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"Munculnya resistansi parasit yang cepat terhadap obat antimalaria yang tersedia saat ini telah menarik perhatian dalam penemuan obat. Andrografolida (ANDRO), suatu senyawa yang diisolasi dari tanaman obat Andrographis panniculata Nees, memperlihatkan sifat antimalaria secara in vitro dan in vivo, tetapi mekanisme kerjanya yang tepat belum dipahami. Penelitian ini bertujuan untuk menjelaskan mekanisme yang mendasari sifat antimalaria dari ANDRO terhadap parasit malaria hewan pengerat, Plasmodium berghei. Parasit diinjeksikan pada mencit BALB/c dan kemudian diberi perlakuan dengan ANDRO dan butionin sulfoksimin (BSO) sebagai kontrol pada konsentrasi berbeda secara ex vivo. Selanjutnya dilakukan pengukuran beberapa parameter status oksidatif, seperti konsentrasi GSH, rasio GSH/GSSG, rasio NADPH/NADP+, aktivitas spesifik dan ekspresi mRNA tioredoksin reduktase (TrxR), kadar malondialdehid (MDA) dan pertumbuhan parasit ex vivo. Pengaruh ANDRO terhadap detoksifikasi hem juga diukur secara in vitro ( cell-parasite free). Hasil menunjukkan bahwa ANDRO mendeplesi GSH tetapi meningkatkan rasio GSH/GSSG. Rasio NADPH/NADP+ dan aktivitas spesifik TrxR mengalami penurunan pada semua konsentrasi yang diuji tetapi ekspresi mRNA TrxR sedikit meningkat pada konsentrasi yang lebih rendah dan meningkat bermakna pada 60 M. ANDRO memperlihatkan efek yang berbeda terhadap pertahanan antioksidan parasit dibandingkan BSO dan peningkatan stres oksidatif tidak menyebabkan peningkatan kadar MDA. Andrografolida juga menghambat pertumbuhan parasit ex vivo dan mengganggu polimerisasi hem dengan IC50 367±171 M serta menghambat degradasi hem bergantung GSH, hambatan maksimal dihasilkan pada konsentrasi 15 g/mL. Kesimpulan, ANDRO menghasilkan aktivitas antimalaria dengan mengganggu sistem pertahanan antioksidan parasit yang dibuktikan dengan penurunan konsentrasi GSH dan aktivitas enzim TrxR. ANDRO memiliki potensi untuk dikembangkan menjadi antimalaria baru baik sebagai obat tunggal atau dalam kombinasi dengan obat antimalaria lainnya.

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The rapid emergence of parasite resistance to currently available antimalarial drugs has re-newed interest on drug discovery. Andrographolides, a compound isolated from the medicinal plant, Andrographis panniculata, Nees, exhibited antimalarial properties in vitro and in vivo but its precise mechanism of action remains elusive. The present study aims to elucidate the mechanism (s) underlying the antimalarial property of the andrographolides in the rodent malarial parasite, Plasmodium berghei. The parasite was initially propagated in BALB/c mice and subsequently be propagated ex vivo in the presence of different concentrations of andrographolide and buthionin sulphoximine (BSO) as control. Several parameters of the oxidative status, such as GSH concentration, GSH/GSSG ratio, NADPH/NADP+ ratio, specific activity and mRNA expression of thioredoxin reductase (TrxR), malondialdehyde (MDA) level and the parasite growth ex vivo were measured. Effect of the andrographolide on heme polymerization and GSH-dependent heme degradation were also tested using cell-free assay system.

The results indicated that the andrographolide depleted the GSH but increased the GSH/GSSG ratio. The NADPH/NADP+ ratio and the specific activity of the TrxR were decreased at all tested concentrations but expression of TrxR mRNA slightly increased at lower concentrations and increased significantly at 60 M. Andrographolide exerted a different effect on the antioxidant defense of the parasite than that BSO and increase in oxidative stress did not result in the increase of the MDA level. Andrographolide also inhibited the parasite growth ex vivo and interfered with the heme polymerization with IC50 of 367±171 M and GSH-dependent heme degradation with maximum concentration of 15 g/mL. In conclusion, andrographolide exerted its antimalarial properties through interference with the parasite oxidant defense system as evidenced by GSH depletion and decrease thioredoxin reductase enzyme activity. Andrographolide is potentially developed into a novel antimalaria either as a single prescription or in combination with other antimalarial drug."

"It has been conducted the synthesis of 3-(2-hydroxyethyl)-2-methyl-1,10-phenanthroline-4-ol was carried out from 8-aminoquinoline which are expected to posses antimalarial activity. ...."

"ABSTRAKTelah dilakukan penelitian mengenai variasi morfologi organ vegetatiftanaman bidara upas (Merremia mammosa) yang dikumpulkan di daerah jawaserta aktivitasnya sebagai anti-plasmodium secara in-vitro. Penelitian bertujuanuntuk memperoleh informasi karakter morfologi organ vegetatif tanaman bidaraupas dan aktivitas anti-plasmodium secara in-vitro. Tahapan penelitian meliputipengambilan sampel di lapangan, pengamatan morfologi secara visual, ekstraksi,skrining fitokimia, uji aktivitas antimalaria ssecara in-vitro. Hasil penelitianmenunjukkan sembilan sampel tanaman yang diamati membentuk dua kelompokutama yaitu kelompok PKL, HAJ dan Purwakarta serta kelompok JJ, HAA,Balittro, KRP, NL dan KRB. Dua kelompok utama dapat dibedakan berdasarkankarakter permukaan daun lebih agak kasar (HAJ) atau lebih licin mengkilat(Purwaka), bentuk umbi, warna pangkal umbi,warna permukaan umbi, banyaknyaserat umbi, warna daging umbi setelah kering, kulit umbi, getah umbi dan warnaakar umbi. Hasil skrining fitokimia kesembilan sampel umbi tanaman bidara upas(Merremia mammosa) menunjukkan bahwa kesembilan umbi tanaman bidaraupas memiliki kandungan senyawa aktif yang sama yaitu mengandung senyawaflavonoid, saponin dan terpenoid. Sehingga secara fitokimia, dari kesembilansampel esktrak n-heksan umbi bidara upas, diambil satu sampel yaitu sampelekstrak n-heksan dari Juragan Jamu (JJ) dari Sleman Jogyakartau ntuk diujiaktivitas anti-plasmodium. Hasil uji aktivitas anti-plasmodium menunjukkanbahwa ekstrak n-heksan umbi bidara upas bersifat anti-plasmodium dengan nilaiIC50 3,36, sehingga umbi bidara upas memiliki aktivitas kuat sebagai antiplasmodiumsecara in-vitro.

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ABSTRACTMorphological Variation study on plant vegetative organs of bidara upas(Merremia mammosa) collected in the area of Java and its activities antiplasmodiumas in-vitro. The aim of the study is to obtaining information onmorphological characters of vegetative organs of plants bidara upas collected inthe area Java and anti-plasmodium activity in vitro. The study include fieldsampling, visual morphological observation, extraction, phytochemical screening,and testing antimalarial activity in-vitro. The results showed whole plant sampleswere observed to form two main groups, namely the first group of PKL, HAJ andPurwakarta and a second group consisting of JJ, HAA, Balittro, KRP, NL andKRB. The two main groups can be distinguished by the character form bulbs,tubers base color, the color of the surface of the bulb, the amount fiber of bulb,such as tuber flesh color after drying, tubers, bulbs and color sap tuber. The resultsof nine samples of phytochemical screening tubers of plants bidara upas(Merremia mammosa) showed that all nine plant bulbs bidara upas containsflavonoids, saponins and terpenoids. So that phytochemicals, of the nine samplesof n-hexane extract the tubers bidara upas, was taken one sample of n-hexaneextracts of Juragan Jamu (JJ) from Yogyakarta's Sleman was tested antiplasmodiumactivity. Anti-plasmodium activity test results showed that n-hexaneextract the tubers are bidara upas anti-plasmodium with IC50 values of 3.36, so thebulbs bidara upas have strong activity as anti-plasmodium in vitro"

"Suatu metode sintesis yang unik telah digunakan dalam membuat senyawa turunan 2-(4-metoksifenil)-4-fenil-1,10-fenantrolin (5) dari 4-metoksibenzaldehida (1), asetofenon (2), dan 8-aminokuinolin (4)dengan reaksi kondensasi aldol dan reaksi siklisasi. Turunan-turunan senyawa tersebut diuji aktivitasnya melalui uji aktivitas antiplasmodial. Sintesis turunan senyawa 5 dilakukan dalam tiga tahap. Senyawa 3-(4-metoksifenil)-1-fenilpropenon3 disintesis melalui reaksi kondensasi aldol dari senyawa1 dan 2 dengan hasil 96,42%. Senyawa 5 disintesis melalui siklisasi senyawa 4 dan 3 dengan hasil 84,55%. Turunan senyawa 5 disintesis dari senyawa 5 menggunakan DMS dan DES yang direfluksberturut-turut selama 21 dan 22 jam untuk menghasilkan (1)-N-metil-9-(4-metoksifenil)-7-fenil-1,10-fenantrolinium sulfat (6) dan (1)-N-etil-9-(4-metoksifenil)-7-fenil-1,10-fenantrolinium sulfat (7) dengan rendemen hasil berturut-turut 91,42 dan 86,36%. Hasil uji in vitro aktivitas antiplasmodium dari turunan senyawa 5 (senyawa 6 dan 7) terhadap P.falciparum resistan klorokuin strain FCR3 menunjukkan bahwa senyawa 7 mempunyai aktivitas antimalaria lebih tinggi dari senyawa 5 and 6. Sedangkan, hasil uji in vitro aktivitas antiplasmodium terhadap P. falciparum sensitif klorokuinstrain D10 menunjukkan bahwa senyawa6 mempunyai aktivitas antimalaria lebih tinggi dari senyawa 5 and 7.

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AbstractA unique of synthetic methods was employed to prepare 2-(4 methoxyphenyl)-4-phenyl-1,10-phenanthroline (5) derivatives from 4-methoxy-benzaldehyde (1), acetophenone (2), and 8-aminoquinoline (4)with aldol condensation and cyclization reactions. The derivatives were tested through antiplasmodial test. The synthesis of derivatives compound 5 was conducted in three steps. The 3-(4-methoxyphenyl)-1 penylpropenone 3 was synthesized through aldol condensation of 1 and 2 which has a yield of 96.42%. The compound 5 was synthesized through cyclization of compound 4 and 3 with 84.55% yield. The derivative of compound 5 was synthesized from compound 5 using DMS and DES reagents which refluxed for 21 and 22 h, to produce (1)-N-methyl-9-(4-methoxyphenyl)-7-phenyl-1,10-phenanthrolinium sulfate (6) and (1)-N-ethyl-9-(4-methoxyphenyl)-7-phenyl-1,10-phenanthrolinium sulfate (7) with 91.42 and 86.36% yields, respectively.Results of in vitrotesting of antiplasmodial activity of compound 5 derivatives(i.e., compound 6 and 7 ) against chloroquine-resistantP. falciparumFCR3 strain showed that compound 7had higherantimalarial activity than compounds 5 and 6 .Whereas, results of in vitrotesting against chloroquine-sensitive P.falciparumD10 strain showed that compound 6has higher antimalarial activity than compounds 5 and 7. "

"[Pada penelitian ini, telah diuji pengaruh pemberian kombinasi ekstrak sambiloto (Andrographis paniculata Nees) dan spirulina (Arthrosphira platensis Gomont) terhadap persen parasitemia, persen survival, jumlah eritrosit dan kadar hemoglobin serta persen apoptosis sel limpa pada mencit yang diinfeksi P. berghei. Penelitian ini dilakukan dengan rancangan acak lengkap menggunakan 75 ekor mencit strain Swiss Webster. Kelompok uji terdiri dari kelompok AP, AP+ES, AP+PS, CMC dan DHP. Seluruh mencit diinfeksi Plasmodium berghei pada hari ke 0. Ekstrak bahan uji diberikan 3 hari sebelum diinfeksi (H-3) dansetiap hari selama 28 hari setelah infeksi. Data parasitemia diambil pada hari ke-3,7,10,15,21 dan 28. Sedangkan data jumlah eritrosit dan kadar Hb diambil pada hari ke 3, 10 dan 21. Pengolahan data dilakukan dengan uji Anova satu arah yang dilanjutkan dengan uji post hoc. Hasil penelitian menunjukkan bahwa kombinasi powder spirulina dan ekstrak sambiloto (AP+PS) memberikan hasil yang berbeda bermakna dalam menekan persen parasitemia (p=0,02), meningkatkan jumlah eritrosit (p=0,03) dan kadar hemoglobin (p=0,01) pada puncak infeksi, dibanding kelompok yang diberi sambiloto saja (AP). Pemberian ekstrak sambiloto dan atau tanpa spirulina dapat menurunkan persen apoptosis sel limpa secara bermakna (AP p= 0,001; AP+ES p= 0,000; AP+PS p= 0,000) dibanding dengan kelompok CMC pada puncak infeksi.;Effect of a combination of extracts of sambiloto (Andrographis paniculata Nees)and spirulina (Arthrosphira platensis Gomont) had been investigated decrease the number of parasitemia, increase erythrocytes count, level of hemoglobin and apoptosis of spleen cell in P. berghei infected mice. This study was conducted by employing a complete random design using 75 Swiss Webster mice. The test group consisted of groups of AP, AP + ES, AP + PS, DHP and CMC. All mice were infected with P. berghei on day 0. Material test given 3 days prior to infection (D-3) and for 28 consecutives days orally after infection. Data of parasitemia, taken on D3, 10,15, 21 and 28 while erythrocytes count, and level of hemoglobin taken on D3,10 and 21. Data processed by one way Anova test followed by post hoc test. Results showed that the combination of extract ofsambiloto and spirulina powder (AP + PS) was significant in suppressing the number of parasitemia (p = 0.02), increase of erythrocytes (p = 0.03) and level of hemoglobin (p = 0.01) in the peak of infection, compared with the group given only sambiloto (AP). Combination of sambiloto extract and or without spirulina had been significant in decrease apoptosis of spleen cell, (AP p= 0,001; AP+ES p= 0,000; AP+PS p= 0,000) compared with group of CMC, Effect of a combination of extracts of sambiloto (Andrographis paniculata Nees)and spirulina (Arthrosphira platensis Gomont) had been investigated decrease thenumber of parasitemia, increase erythrocytes count, level of hemoglobin andapoptosis of spleen cell in P. berghei infected mice. This study was conducted byemploying a complete random design using 75 Swiss Webster mice. The testgroup consisted of groups of AP, AP + ES, AP + PS, DHP and CMC. All micewere infected with P. berghei on day 0. Material test given 3 days prior toinfection (D-3) and for 28 consecutives days orally after infection. Data ofparasitemia, taken on D3, 10,15, 21 and 28 while erythrocytes count, and level ofhemoglobin taken on D3,10 and 21. Data processed by one way Anova testfollowed by post hoc test. Results showed that the combination of extract ofsambiloto and spirulina powder (AP + PS) was significant in suppressing thenumber of parasitemia (p = 0.02), increase of erythrocytes (p = 0.03) and level ofhemoglobin (p = 0.01) in the peak of infection, compared with the group givenonly sambiloto (AP). Combination of sambiloto extract and or without spirulinahad been significant in decrease apoptosis of spleen cell, (AP p= 0,001; AP+ESp= 0,000; AP+PS p= 0,000) compared with group of CMC]"