Safety Evaluation of the Ethyl Acetate Extract on Irradiated Tea Parasite: Acute Toxicity Study on Mice

Many studies of the pharmacological efficacy of tea parasite and the use of ionizing radiation for decontamination of microbes and extending shelf life have been reported, but there is no information on its safety, such as the acute toxicity. In this study, the acute toxicity of two ethyl acetate extracts from unirradiated and irradiated (irradiation dose of 10 kGy) tea parasites Scurrula atropurpurea on Swiss Webster mice have been examined. The observation was done after the treatment of a single oral dose of ethyl acetate extract in various dose groups, i.e.: control (0 g/kg of mice body weight), D1 (0.625 g/kg), D2 (1.25 g/kg), D3 (2.5 g/kg) D4 (5 g/kg), D5 (10 g/kg) by observing the effect on behavioral response (pharmacological profile), the body weight gains and mortality until the day 14 th . At the last day, the observation of vital organs has also been done. The result showed thatno acute toxicity was found in mice treated with a single oral dose of ethyl acetate extract from unirradiated tea parasite and irradiated tea parasite at the dose of 10 kGy. At the dose up to 10 g/kg (equivalent to 77.6 g of extract which administered to human), the normal body weight gains were observed in mice of all dose groups, no mice deaths in any of the dose groups, and no significant change (p > 0.05) in organ weights relative to the body weight i.e.: liver, spleen, kidneys, lung, heart, testes and seminal vesicle (for male), and ovaries and uterus (for female). The approximate lethal doses for male and female mice were determined to be higher than 10 g/kg of mice body weight. It is suggested that the treatment of ethyl acetate extract from unirradiated and irradiated tea parasites until dose up to 10 g/kg of mice body weight was stillsafe

RAPID ISOMERIZATION OF ALKYNOL BY POTASSIUM AMINOPROPYLAMIDE REAGENT

Terminal alkynol (w-alkynol) is an intermediate compound in synthesis of a potent anticancer agent, namely C-16 alkynic fatty acid. For synthesis of this intermediate compound, it is needed to synthesize the appropriate internal alkynol, namely 2-nonyn-1-ol (10), 2-undecyn-1-ol (11), and 2-heptyn-1-ol (12), subsequently to convert these internal alkynol into terminal alkynol, namely 8-nonyn-1-ol (7), 10-undecyn-1-ol (8), and 6-heptyn-1-ol (9), an isomerization reaction was needed. Based on the method which developed by ABRAMS by using potassium 3-aminopropylamide (KAPA) reagent, the isomerization reaction could be done within 5 minutes in 93-94% yield.   Keywords : Isomerization, KAPA reagent, alkynol

Safety Evaluation of the Ethyl Acetate Extract on Irradiated Tea Parasite: Acute Toxicity Study on Mice

Many studies of the pharmacological efficacy of tea parasite and the use of ionizing radiation for decontamination of microbes and extending shelf life have been reported, but there is no information on its safety, such as the acute toxicity. In this study, the acute toxicity of two ethyl acetate extracts from unirradiated and irradiated (irradiation dose of 10 kGy) tea parasites Scurrula atropurpurea on Swiss Webster mice have been examined. The observation was done after the treatment of a single oral dose of ethyl acetate extract in various dose groups, i.e.: control (0 g/kg of mice body weight), D1 (0.625 g/kg), D2 (1.25 g/kg), D3 (2.5 g/kg) D4 (5 g/kg), D5 (10 g/kg) by observing the effect on behavioral response (pharmacological profile), the body weight gains and mortality until the day 14 th . At the last day, the observation of vital organs has also been done. The result showed thatno acute toxicity was found in mice treated with a single oral dose of ethyl acetate extract from unirradiated tea parasite and irradiated tea parasite at the dose of 10 kGy. At the dose up to 10 g/kg (equivalent to 77.6 g of extract which administered to human), the normal body weight gains were observed in mice of all dose groups, no mice deaths in any of the dose groups, and no significant change (p > 0.05) in organ weights relative to the body weight i.e.: liver, spleen, kidneys, lung, heart, testes and seminal vesicle (for male), and ovaries and uterus (for female). The approximate lethal doses for male and female mice were determined to be higher than 10 g/kg of mice body weight. It is suggested that the treatment of ethyl acetate extract from unirradiated and irradiated tea parasites until dose up to 10 g/kg of mice body weight was stillsafe

The Effect of Gamma Irradiation on Ethanolic Extract of Temulawak (Curcuma xanthorrhiza Roxb.) Against Human Cancer Cell Lines

The Effect of Gamma Irradiation on Ethanolic Extract of Temulawak (Curcuma xanthorrhiza Roxb.) Against Human Cancer Cell Lines. One of the medicinal plants that are widely used by the people of Indonesia is temulawak (Curcuma xanthorrhiza Roxb.) with the active ingredient is curcuminoid. The curcuminoid is a yellow compound that is believed to have anti-cancer properties, therefore its properties must be maintained in the post-harvest process. This research aimed to study the effect of gamma irradiation on the simplicia of C. xanthorrhiza rhizomes in inhibiting the proliferative activity against human cancer cell lines. The dry powder of C. xanthorrhiza rhizome was irradiated with gamma at a dose of 10 kGy in 2 replications, then extracted using ethanol solvent, evaporated, to obtain an ethanol extract. As a control, an un-irradiated sample was prepared and extracted in the same manner. Each ethanol extract from irradiated and control samples was then tested for their antioxidant activity by DPPH method and antiproliferative activity against human cancer cell lines (HUT78, A549, HeLa, and THP1). The results showed that the ethanol extract of irradiated C. xanthorrhiza rhizome with a dose of 10 kGy still had antioxidant activity and anticancer properties based on the bioassay against four those human cancer cell lines, although the antiproliferative activity decreased between 8-30% compared to the control sample. The highest antiproliferative activity was shown by the ethanol extract against HUT78 cancer cell line with IC50 values of 5.4 and 10.7 µg/ml for control and irradiated samples respectively. Based on the silica gel TLC plate, the ethanolic extracts of C. xanthorrhiza rhizome both unirradiated- and irradiated samples contained curcumin (Rf = 0.58) and demethoxycurcumin (Rf = 0.38)

Cytotoxic Activity Against L1210 Leukemia Cells from the Ethyl Acetate Fraction of Kenikir Leaves (Cosmos. Caudatus) Preserved by Gamma Irradiation

Kenikir leaves (Cosmos caudatus) Has been used as traditional medicine, especially as an anti-cancer, this plant has been in Indonesia both in herbs and capsules. Microbial contamination of herbal medicinal raw materials occurs when the storage process is done. One of the preservation techniques used in the industry is using gamma irradiation techniques to reduce microbial and fungal contamination. The purpose of this research was to study the effect of gamma irradiation for the preservation of kenikir leaves (C. caudatus) as an anti-cancer based on cytotoxic activity using L1210 leukaemia cells. The simplicia was gamma-irradiated by Co-60 source with variation doses of 0 (control); 5; 7.5; 10; and 15 kGy. Then the irradiated and control samples were macerated successively using n-hexane, ethyl acetate, and ethanol. The active extract (ethyl acetate) was further fractionated using column chromatography, obtained seven fractions (F1 - F7). The seven fractions' cytotoxic activity against L1210 leukaemia cells showed that fraction 3 (F3) was the most active fraction with an IC50 of 1.26 µg/mL. Each dose's F3 cytotoxic activity showed that the IC50 7.5 kGy irradiation sample did not change significantly with control (0 kGy) based on ANOVA analysis using SPSS 24 with a 95% confidence level. In comparison, irradiation samples of 10 and 15 kGy showed a change in the IC50 value is significant with the control (0 kGy). These results indicate that gamma irradiation can be used as an alternative for preserving C. caudatus with a maximum dose of 7.5 kGy, so that its anti-cancer properties do not change with those without irradiation

Gamma Irradiation for Preservation of Suruhan Herbs (Peperomia pellucida L. Kunth.) and its Bioactivity Against L1210 Leukemia Cells

Peperomia pellucida includes the Piperaceae family that has anti-cancer, anti-inflammatory, antioxidant, and anti-microbial activities. Microbes easily contaminate dry herbs during storage, so special handling is needed. One of the preservation techniques is using irradiation technology. This technique can be used to extend the shelf life of herbal medicinal ingredients. This research aimed to study the effects of irradiation on the anti-cancer activity of P. pellucida leaves. P. pellucida leaves' dried powder was irradiated at doses of 5, 7.5, 10, and 15 kGy. The anti-cancer activity test was carried out against L1210 leukaemia cells. The un-irradiated irradiated samples were macerated successively with n-hexane, ethyl acetate, and ethanol, then be concentrated. The ethyl acetate extract was fractionated using silica gel column chromatography, obtained seven fractions. Their IC50 values < 20 mg/mL, with fraction F4 was the most active fraction (IC50 1.9 mg/mL). The result showed that gamma radiation at doses of 5 - 15 kGy reduced their cytotoxic activity significantly. However, the fractions were still in the active category as anti-cancer (IC50 values were < 20 mg/mL)

PENGGUNAAN [3H]-LEUSIN UNTUK MEMPELAJARI SENYAWA KOMPLEKS PERSEITOL·K+ YANG DIISOLASI DARI BENALU ALUS Scurrula fusca SEBAGAI INHIBITOR SINTESIS PROTEIN PADA SEL

Telah dilakukan pengujian aktivitas senyawa perseitol·K+ (2) yang diisolasi dari benalu alus Scurrula fusca (BL.) G. DON terhadap inhibisi sintesis protein oleh sel kanker Ehrlich ascites dari tikus. Pengujian dilakukan dengan menggunakan L-[3,4,5-3H(N)] leusin dan pengukuran dilakukan dengan pencacah sintilasi cair. Hasil percobaan menunjukkan bahwa senyawa isolat tersebut mnunjukkan aktivitas inhibisi sebesar 13% pada konsentrasi sampel 10-7 M. Aktivitas ini lebih tinggi dibandingkan senyawa perseitol (3) tanpa ion K+ yang hanya menunjukkan aktivitas inhibisi sebesar 5%. Keberadaan ion K+ dalam senyawa kompleksmerupakan faktor esensial dalam aktivitasnya sebagai inhibitor sintesis protein oleh sel kanker. Percobaan yang sama yang dilakukan terhadap berbagai komposisi campuran senyawa perseitol (3) dan ion K+ dengan perbandingan molar 24:1, 22:1, 20:1, dan 18:1 menunjukkan bahwa komposisi perseitol : K+ = 20:1 memberikan aktivitas inhibisi tertinggi terhadap sintesis protein yaitu 40% pada konsentrasi 10-4 M. Aktivitas inhibisi ini lebih tinggi dibandingkan cycloheximide sebagai kontrol positif (25% inhibisi pada 0.5×10-6 M). Hal ini diduga pada komposisi perbandingan molar tersebut, perseitol (3) dan ion K+ membentuk senyawa kompleks perseitol·K+ seperti isolat benalu alus. Selain pengaruh keberadaan ion K+, perbandingan molar 20:1 merupakan faktor yang sangat berperan dalam aktivitasnya sebagai inhibitor sintesis protein oleh sel kanke

Isolasi dan Identifi kasi Senyawa Kimia Zat Anti Kanker dari Daun Kopasanda (Chromolaena odorata (L.))

Isolation and identifi cation of chemical compound as anticancer from the leaves of Kopasanda (Chromolaena odorata L.) had been done. Extraction was conducted successfully with n-hexane, ethylacetate and ethanol by maceration, and by refl ux for water solvent. Fractionation of ethylacetate extract by column chromatography (SiO2). n-hexane-ethylacetate = 10:1 ~ 1:1; ethylacetate). n-hexaneethylacetate = 5:1) gave one pure isolated fraction fr. 5-3 with inhibition activity against leukemia cell line L1210 at concentration 1.515 ppm. Chemical structure determination was done based on spectral data interpretation of Infra Red, 1D NMR (1H, 13C) and 2D NMR (H-H COSY, HMQC and HMBC) and mass spectra (LC-MS). Pure isolated fraction fr. 5-3 was deducted as methyl ether naragenine.Isolasi dan identifi kasi senyawa kimia sebagai antikanker dari daun Kopasanda (Chromolaena odorata L.) telah dilakukan. Ekstraksi dilakukan secara berturut-turut dengan n-heksan, etilasetat, dan etanol secara maserasi kecuali dengan air dilakukan secara refl uks. Fraksinasi ekstrak etilasetat dengan kromatografi kolom (SiO2,: i). n-heksan-etilasetat = 10:1 ~ 1:1; etilasetat, ii). n-heksan-etilasetat = 5:1) memberikan satu isolat murni fr. 5-3 yang mempunyai aktivitas daya hambat terhadap sel leukemia L1210 sebesar 1,515 bpj. Penentuan struktur kimia dilakukan berdasarkan interpretasi data spektra infra merah, RMI 1D (1H, 13C) dan RMI 2D (H-H COSY, HMQC dan HMBC) dan spektra masa (LC-MS). Isolat fr. 5-3 diduga adalah metil eter naragenin

EFFECT OF GAMMA IRRADIATION ON PHYTOCHEMICAL CONTENT AND ANTICANCER ACTIVITIES OF ROSELLE (Hibiscus sabdariffa Linn)

Gamma irradiation is widely used in herbal medicine industries as an efficient preservative method in reducing microorganism contaminants. The aim of this study was to evaluate the effect of gamma irradiation at the doses of 5; 7.5; and 10 kGy on H. sabdariffa ethanolic extract (HS-EE). The Co-60 was used for irradiation the samples. The phytochemical content of HS-EE was carried out by total microorganism analysis using dilution method, TPC by Follin-Cicalteu method, TFC by aluminium chloride colorimetric method, antioxidant activity using DPPH method, TLC profiling on silica gel F254, in vitro anticancer activity using A-549, HUT-78, and MCF-7 cancer cell lines. The irradiation at 10 kGy caused the total bacteria decreased, while dose of 5 kGy could eliminate the total mold. Irradiation at 5 kGy caused TPC, TFC, and antioxidant activity decreased by 5-11%. TLC chromatograms analysis confirmed that one of the compounds contained in HS-EE was quercetin. The HS-EE has the strongest anticancer property against HUT-78 (IC50 10.51 µg/mL) followed by against MCF-7 (IC50 13.39 µg/mL), and A-549 (IC50 14.19 µg/mL). It can be concluded that irradiation at a dose of 10 kGy could remove total bacteria and molds, decreasing the phytochemical content and anticancer activities of HS-EE. It is recommended to increase the active ingredient level in the formulation

Radiation-Induced Degradation of Pirimiphos Methyl in Aerated Solution

Degradation of pirimiphos methyl (1) as an active ingredient in Minawet insecticide 250 EC formulation in aqueous solution was studied. The absorbance, pH, COD (Chemical Oxygen Demand) in aerated solution, and the analyses of degradation products at various irradiation doses with dose rate of 5 kGy/h were observed. The absorbance decreased rapidly at low doses (£ 10 kGy), while at high doses (> 10 kGy) decreased slowly. The optimum irradiation dose for pirimiphos methyl degradation in aerated solution was found to be 15 kGy at pH 3.6. At that condition, more than 99% of pirimiphos methyl has been degraded and the COD of solution decreased about 82%. The analysis of irradiated samples by GC-MS and HPLC showed that 2-diethylamino-6-methyl-4-oxo-3,4-dihydropyrimidine (3) and oxalic acid were clarified as degraded product