC 77.5mg), combination dose 2 (BD 81 mg + HC 155 mg), and combination dose 3 (BD 121.5 mg + HC 232.5mg). Blood pressure and weight were measured weekly for 49 days. The results of the antihypertensive test showed that the combined dose of 1, 2, and 3 was effective in reducing hypertension by p<0.05 compared to blood pressure on day 28. The combination dose 1 lowered systolic pressure by 32 mmHg (27%), diastolic by 29 mmHg (37%), and MAP by 30 mmHg (33%). A combination dose of 1 is sufficient to lower blood pressure, levels of angiotensin 2, malondialdehyde, VEGF, and kaveolin-1 in plasma and reduce thickening of the aortic wall. "