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"ABSTRAKMalaria merupakan salah satu penyakit yang menyebabkan korban jutaan jiwasetiap tahun. Plasmepsin adalah enzim utama di antara enzim lain dalam siklushidup plasmodium penyebab malaria yang mendegradasi hemoglobin selama faseeritrosit di dalam vakuola makanan. Dewasa ini, industri farmasi telah berupayauntuk mengembangkan agen terapetik yang dapat menyembuhkan penyakitmalaria melalui penemuan senyawa baru penghambat plasmepsin mengingatadanya penyebaran strain yang resisten terhadap obat antimalaria. Namun, karenabiaya yang tinggi dan waktu yang lama, metode konvensional untuk penemuanobat baru yang dilakukan secara in vivo dan in vitro sulit terealisasikan sehinggapara ilmuwan kemudian beralih kepada metode baru yaitu penapisan in silico.Jenis penapisan in silico yang akan dilakukan dalam penelitian ini adalahpenapisan berbasis struktur dengan menggunakan Basis Data Tanaman ObatIndonesia dan perangkat lunak GOLD. Berdasarkan penapisan ini, didapatkanhasil 11 kandidat senyawa inhibitor yang diharapkan dapat dikembangkan sebagaiobat antimalaria. Senyawa tersebut yaitu Trimyristin; Cyanidin 3,5-di-(6-malonylglucoside); Isoscutellarein 4?-methyl ether 8-(6?-n-butylglucuronide);Cyanidin 3-(6?-malonylglucoside)-5-glucoside; Multifloroside; Delphinidin 3-(2-rhamnosyl-6-malonylglucoside); Delphinidin 3-(6-malonylglucoside)-3?,5?-di-(6-p-coumaroylglucoside); Cyanidin 3-[6-(6-sinapylglucosyl)-2-xylosylgalactoside;Kaempferol 3-glucosyl-(1-3)-rhamnosyl-(1-6)-galactoside; Sanggenofuran A; danLycopene dengan kisaran GOLDScore dari 78,4647 sampai 98,2836. Duakandidat di antaranya berikatan dengan seluruh residu dari sisi katalitikplasmepsin yaitu Asp34 dan Asp214.

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ABSTRACTMalaria is one of diseases that annually emerge millions victim. Among the other

enzymes, plasmepsin is the main enzyme in plasmodium life cycle that degrades

hemoglobin during erythrocytic phase in food vacuole. Recently, pharmaceutical

industries have been trying to develop therapeutic agents that be able to cure

malaria through discovery of new plasmepsin inhibitor compounds, regarding to

the spread of drug-resistant strains for antimalarial. However, due to high cost and

long term, conventional methods for discovery of new drugs that were done in

vivo and in vitro were difficult to be realized so that the scientists then shift to the

new method called in silico screening. The chosen in silico screening method in

this experiment is structure-based screening by using GOLD software and

Indonesian Medicinal Plants Database. Based on the obtained results from this

screening, there are 11 inhibitor candidates which are expected to be developed as

antimalarial. These compounds are Trimyristin; Cyanidin 3,5-di-(6-

malonylglucoside); Isoscutellarein 4?-methyl ether 8-(6?-n-butylglucuronide);

Cyanidin 3-(6?-malonylglucoside)-5-glucoside; Multifloroside; Delphinidin 3-(2-

rhamnosyl-6-malonylglucoside); Delphinidin 3-(6-malonylglucoside)-3?,5?-di-(6-

p-coumaroylglucoside); Cyanidin 3-[6-(6-sinapylglucosyl)-2-xylosylgalactoside;

Kaempferol 3-glucosyl-(1-3)-rhamnosyl-(1-6)-galactoside; Sanggenofuran A; and

Lycopene with GOLDScore range from 78,4647 to 98,2836. Two of them bind

with all residues in catalytic site of plasmepsin which are Asp34 and Asp214."

"Sambiloto atau Andrographis panniculata merupakan tanaman tradisional herbal yang yang banyak ditemui di Indonesia. Penelitian Biokimia tentang efek antioksidan zat berkhasiatnya belum banyak diteliti. Penelitian ini bertujuan untuk menganalisa aktivitas antimalaria ekstrak etanol sambiloto (EES) pada hati mencit yang diinfeksi dengan Plasmodium berghei melalui pengukuran kadar malondialdehid (MDA) dan glutation (GSH). Metode: Mencit jantan galur Balb/c dengan berat 28-30 g, 7-8 minggu, dibagi menjadi 4 kelompok secara acak, tiap kelompok terdiri atas 5 ekor mencit. Kelompok K: Kontrol, Kelompok A: kontrol negatif, Kelompok B: EES 2 mg/kgBB/hari selama 7 hari, C: klorokuin 10 mg/kgBB/hari selama 3 hari. MDA dan GSH diperiksa dengan metode spektrofotometri. Hasil: Terlihat kadar MDA hati yang lebih rendah pada kelompok perlakuan EES dan klorokuin, walaupun tidak berbeda bermakna dibandingkan dengan kelompok kontrol negatif (p≥0,05). Pada kelompok B dan C terlihat peningkatan kadar GSH dibandingkan kelompok kontrol negatif, kenaikan ini mendekati kadar kelompok kontrol. Pada pengujian statistik, tidak terlihat perbedaan yang bermakna antara kelompok K, B dan C (p≥0,05). Kesimpulan: EES dapat menurunkan kadar MDA dan meningkatkan kadar GSH pda hati mencit yang diinfeksi dengan Plasmodium berghei, walaupun hasil ini belum bermakna dibandingkan dengan kontrol negatif. Untuk aktivitas yang lebih signifikan di hati diperlukan pemberian EES dengan dosis yang lebih tinggi dari 2 mg/kgBB.

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Andrographis paniculata is a traditional herb medicine usually used in Indonesia. The aim of this study were to determine the anti-malarial activity of ethanolic extract of sambiloto (EES) in Plasmodium berghei-infected mice through measuring the malondialdehyde MDA) and glutathione (GSH) levels.

Methods: Male mice (Balb/c strain) with weight 28-30 g, 7-8 weeks old, were randomly devided into 4 groups of 5 animals each. Group K: control (nil), Group A: negative control, and 2 treatment groups (B, C). Group B: EES 2 mg/kgBW, once per day for 7 days, and group C: chloroquine 10 mg/kgBW, once a day, for 3 days. All treatment was administered orally.

Results: MDA level of liver occurs lower in the EES and chloroquine treatment groups, although is not significant with negative control group (p ≥ 0.05). In B and C groups shown the increase of GSH liver level compared to the negative control group, but the level is approaching control group. On statistical analysis, there is no significant difference seen between the control, B and C groups (p ≥ 0.05).

Conclusion: EES can reduce MDA level and increased GSH level in mice liver infected with Plasmodium berghei, although this result is not significant compared to the negative control. For the significant effect, need further investigation to find the appropriate dose for hepar tissue."

"Artemisinin merupakan senyawa SOH-seskuiterpen lakton dengan gugus unik peroksida yang berhasil diisolasi dari tanaman Artemisia annua. Dari hasil uji in vitro dan in vivo, artemisinin terbukti efektif melawan malaria dan menunjukkan hasil yang menggembirakan, bahkan untuk galur Plasmodium yang telah kebal sekalipun. Dihidroartemisinin adalah salah satu derivat artemisinin dari hasil semisintesis sederhana, yang lebih poten dari artemisinin. Penelitian ini bertujuan memodifikasi struktur artemisinin menjadi dihidroartemisinin menggunakan katalis Ni/TiO2 melalui proses hidrogenasi dan mengkaji aktivitasnya sebagai antimalaria melalui uji in vitro. Cara baru modifikasi struktur artemisinin menjadi derivatnya dihidroartemisinin telah berhasil dilakukan melalui reaksi hidrogenasi menggunakan katalis Ni/TiO2 Sintesis senyawa ini menghasilkan kristal berbentuk jarum dengan titik leleh 151- 153oC. Rendemen yang diperoleh sebesar 16.58%. Analisa TLC dengan plat silika gel 60 F254 menggunakan eluen toluene: etil asetat: asam formiat menunjukkan satu spot dengan Rf 0,44. Analisa LC-MS menunjukkan satu puncak dengan tR 2.2 menit serta berat molekul 284.29 sama dengan dihidroartemisinin yaitu C15H24O5. Spektrum IR menunjukkan adanya gugus hidroksil pada frekuensi 3371.57 cm-1 didukung dengan munculnya pita serapan dari vibrasi ulur C-O pada frekuensi 1034.14 cm-1. Reaksi hidrogenasi tidak merusak keberadaan gugus endoperoksida. Hal ini terbukti dengan masih terdapatnya serapan vibrasi ulur dari C-O-O-C pada frekuensi 1091.71; 875.68; 844.82 cm-1. Dari data NMR membuktikan bahwa senyawa tersebut adalah campuran rasemat STX/ETX dihidroartemisinin. Senyawa ini mempunyai aktivitas antimalaria dengan IC50 0.20 nM, melalui uji in vitro menggunakan biakan Plasmodium falciparum kultur 3D7.

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Artemisinin is a SOH-sesquiterpene lactone that incorporates an endoperoxide moiety. This compound is isolated as the active compound of Artemisia annua. Based on the result of in vitro and in vivo assay, artemisinin is an effective antimalarial drug and it shows possitive result, moreover strain of Plasmodium resistant. Dihydroartemisinin is the simplest semisynthetic derivative of artemisinin and is more potent than artemisinin. The objective of this research are to modify the structure of artemisinin into dihydroartemisinin. A new way to modify the structure of artemisinin into dihydroartemisinin, had been successfully done using hydrogenation process with Ni/TiO2 catalyst, and the result was a soft white needle like crystal with melting point of 151-153oC. The yield of the crystal was 16.58%. the TLC analysis on TLC plate silica gel 60 F254 using toluene: etil asetat: asam formiat showed a spot with Rf 0.44. LC-MS analysis showed that the compound contained mainly a peak with tR 2.2 minutes and mass spectrum showed that the molecular weight of the compound was 284.29 which is similar to that of dihydroartemisinin, C15H24O5. The IR spectrum showed that there was a spectrum from C-O in a frequency of 1034.14 cm-1. Hydrogenation reaction did not destroy the existance of endoperoxide group. This was proven by the existance of C-O-O-C in a frequency of 1091.71; 875.68; 844.82 cm-1. NMR data showed that the compound was the mixture of racemic. The compund also had the activity of antimalarial with IC50 0.20 ng/ml by using in vitro test with Plasmodium falciparum strain 3D7."

"Latar belakang: Bayamduri (Amaranthus spinosus L.) adalah herbal tradisional yang digunakan untuk pengobatan malaria dan belum banyak data penelitian tentang ini. Penelitian ini bertujuan untuk mengetahui aktivitas skizontisidal ekstrak air bayam duri (Amaranthus spinosus L) (EABD) terhadap mencit yang diinfeksi Plasmodium berghei secara in vivo. Metode: Mencit jantan (galur Balb/c) dengan berat 28-30 g, 7-8 minggu, dibagi menjadi 4 kelompok secara acak, tiap kelompok terdiri atas 5 ekor mencit. Kelompok K: kontrol, Kelompok A: kontrol negatif, 2 Kelompok perlakuan (B dan C). Kelompok B: ekstrak Amaranthus 120 mg/kgBB, 1 kali per hari selama 4 hari. dan kelompok C: klorokuin 10 mg/kgBB sekali sehari selama 3 hari. Seluruh perlakuan diberikan melalui oral. Hasil: Aktivitas skizontisidal darah terlihat pada semua kelompok perlakuan (B dan C), Aktivitas tertinggi terlihat pada kelompok B yaitu 91,20 ± 0,73 %, sedang kelompok C sebesar 88,92 ± 1,10 %. Kedua kelompok berbeda secara bermakna dibandingkan dengan kontrol, p≤0,05, namun kedua kelompok tidak berbeda bermakna satu sama lain, p≥0,05. Terjadi peningkatan berat badan pada kelompok EABD yang hampir sama dengan kelompok kontrol dan lebih besar dibanding kelompok klorokuin (7,6 % vs 7,05% dan 5,48%). Kesimpulan: Ekstrak air bayam duri (Amaranthus spinosus) (EABD) dosis 120 mg/kgBB menunjukkan aktivitas skizontisidal darah yang sama baik dengan pemberian klorokuin 10 mg/kgBB terhadap mencit yang diinfeksi Plasmodium berghei secara in vivo.

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Background: Amaranthus spinosus is a traditional herb used for the treatment of malaria, but the information of it?s activity still limited. The aim of this study was to determine the schizonticidal effect of a water extract of Amaranthus spinosus against Plasmodium berghei-infected mice.

Methods: Male mice (Balb/c strain) weighing 28-30 g, 7-8 weeks old, were randomly devided into 4 groups of 5 animals each. Group K: controls (nil), Group A: negative controls, and 2 treatment groups (B and C). Group B: Amaranthus 120 mg/kgBW, once per day for 4 days and group C: Chloroquine 10 mg/kgBW, once a day for 3 days. All treatments administrated orally.

Results: Blood schizonticidal activity was seen in all treatment groups, the highest activity was seen in group B ( 91.20 ± 0.73%), and group C was 88.92 ± 1.10%. Both groups were significantly different compared to control, p≤0,05), but there were no different within both group. An increase in body weight in group B are almost the same as group K and greater than group C (7.6% vs 7.05% and 5.48%).

Conclusion: The Amaranthus spinosus water extract (ASWE) at a dose 120 mg/kgBW demonstrated a good blood schizonticidal activity as well as chloroquine against Plasmodium berghei-infected mice."

"Resistensi Plasmodium terhadap obat antimalaria merupakan masalah yang harus diatasi. Salah satu caranya dengan mencari obat baru. Penelitian ini bertujuan untuk mengetahui pengaruh ekstrak bunga dan ekstrak kulit buah Delonix regia dalam menurunkan densitas Plasmodium. Penelitian menggunakan desain uji eksperimental. Berdasarkan hasil uji fitokimia diketahui kadar alkaloid dalam esktrak kulit buah lebih tinggi dibandingkan kadar alkaloid dalam ekstrak bunga. Hal ini sesuai dengan hasil uji in vivo pada mencit yang diinfeksi Plasmodium berghei. Mencit yang mendapatkan ekstrak kulit buah dengan dosis 2,8 mg/mencit, 8,4 mg/mencit dan 14 mg/mencit mengalami penurunan densitas Plasmodium sedangkan pada mencit yang mendapatkan ekstrak bunga terjadi kenaikan densitas Plasmodium. Berdasarkan uji Post Hoc LSD didapatkan adanya perbedaan perubahan densitas Plasmodium yang signifikan pada mencit yang mendapatkan kontrol negatif dibandingkan dengan mencit yang mendapatkan ekstrak kulit buah dosis kecil, sedang maupun besar dengan nilai p 0,00; 0,03 dan 0,022. Sedangkan perbedaan yang tidak signifikan di dapatkan saat perubahan densitas Plasmodium pada mencit yang mendapatkan kontrol negatif dibandingkan dengan mencit yang mendapatkan ekstrak bunga dengan nilai p 0,156; 0,064 dan 0,923. Dapat disimpulkan ekstrak kulit buah dapat menurunkan densitas Plasmodium.

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Resistance of Plasmodium to anti-malaria drugs is a problem that necessary to be solved. One of the way is create new drugs. The purpose of this study to determine the effect of flowers extracts and rinds extracts of Delonix regia to decrease density of Plasmodium. This study use experimental design. Based on the results of phytochemical test known that alkaloid levels in rind's extract is higher than flower's extract. This is consistent with the results of in vivo test in mice infected by Plasmodium berghei. The mice whom get rind's extract dose ie 2,8 mg/mice, 8,4 mg/mice dan 14 mg/mice shown decrease of parasitemia, mean while mice whom get flowers shown increase of parasitemia.

Based on Post Hoc LCD test, there is significantly difference in density change of plasmodium in mice whom get negative control compare with mice whom get small dose, medium dose and high dose of rinds extracts with the value of p 0,00; 0,03 and 0,022. While there is no significantly difference when mice whom get negative control compare with mice whom get small dose, medium dose and high dose of flowers extracts with the value of p 0,156; 0,064 and 0,923. It can be concluded that rind's extract of Delonix regia can decrease parasitemia."

"ABSTRAKPendahuluan: Sambiloto atau Andrographis panniculata merupakan sebuahtanaman herbal yang memiliki khasiat sebagai antimalaria dengan carameningkatkan kerja antioksidan dalam tubuh. Hati merupakan salah satu tempatterjadinya fase perkembangan Plasmodium pada penyakit malaria. Penelitian inibertujuan untuk menganalisis aktivitas antimalaria dari Ekstrak Etanol Sambiloto(EES) pada mencit yang diiinfeksi Plasmodium berghei secara in vivo melalupengukuran kadar MDA dan aktivitas spesifik katalase jaringan hati.Metode: Desain penelitian yang digunakan adalah eksperimental in vivomenggunakan hewan coba mencit Balb/c. Metode penelitian dilakukan denganmengelompokkan mencit ke dalam empat kelompok yaitu kelompok kontrol yangtidak diberi perlakuan, kelompok I yang diinduksi Plasmodium berghei tetapitidak diterapi, kelompok II yang diinduksi Plasmodium berghei dan diberi EES 2mg/kgBB serta kelompok III yang diinduksi Plasmodium berghei dan diberiklorokuin 10 mg/kgBB selama 3 hari. Analisis kadar MDA dilakukan denganmetode Wills dan aktivitas spesifik katalase dengan metode Mates et al.Hasil: Hasil penelitian menunjukkan terjadi penurunan kadar MDA yang tidaksignifikan pada mencit yang diinfeksi dengan Plasmodium berghei dan diberiekstrak etanol sambiloto (EES) 2 mg/kgBB dibandingkan dengan kontrol negatif(66.49 ± 22,92 vs 69.40 ± 11,69 nmol/g jaringan hati). Namun pada kelompokyang diberi perlakuan klorokuin juga terlihat penurunan kadar MDA yang tidaksignifikan dibandingkan dengan kontrol negatif (67.49 ± 7,04 vs 69.40 ± 11,69nmol/g jaringan hati). Sedangkan aktivitas spesifik katalase kelompok yang diberiEES menunjukkan peningkatan yang tidak berbeda bermakna dibandingkandengan kelompok kontrol (2,73 ± 0,59 vs 3,73 ± 1.56 Unit/mg jaringan hati).Begitupula dengan klorokuin yang menunjukkan peningkatan aktivitas spesifikkatalase yang tidak berbeda bermakna dibandingkan dengan kelompok kontrol(2,97 ± 1,53 vs 3,73 ± 1.56).Kesimpulan: Pada kelompok dengan pemberian EES 2 mg/kgBB terjadipenurunan kadar MDA serta peningkatan aktivitas spesifik katalase jaringan hatimencit dibandingkan dengan kelompok negatif, tetapi secara statistik tidakbermakna demikian pula dengan kelompok yang diberi klorokuin.

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ABSTRACTIntroduction: Andrographis panniculata or Sambiloto is a herbal plant that hasantimalarial efficacy by increasing antioxidant in body. Liver is one of the placesfor Plasmodium to develop themselves in malaria. This research aims to analyzethe activity of antimalarial from Sambiloto Ethanol Extract (SEE) in mice whichinfected by Plasmodium berghei in vivo through the measurement of MDA leveland the specific activity of catalase in liver tissue.Method: We used experimental in vivo as the reserach design, using balb/c. Theresearch design is done by grouping the mices into four groups which of theuntreated group, group I-induced by Plasmodium berghei but not treated, groupII-induced Plasmodium berghei and treated with SEE 2 mg/kg Body weight,group III-induced Plasmodium berghei and treated with chloroquine with 10mg/kg Body weight in three days. The MDA level analyze is done by the Willsmethod and the specific activity of catalase with Mates et al method.Result: The research result showed the decrease of MDA level which notsignificant in mice that is infected by Plasmodium berghei and treated by SEE 2mg/ kg BW compared to negative control (66.49 ± 22,92 vs 69.40 ± 11,69 nmol/gliver tissue). However, group that is infected by Plasmodium berghei and treatedby chloroquine also showed the decrease of MDA level which not significantcompared the negative control (67.49 ± 7,04 vs 69.40 ± 11,69 nmol/g liver tissue).Instead, group which treated by SEE showed the increase in specific activity ofcatalase compared with control (2,73 ± 0,59 vs 3,73 ± 1.56 Unit/mg liver tissue).Similarly with chloroquine group which showed an increase in specific activity ofcatalase were not significantly different compared with the control group (2.97 ±1.53 vs 3.73 ± 1.56 Unit/mg liver tissue).Conclusion: Group that treated with SEE 2 mg/kg Body weight showed decreaseof MDA level and also the increase of catalase specific activity in mice liver tissuecompared negative control, but statistically not significant as well as the groupgiven chloroquine;Introduction: Andrographis panniculata or Sambiloto is a herbal plant that hasantimalarial efficacy by increasing antioxidant in body. Liver is one of the placesfor Plasmodium to develop themselves in malaria. This research aims to analyzethe activity of antimalarial from Sambiloto Ethanol Extract (SEE) in mice whichinfected by Plasmodium berghei in vivo through the measurement of MDA leveland the specific activity of catalase in liver tissue.Method: We used experimental in vivo as the reserach design, using balb/c. Theresearch design is done by grouping the mices into four groups which of theuntreated group, group I-induced by Plasmodium berghei but not treated, groupII-induced Plasmodium berghei and treated with SEE 2 mg/kg Body weight,group III-induced Plasmodium berghei and treated with chloroquine with 10mg/kg Body weight in three days. The MDA level analyze is done by the Willsmethod and the specific activity of catalase with Mates et al method.Result: The research result showed the decrease of MDA level which notsignificant in mice that is infected by Plasmodium berghei and treated by SEE 2mg/ kg BW compared to negative control (66.49 ± 22,92 vs 69.40 ± 11,69 nmol/gliver tissue). However, group that is infected by Plasmodium berghei and treatedby chloroquine also showed the decrease of MDA level which not significantcompared the negative control (67.49 ± 7,04 vs 69.40 ± 11,69 nmol/g liver tissue).Instead, group which treated by SEE showed the increase in specific activity ofcatalase compared with control (2,73 ± 0,59 vs 3,73 ± 1.56 Unit/mg liver tissue).Similarly with chloroquine group which showed an increase in specific activity ofcatalase were not significantly different compared with the control group (2.97 ±1.53 vs 3.73 ± 1.56 Unit/mg liver tissue).Conclusion: Group that treated with SEE 2 mg/kg Body weight showed decreaseof MDA level and also the increase of catalase specific activity in mice liver tissuecompared negative control, but statistically not significant as well as the groupgiven chloroquine;Introduction: Andrographis panniculata or Sambiloto is a herbal plant that hasantimalarial efficacy by increasing antioxidant in body. Liver is one of the placesfor Plasmodium to develop themselves in malaria. This research aims to analyzethe activity of antimalarial from Sambiloto Ethanol Extract (SEE) in mice whichinfected by Plasmodium berghei in vivo through the measurement of MDA leveland the specific activity of catalase in liver tissue.Method: We used experimental in vivo as the reserach design, using balb/c. Theresearch design is done by grouping the mices into four groups which of theuntreated group, group I-induced by Plasmodium berghei but not treated, groupII-induced Plasmodium berghei and treated with SEE 2 mg/kg Body weight,group III-induced Plasmodium berghei and treated with chloroquine with 10mg/kg Body weight in three days. The MDA level analyze is done by the Willsmethod and the specific activity of catalase with Mates et al method.Result: The research result showed the decrease of MDA level which notsignificant in mice that is infected by Plasmodium berghei and treated by SEE 2mg/ kg BW compared to negative control (66.49 ± 22,92 vs 69.40 ± 11,69 nmol/gliver tissue). However, group that is infected by Plasmodium berghei and treatedby chloroquine also showed the decrease of MDA level which not significantcompared the negative control (67.49 ± 7,04 vs 69.40 ± 11,69 nmol/g liver tissue).Instead, group which treated by SEE showed the increase in specific activity ofcatalase compared with control (2,73 ± 0,59 vs 3,73 ± 1.56 Unit/mg liver tissue).Similarly with chloroquine group which showed an increase in specific activity ofcatalase were not significantly different compared with the control group (2.97 ±1.53 vs 3.73 ± 1.56 Unit/mg liver tissue).Conclusion: Group that treated with SEE 2 mg/kg Body weight showed decreaseof MDA level and also the increase of catalase specific activity in mice liver tissuecompared negative control, but statistically not significant as well as the groupgiven chloroquine"

"Malaria merupakan masalah kesehatan di dunia. Tantangan yang muncul di mengatasi malaria adalah munculnya resistensi terhadap klorokuin, salah satu obat antimalaria. Perlawanan telah mendorong berbagai penelitian untuk menemukan senyawa antimalaria baru. Salah satu potensinya adalah propolis, produk lebah madu, yang mengandung luteolin 7-O glukosida dan kalkon. Luteolin 7-O glukosida menghambat tipe 2. biosintesis asam lemak parasit dan chalcone menghambat proses hemolisis. Tujuan dari penelitian ini mempelajari efektivitas kombinasi propolis dan klorokuin dibandingkan diobati dengan klorokuin, propolis saja, dan terapi kombinasi dalam parasitemia mencit (Mus musculus) yang terinfeksi Plasmodium berghei. Dosis propolis yang diuji adalah 30 mg/kgBB dan 60 mg/kgBB. Perbedaan tingkat parasitemia yang terkecil dan terbesar masing-masing berada pada kelompok perlakuan terapeutik klorokuin saja, terapi kombinasi dengan dosis 60 mg/kg, terapi kombinasi dengan dosis 60 mg/kgBB, terapi tunggal propolis dengan dosis 30 mg/kgBB, dan terapi tunggal propolis dosis 60 mg/kg berat badan. Terapi tunggal propolis 30 mg/kgBB berhasil dihambat pertumbuhan parasit yang signifikan Namun terapi tunggal propolis 60 mg/kgBB memiliki pengaruh yang tidak signifikan terhadap percepatan pertumbuhan parasit. Namun, terapi tunggal propolis masih belum sebanding dengan terapi tunggal klorokuin. Terapi kombinasi propolis tidak memberikan perubahan yang signifikan pada efek antimalaria klorokuin. Oleh karena itu, dapat disimpulkan bahwa propolis pada dosis 30 mg/kgBB dan 60 mg/kgBB tidak sesuai untuk digunakan pada terapi kombinasi dengan klorokuin.Malaria is a health problem in the world. Challenges that appear in to overcome malaria is the emergence of resistance to chloroquine, one of the antimalarial drugs. The resistance has prompted various studies to find new antimalarial compounds. One of the potential ispropolis, a honey bee product, which contains luteolin 7-O glucoside and chalcone. Luteolin 7-O glucoside inhibits type 2 . Parasite fatty acid biosynthesis and chalcone inhibit hemolysis. The aim of this study was to study the effectiveness of the combination of propolis and chloroquine compared to treatment with chloroquine, propolis alone, and combination therapy in parasitaemia of mice (Mus musculus) infected with Plasmodium berghei. The doses of propolis tested were 30 mg/kgBW and 60 mg/kgBW. The smallest and largest differences in parasitaemia levels were in the chloroquine only therapeutic treatment group, combination therapy at a dose of 60 mg/kg, combination therapy at a dose of 60 mg/kgBW, propolis single therapy at a dose of 30 mg/kgBW, and propolis single therapy. dose of 60 mg/kg body weight. Propolis single therapy 30 mg/kgBW was successfully inhibited by significant parasite growth. However, propolis 60 mg/kgBW single therapy had no significant effect on the acceleration of parasite growth. Although However, propolis single therapy is still not comparable to chloroquine single therapy. Propolis combination therapy did not give a significant change in the antimalarial effect of chloroquine. Therefore, it can be concluded that propolis at doses of 30 mg/kgBW and 60 mg/kgBW is not suitable for use in combination therapy with chloroquine."

"Sebagian marga Calophyllum telah diteliti dan memiliki khasiat sebagai tanaman obat. C. macrophyllum Scheff merupakan salah satu jenis Calophyllum yang ditemukan di gunung Kerinci provinsi Jambi. Penelitian terhadap kulit batang tanaman ini diawali dengan pengeringan simplisia yang dilanjutkan dengan proses ekstraksi, partisi, isolasi dan rekristalisasi menggunakan sistem dua pelarut. Penentuan struktur senyawa hasil isolasi dilakukan secara fisika, kimia dan spektroskopi meliputi UV-Vis, IR, GC-MS/LC-MS dan RMI (1HNMR, 13CNMR). Penentuan bioaktivitas secara in vitro meliputi uji toksisitas dengan metode BSLT (Brine Shrimp Lethality Test), uji antioksidan dengan metode DPPH (1,1-diphenil-2-pikrilhidrazil), uji antidiabetes menggunakan enzim α-glukosidase dan uji antimalaria terhadap parasit plasmodium. Dua senyawa berhasil diisolasi yaitu turunan metil ester asam lemak (metil-oktadek-14 enoik), berupa cairan berwarna kuning dengan titik didih 173-175°C dan senyawa flavan-3-ol (5,7,2?,5?-tetrahidroksi flavan-3-ol), berupa kristal berwarna coklat dengan titik leleh besar dari 300°C. Hasil uji toksisitas menunjukkan kedua senyawa toksis terhadap larva udang Artemia salina Leach dengan LC50 masing-masing sebesar 141,2 µg/mL dan 154,9 µg/mL. Uji antioksidan menunjukkan hanya senyawa flavan-3-ol yang memiliki aktivitas antioksidan dengan IC50 5,31 µg/mL. Uji antidiabetes juga menunjukkan hanya senyawa flavan-3-ol yang memiliki aktivitas antidiabetes dengan IC50 9,10 µg/mL. Tidak ada sama sekali aktivitas antimalaria diperlihatkan oleh kedua senyawa hasil isolasi.

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Several of Calophyllums genus have been searched and proven as medicinal plants. Calophyllum macrophyllum Scheff is plant growing in Sumatera island in Kerinci mounted area. The dried simplicia was extracted using maceration technique, then fractionated using coloumn chromatography and purified by crystallization using two solvents system. Molecule structure were determined using physical and spectroscopic data from LC-MS, GC-MS, UV, IR and 1H and 13C-NMR.

Bioactivity were assayed for toxicity using BSLT method, antioxidant activity using DPPH method, antimalarial activity by Trager and Jensen method, and antidiabetic activity was determined by inhibitory activity of α-glycosidase enzyme. Two compounds have been isolated from ethyl acetate fraction of the stem-bark. The compounds were methyl ester derivate [(Z) methyl-octadec-14-enoic], a yellow liquid with boiling point 173-175°C and flavan-3-ol (5,7,2?,5?-tetrahydroxy flavan-3-ol), a brown crystal with melting point > 300°C.

Toxicity activity showed for methyl ester derivate [(Z) methyl-octadec-14-enoic] and flavan-3-ol by LC50 of 141.2 µg/mL and 154.9 µg/mL respectively. On the other hand, antioxidant and antidiabetic activity only showed by flavan-3-ol by IC50 of 5.31 µg/ml and 9.10 µg/ml. No antimalarial activity showed by those isolated compounds."

"[Resistensi yang terjadi pada beberapa obat antimalaria, seperti klorokuin, mendasari gencarnya dilakukan penelitian yang bertujuan untuk menemukan terapi antimalaria alternatif, salah satunya dengan memanfaatkan potensi herbal dari alam Indonesia. Ekstrak tanaman yang terbukti pada penelitian in-vivo memiliki efek antimalaria adalah akar pasak bumi (Eurycoma longifolia jack). Penelitian ini merupakan penelitian eksperimental in-vivo yang menguji ekstrak akar pasak bumi dengan dosis 60 mg/kgbb, 75 mg/kgbb, dan 90 mg/kgbb terhadap mencit (Mus musculus) yang terinfeksi Plasmodium berghei. Peningkatan densitas parasitemia pada hari ke-4 terapi dosis 60 mg/kgbb lebih tinggi dari kontrol negatif, sedangkan terapi dosis 75 mg/kgbb dan 90 mg/kgbb lebih rendah dari kontrol negatif namun perbedaannya tidak signifikan secara statistik. Ditinjau dari persentase inhibisi parasitemia, terapi dosis 60 mg/kgbb memiliki persentase inhibisi parasitemia negatif, sedangkan terapi dosis 75 mg/kgbb dan 90 mg/kgbb memiliki persentase inhibisi parasitemia < 50%. Ditinjau dari kadar hemoglobin, ketiga dosis perlakuan memiliki kadar hemoglobin yang fluktuatif dan cenderung menurun hingga pada kondisi anemia. Hal ini menunjukkan bahwa ekstrak akar pasak bumi dosis 60 mg/kgbb tidak memiliki efek antimalaria, sedangkan dosis 75 mg/kgbb dan 90 mg/kgbb memiliki efek antimalaria namun kurang adekuat. Terapi dosis 90 mg/kgbb menunjukkan peningkatan densitas parasitemia hari ke-4 yang paling rendah dan persentase inhibisi parasitemia paling baik. Dengan demikian disimpulkan bahwa terapi ekstrak akar pasak bumi kurang tepat digunakan sebagai terapi tunggal malaria;Resistance on malaria medication, for example klorokuin, underlie the study that aim to find alternative malaria treatment by using herbal potention from the nature of Indonesia. Herbal extract that had been proven in vivo experimental study that has antimalarial effect is Pasak bumi root (Eurycoma longifolia jack). This study is in vivo experimental study that giving Pasak bumi root extract by dose 60 mg/kgbw, 75 mg/kgbw, and 90 mg/kgbw to mice (Mus musculus) infected by Plasmodium berghei. The increase of parasitemia density in the 4th day of treatment by dose 60 mg/kgbw is higher than negative control, while treatment by dose 75 mg/kgbw and 90 mg/kgbw are lower than negative control, but the difference is not significant in statistic analysis. Reviewed from parasitemia inhibition persentage, treatment by dose 60 mg/kgbw has negative parasitemia inhibition persentage, while treatment by dose 75 mg/kgbw and 90 mg/kgbw have parasitemia inhibition persentage <50%. Reviewed from hemoglobin level, those treatment by three doses have fluctuative hemoglobin level and tend to be decreasing till reaching anemia. It shows that pasak bumi root extract by dose 60 mg/kgbw does not have antimalarial effect, while 75 mg/kgbw and 90 mg/kgbw have inadequate antimalarial effect. Treatment by dose 90 mg/kgbw shows the lowest increase of 4th day parasitemia density and the best parasitemia inhibition persentage. Thus, it could be concluded that pasak bumi root extract is not good enough to be used as single treatment of malaria, Resistance on malaria medication, for example klorokuin, underlie the study that aim to find alternative malaria treatment by using herbal potention from the nature of Indonesia. Herbal extract that had been proven in vivo experimental study that has antimalarial effect is Pasak bumi root (Eurycoma longifolia jack). This study is in vivo experimental study that giving Pasak bumi root extract by dose 60 mg/kgbw, 75 mg/kgbw, and 90 mg/kgbw to mice (Mus musculus) infected by Plasmodium berghei. The increase of parasitemia density in the 4th day of treatment by dose 60 mg/kgbw is higher than negative control, while treatment by dose 75 mg/kgbw and 90 mg/kgbw are lower than negative control, but the difference is not significant in statistic analysis. Reviewed from parasitemia inhibition persentage, treatment by dose 60 mg/kgbw has negative parasitemia inhibition persentage, while treatment by dose 75 mg/kgbw and 90 mg/kgbw have parasitemia inhibition persentage <50%. Reviewed from hemoglobin level, those treatment by three doses have fluctuative hemoglobin level and tend to be decreasing till reaching anemia. It shows that pasak bumi root extract by dose 60 mg/kgbw does not have antimalarial effect, while 75 mg/kgbw and 90 mg/kgbw have inadequate antimalarial effect. Treatment by dose 90 mg/kgbw shows the lowest increase of 4th day parasitemia density and the best parasitemia inhibition persentage. Thus, it could be concluded that pasak bumi root extract is not good enough to be used as single treatment of malaria]"

"ABSTRAKMalaria masih menjadi salah satu masalah di dunia. Salah satu tantangan dalam eliminasi malaria adalah timbulnya resistensi obat antimalaria. Terjadinya resistensi telah mendorong usaha untuk penemuan kandidat obat antimalaria. Beberapa studi yang dilakukan memperlihatkan adanya aktivitas antimalaria dari produk fermentasi Streptomyces sp. Streptomyces sp. menghasilkan beberapa metabolit sekunder yang diantaranya memilki aktivitas antimalaria yaitu prodigiosin. Penelitian ini bertujuan untuk mengetahui efektivitas produk fermentasi Streptomyces sp. sebagai antimalaria, mekanisme kerja hambatannya dan sifat toksisitasnya terhadap sel HepG2. Penelitian ini merupakan penelitian eksperimental dengan teknik in vitro, menggunakan galur parasit Plasmodium falciparum 3D7 drug sensitive . Penelitian dilakukan untuk mengetahui potensi produk fermentasi Streptomyces sp. sebagai antimalaria dengan melakukan uji IC50, dan mekanisme kerja dengan Transmission Electron Microscopy TEM . Dilakukan pula uji toksisitas produk fermentasi Streptomyces sp. pada sel HepG2. Produk fermentasi Streptomyces sp. memiliki aktivitas sebagai antimalaria dengan nilai IC50 sebesar 0,001 ?g/mL, sedangkan kontrol kuinidin yang digunakan memiliki nilai IC50 sebesar 0,054 ?g/mL dan prodigiosin 0,022 ?g/mL. Hasil pengamatan dengan TEM menunjukkan tidak terbentuknya hemozoin. Produk fermentasi Streptomyces sp. bersifat tidak toksik terhadap sel hati HepG2 dengan nilai CC50 1380 ?g/mL. Produk fermentasi Streptomyces sp. memiliki potensi sebagai antimalaria dan tidak memiliki efek toksik terhadap sel HepG2

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ABSTRACTMalaria remains one of the problem in the world. One of the challenge in malaria elimination is the emergence of antimalarial drug resistance. The occurance of drug resistance has been encouraging efforts to find antimalarial drugs candidate. Some studies showed that there was antimalarial activity from Streptomyces sp. fermentation. Streptomyces sp. produced some secondary metabolite, which include prodigiosin who had antimalarial activity. This research aim to know the activity of Streptomyces sp. fermentation product as antimalarial, worked mechanism and toxicity on HepG2 cell. This research was experimental research with in vitro technique using Plasmodium falciparum 3D7 drug sensitive parasite. The research was done to know potency of Streptomyces sp. fermentation product as antimalarial by IC50 test, and worked mechanism by Transmission Electron Microscopy TEM . Toxicity tests was also done on HepG2 cell. Streptomyces sp. fermentation product has activity as antimalarial with IC50 value 0,001 g mL, quinidine control has IC50 value 0,054 g mL and prodigiosin 0,022 g mL. Observation with TEM showed no formation of hemozoin. Streptomyces sp. fermentation product was not toxic for HepG2 sel with CC50 value 1380 g mL. Streptomyces sp. fermentation product has a potency as antimalarial and not toxic for HepG2 cell."