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"ABSTRACT

Malaria is one of problematic infectious diseases worldwide. The absence of an effective vaccine and the spread of drug resistant strains of Plasmodium clearly indicate the necessity for the deveploment of new chemotherapeutic agents. Recent method being developed is searching a new drug of antimalarial using in silica screening, or also know as virtual screening. One of enzyme target that important for growth of the malaria parasite is P/asmodium /a/ciparum Enoyl' Acyl Canier Protein Reductase (PfENR). Inhibition of this enzyme cause the fatty acid biosynthesis type ll will be tem1inated. In this research, in silica screening was performed using GOLD softwa,<;_ to find inhibitor candidates of PfENR by using I igands from the natural compound database of Medicinal Plants in Indonesia. On the GOLD software moleculer docking experiments were perfom1ed between ligands and macromolecule target PfENR. This target that has been optimized with residue removal and charges addition. Ligand is expected to be the PfENR inhibitors. Based on the results obtained from the in silico screening there were S inhibitor candidates which expected to be developed as an antimalarials. These compounds \\"ere Kacmpferol 3-rhamnosyl-(1-3)-rhamnosyl- (1-6)­glucoside, Cyanidin 3.5-di-(6-1mlonylglucoside), 8-Hydroxyapigenin 8-(2",4"­disulfatoglucuronidc). Epigallocmechin 3.5.-di-O-gallate, a··;d Querceti.r1 3.4'-dimethyl ether 7-alpha-L- Arabinofuranosyl-(1-6)-glucoside with the GoldScore ranged from 80,63 to I 00,4 I."

"Nigella sativa L. dilaporkan memiliki berbagai efek farmakologis termasuk sebagai anti parasit. Pengujian efek antimalaria dari ekstrak air biji N. sativasecara invivo terhadap mencit (Mus musculus) yang diinfeksi parasit malaria Plasmodium berghei NK65 telah dilakukan. Metode yang digunakan adalah pengujian mikroskopik dengan pewarnaan Giemsa terhadap sampel darah hewan uji. Penentuan kadar NO dengan metoda spektrofotometri dilakukan untuk mengetahui efek ekstrak air biji N. sativa terhadap kadar NO mencit yang terinfeksi parasit malaria P. berghei NK65. Ekstrak air biji N. sativadiberikan kepada mencit yang terinfeksi parasit malaria dalam periode 20 hari untuk mengetahui efek pemberian ekstrak air tersebut terhadap kelangsungan hidup (survival life) mencit. Hasil penelitian menunjukkan bahwa ekstrak air biji N. sativa dapat menurunkan jumlah parasit malaria P. berghei NK65 dan menurunkan kadar NO pada hewan coba pada dosis yang digunakan. Pemberian ekstrak air biji N. sativa pada dosis 100μg/kgBB memberikan efek relatif lebih baik terhadap kelangsungan hidup mencit yang diinfeksi P. berghei NK65 dibanding dosis lain. N. sativa dapat menghambat jumlah parasit dan kadar NO. NO dapat berfungsi sebagai anti parasit pada kadar tertentu, apabila kadarnya terlalu kecil fungsi sebagai antiparasitnya tidak optimal, namun jika kadarnya terlalu tinggi akan bersifat merusak karena sifat radikal bebasnya.

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AbstractNigella sativa L. has been reported to exhibit many pharmacologicaleffects, including anti-parasitic properties. This study investigated the anti-malarial effects of a water extract of N. sativa seed in Mus muculus mice infected with the Plasmodium berghei NK65 parasite. The method used was to take a blood parasitaemia count, following the use of Giemsa dye, determining the level of nitric oxide in mice that were infected with P. berghei malaria, using the spectrophotometric method, and determining their survival rate after 20 days of being infected with P. berghei malaria. The results showed that the decrease in the number of parasitaemia and the level of nitric oxide in subjects treated with doses of N. sativa was significant (p < 0.05). Further results showed that P. berghei-infected mice that were given 100 μg/kg of body weight had a better chance of survival. The conclusion is that the provision of N. sativa may reduce thenumber of malaria parasites and reduce levels of NO. The decrease in the number of parasites may be caused by an immune mechanism, through the regulation of NO levels (lower levels of NO), due to the influence of the anti-oxidant effects of N. sativa. Survival rates of the mice did not show significant results with reduced levels of parasitaemia and NO. This is likely to be because the levels of NO in this group were below the threshold levels at which NO can function as an anti-parasitic. It is alleged that, while NO can function as an anti-parasitic at certain levels, at lower levels its function as an antiparasitic is not optimal. On the other hand, if the levels are too high, damage will result, because of the nature of free-radicals. "

"[ABSTRAKPasak bumi (PB) (Eurycoma longifolia Jack), adalah tanaman herbal Indonesia yangdigunakan sebagai antimalaria. Penelitian terdahulu meliputi efek anti ageing dan antiinflamasi, namun belum pernah diteliti tentang efek terhadap aktivitas enzimantioksidan pada penggunaan ekstrak akar PB. Penelitian ini bertujuan untukmengetahui apakah pengaruh ekstrak akar PB sebagai antimalaria dapat menurunkanaktivitas spesifik antioksidan enzimatik. Penelitian ini menggunakan mencit yangdiinfeksi Plasmodium berghei, diterapi dengan ekstrak akar PB, klorokuin 10 mg/kgBB (kontrol positif, KP), kontrol negatif (akuades, KN), kontrol normal (K0), PB 30(TI), 60 (TII) dan 90 mg/kg BB (TIII). Parameter yang diukur adalah inhibisiparasitemia, kadar karbonil, aktivitas spesifik SOD, katalase (CAT). Inhibisiparasitemia hari ke 7 dari KP, TI, TII dan TIII adalah 69,81%, 39,37%, 41,72% dan12,92%. Aktivitas spesifik enzim SOD dan CAT plasma tidak ada perbedaanbermakna. Aktivitas spesifik SOD hati menunjukan perbedaan bermakna antara K0-KN (p=0,000), K0-KP (p= 0,025), KN-TI (p=0,001), KP-TI (p=0,042), KN-TII(p=0,002), KN-TIII (0,005). Aktivitas spesifik CAT hati menunjukkan perbedaanbermakna antara KP-TI (p=0,009), KP-TII (p=0,009), KP-TIII (p=0,014), KP-K0(p=0,009), TI-TIII (p=0,014), KN-TI (p=0,009), KN-TII (p=0,047), K0-KN(p=0,047). Kadar karbonil plasma dan hati tidak menunjukkan perbedaan bermaknaantar kelompok. Korelasi positif bermakna (r=0,690, p=0,000) terjadi antara aktivitasspesifik SOD dan CAT hati. Korelasi negatif bermakna terjadi antara aktivitasspesifik SOD, CAT hati dan parasitemia (r= -0,637, p=0,000) (r=-0,557, p=0,002).Kesimpulan: Potensi PB sebagai antimalaria diragukan karena herbal ini jugamemiliki efek antioksidan yang menguntungkan bagi parasit.

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ABSTRACTPasak bumi (PB)(Eurycoma longifolia Jack), is an Indonesian herb used asantimalarial. Previous studies had been done on its anti-ageing and anti-inflammationproperties, but its effect on antioxidant enzyme had not been researched. This studyaim to investigate the antimalarial influence of PB extract on the reduction of specificantioxidant activity of the SOD and CAT enzyme. We used mice infected byPlasmodium berghei treated with: PB 30, 60, and 90 mg/kg BW as (TI, TII, andTIII), positive control (chloroquine 10 mg/kg BW) (KP), negative control (aquadest)(KN), normal mice control (K0). The parameters were: growth inhibition, carbonylconcentration, specific activity of SOD and CAT. Growth inhibition in 7 day groupsof KP, TI, TII, and TIII were 69,81%, 39,37%, 41,72%, and 12,92%. Specific activityof plasma SOD and CAT were insignificant between groups. Liver SOD specificactivity showed significant different between K0-KN (p=0,000), K0-KP (p= 0,025),KN-TI (p=0,001), KP-TI (p=0,042), KN-TII (p=0,002), KN-TIII (0,005). Specificactivity of liver CAT showed significant different between KP-TI (p=0,009), KP-TII(p=0,009), KP-TIII (p=0,014), KP-K0 (p=0,009), TI-TIII (p=0,014), KN-TI(p=0,009), KN-TII (p=0,047), K0-KN (p=0,047). Carbonyl concentrations showinsignificant between groups in plasma and liver. Positive correlation (r=0,690,p=0,000) showed between liver SOD and CAT specific activity, negative correlationshowed between liver SOD (r= -0,637, p=0,000), CAT (r= -0,557, p=0,002) specificactivity and paracytemia. Therefore, The potential use of PB as an antimalarial was ofdoubtful effectiveness due to its antioxidant effect which could be beneficial to theparasite, Pasak bumi (PB)(Eurycoma longifolia Jack), is an Indonesian herb used asantimalarial. Previous studies had been done on its anti-ageing and anti-inflammationproperties, but its effect on antioxidant enzyme had not been researched. This studyaim to investigate the antimalarial influence of PB extract on the reduction of specificantioxidant activity of the SOD and CAT enzyme. We used mice infected byPlasmodium berghei treated with: PB 30, 60, and 90 mg/kg BW as (TI, TII, andTIII), positive control (chloroquine 10 mg/kg BW) (KP), negative control (aquadest)(KN), normal mice control (K0). The parameters were: growth inhibition, carbonylconcentration, specific activity of SOD and CAT. Growth inhibition in 7 day groupsof KP, TI, TII, and TIII were 69,81%, 39,37%, 41,72%, and 12,92%. Specific activityof plasma SOD and CAT were insignificant between groups. Liver SOD specificactivity showed significant different between K0-KN (p=0,000), K0-KP (p= 0,025),KN-TI (p=0,001), KP-TI (p=0,042), KN-TII (p=0,002), KN-TIII (0,005). Specificactivity of liver CAT showed significant different between KP-TI (p=0,009), KP-TII(p=0,009), KP-TIII (p=0,014), KP-K0 (p=0,009), TI-TIII (p=0,014), KN-TI(p=0,009), KN-TII (p=0,047), K0-KN (p=0,047). Carbonyl concentrations showinsignificant between groups in plasma and liver. Positive correlation (r=0,690,p=0,000) showed between liver SOD and CAT specific activity, negative correlationshowed between liver SOD (r= -0,637, p=0,000), CAT (r= -0,557, p=0,002) specificactivity and paracytemia. Therefore, The potential use of PB as an antimalarial was ofdoubtful effectiveness due to its antioxidant effect which could be beneficial to theparasite]"

"Sejalan dengan semakin tingginya resistensi terhadap obat antimalaria dalam klinis, terdapat kebutuhan dilakukan pencarian senyawa-senyawa kimia yang berpotensi. Metode komputasi digunakan untuk membantu pencarian karena memiliki keunggulan seperti tidak banyak mengeluarkan biaya dan dapat dipercaya memprediksi afinitas ikatan ligan dengan target obat (protein). Tujuan penelitian adalah untuk mendapatkan senyawa analog triklosan dan senyawa herbal Indonesia yang berpotensi sebagai antimalaria. Analog triklosan dan beberapa senyawa basis data herbal Indonesia dihitung afinitas ikatannya dengan metode Molecular Mechanics Poisson-Blotzmann Surface Area (MM-PBSA) pada Plasmudium falciparum Enoyl Reductase(PfENR), dengan tiga titik variabel suhu 27oC, 37oC, dan 39oC. Didapatkan nilai energi bebas Gibbs (ΔG) pada analog triklosan enansiomer 1b -18,5009 kkal/mol suhu 37oC dan pada senyawa herbal spinasterol -31,3435 kkal/mol suhu 37oC dan limasin -24,9885 kkal/mol suhu 37oC. Dengan nilai energi bebas Gibbs tersebut menunjukkan bahwa senyawa tersebut memiliki potensi sebagai antimalaria.

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Keeping pace with emerging drug resistance in clinically important pathogens will be greatly aided by inexpensive yet reliable computational methods that predict the ligands binding affinities for drug targets. the aim of this study to obtain potention antimalaria from analogues triclosan compound and Indonesia herbal compound. Analogues triclosan and several compound from Indonesia herbal database form Indonesia be calculated with molecular mechanics Poisson-Boltzmann surface area (MM-PBSA) for the Plasmodium falciparum Enoyl Reductase (PfENR), at three point variable of temperature 27oC, 37oC, and 39oC. Obtained Gibbs free energy (ΔG) for analogues triclosan enansiomer 1b -18,5009 kkal/mol 37oC and for herbal compound spinasterole -31,3435 kkal/mol 37oC dan limacine -24,9885 kkal/mol 37oC. With that Gibbs free enrgy enansiomer 1a, spinasterole, and limacine shows that compound have potention as antimalaria."