BACKGROUND Coffee used in Indonesia reached 276 thousand tons in 2016 and will be predicted to in... more BACKGROUND Coffee used in Indonesia reached 276 thousand tons in 2016 and will be predicted to increase 8.22 percent to 370 thousand tons in the 2016-2021 period11. The abundant use of coffee produces a by-product, namely coffee skin waste (cascara). In Indonesia, coffee skin is used as animal feed and fertilizer 1. However, the use of cascara in medicinal raw materials and beverages has not been widely used, while cascara can be used as a functional tea useful as an antioxidant 2,3. Coffee skin by-products, namely cascara, have several benefits, namely, can ward off free radicals, with the ability of cascara to ward off free radicals so that cascara can potentially prevent the emergence of cancer cells. Cascara contains active compounds: caffeine 1.3%, chlorogenic acid 2.6%, and caffeic acid 1.6% 4,5. Caffeine compounds found in robusta coffee cascara in addition to having a positive effect, but caffeine also has negative effects if consumed in large quantities, including accelerating heart rate, stimulating the central nervous system, and blood vasodilation 6,7 , so that decaffeination is carried out so that there is a decrease in caffeine levels in robusta coffee cascara. MATERIALS AND METHODS Materials The materials used in this study were robusta coffee cascara derived from Bogor,
Robusta coffee from Malang Regency, East Java is one of the superior products of the largest coff... more Robusta coffee from Malang Regency, East Java is one of the superior products of the largest coffeeproducing region in Indonesia. The coffee has high antioxidants. The component that acts as an antioxidant is the tannin content, and these tannins are also anti-cancer. Using the UV-Vis spectrophotometry method the tannin content in Malang Robusta coffee beans is known and then to measure its ability as an anticancer in-vitro against breast cancer cells using MCF-7. The results showed that the tannin contained in Malang Robusta coffee bean extract was 2.81 % and inhibited MCF-7 at 400 µg/mL, it has potential as an anticancer with an inhibition value of 68.88 %. Therefore, the use of Robusta coffee from Malang at this concentration can be used as an anti-breast cancer agent.
Context: One approach to cancer therapy medication is exploring medicinal plants that contain one... more Context: One approach to cancer therapy medication is exploring medicinal plants that contain one or more compounds specifically targeting cancer cells with fewer side effects. Cascara from coffee fruit (Coffea canephora Pierre ex A.Froehner) is a waste rarely processed but has various chemical contents that can be used in medicine. Aims: To evaluate the in silico and in vitro activity of compounds isolated from ethanolic extract of C. canephora cascara against HeLa and MCF-7 breast cancer cells. Methods: Isolation of the compounds by radial chromatography and thin layer chromatography techniques, and the chemical structures were elucidated by infrared radiation, ultraviolet, nuclear magnetic resonance spectroscopy, and mass spectrometry. In silico study about the compounds binding with the receptor responsibility to cancer (caspases 3 and 9). In vitro study by examining the cytotoxicity of HeLa and MCF-7 cells of the isolated compounds from C. canephora. Results: Four known bioacti...
Tyrosinase is an enzyme that catalyzes melanin biosynthesis. Recently, it has become a popular ta... more Tyrosinase is an enzyme that catalyzes melanin biosynthesis. Recently, it has become a popular target for developing cosmetics as a skin lightening or skin whitening agent, an anti-aging agent, an anti-wrinkle agent, and other therapeutics for skin disorders. Based on the previous reports, many compounds have been developed and designed to be tyrosinase inhibitors, including ferulic acid and cinnamic acid derivatives. However, until now, the use of these compounds in commercial cosmetic products has been limited. It may be due to chemical instability, lipophilicity, and poor efficacy. In this review, we assessed research studies to discuss the structure-activity of ferulic acid and its derivatives, which can contribute to their better efficacy as anti-tyrosinases. Either ferulic acid as a single compound or its hybridization with other cinnamic acid derivatives proved beneficial in designing tyrosinase inhibitors as active functional groups. The structure-activity of the phenyl ring's substituent improved inhibitory effects on monophenolase activity, especially the halogen substituent. In addition, the alkyl chain length and other functional groups linked, such as amide and acetyl groups, could alter the inhibitory properties, including hydrophobicity, to produce a more stable complex ligand-receptor.
Asam salisilat memiliki aktivitas anti-inflamasi dan antioksidan, namun dapat menimbulkan efek sa... more Asam salisilat memiliki aktivitas anti-inflamasi dan antioksidan, namun dapat menimbulkan efek samping pada saluran cerna. Modifikasi gugus karboksilat senyawa tersebut menjadi turunan amida dapat menjadi solusi untuk mengatasi kekurangannya. Pada penelitian ini dilakukan sintesis senyawa analog salisilamida,2‐hidroksi‐N‐(piridin‐2‐il)benzamida (1) dan turunan basa Mannich-nya (2a-b). Berdasarkan uji aktivitas penghambatan denaturasi protein senyawa sintesis menunjukkan aktivitas antiinflamasi, dengan rentang nilai IC50 = 0.121-0.145 mM. Aktivitas tersebut lebih rendah dibandingkan piroksikam yang digunakan sebagai senyawa standar (IC50 = 0,0073 mM). Hasil penambatan molekuler menunjukkan bahwa rasio afinitas ikatan COX-2/COX-1 dan interaksi ligan semua senyawa hasil sintesis tidak selektif terhadap COX-2.
Tyrosinase is an enzyme that catalyzes melanin biosynthesis. Recently, it has become a popular ta... more Tyrosinase is an enzyme that catalyzes melanin biosynthesis. Recently, it has become a popular target for developing cosmetics as a skin lightening or skin whitening agent, an anti-aging agent, an anti-wrinkle agent, and other therapeutics for skin disorders. Based on the previous reports, many compounds have been developed and designed to be tyrosinase inhibitors, including ferulic acid and cinnamic acid derivatives. However, until now, the use of these compounds in commercial cosmetic products has been limited. It may be due to chemical instability, lipophilicity, and poor efficacy. In this review, we assessed research studies to discuss the structure-activity of ferulic acid and its derivatives, which can contribute to their better efficacy as anti-tyrosinases. Either ferulic acid as a single compound or its hybridization with other cinnamic acid derivatives proved beneficial in designing tyrosinase inhibitors as active functional groups. The structure-activity of the phenyl ring's substituent improved inhibitory effects on monophenolase activity, especially the halogen substituent. In addition, the alkyl chain length and other functional groups linked, such as amide and acetyl groups, could alter the inhibitory properties, including hydrophobicity, to produce a more stable complex ligand-receptor.
We prepared six novel curcumin indazole analogs and confirmed their structures by Fourier transfo... more We prepared six novel curcumin indazole analogs and confirmed their structures by Fourier transform infrared, nuclear magnetic resonance, and mass spectra. Subsequently, their cytotoxicity was tested using the Michigan Cancer Foundation (MCF-7) proliferation assay against the Michigan Cancer Foundation (MCF-7), HeLa, WiDr, and vero cell lines. This study found that the compounds we prepared were more active against WiDr than HeLa and MCF-7. The activity of 3b, 3c, 3d, and 5a against WiDr (colorectal carcinoma) cells was higher than curcumin and tamoxifen. Their selectivity index (SI) indicated that several synthesized compounds showed more selectivity (SI value > 2) than positive controls tamoxifen and doxorubicin (SI value < 2.00). Three compounds (3a, 3b, and 3c) showed high SI against WiDr cells (3.74, 5.27, and 4.39, respectively). Compound 3b produced the highest cytotoxic activity, especially against WiDr cells (IC 50 = 27.20 µM) with excellent selectivity (SI = 5.27). Therefore, the compound should be further developed as an anticancer agent for colorectal carcinoma.
Allantoin is a compound contained in comfrey leaves. This research aims to obtain optimal conditi... more Allantoin is a compound contained in comfrey leaves. This research aims to obtain optimal condition parameters of ionic liquid-ultrasound-assisted extraction (IL-UAE) comfrey leaves to attract allantoin compounds. Comfrey leaves are extracted with eight ionic liquids by ultrasound-assisted extraction (UAE) and screened for allantoin levels. The best ionic liquid from the screening results is optimized response surface methodology (RSM) with Box-Behnken design with three factors and three levels to determine the optimum extraction conditions for allantoin levels. Determination of levels is carried out with TLC densitometry. The results of the IL screening obtained [HMIM]Cl as the best IL in the evaluation of optimization of extraction parameters. The results of optimization of extraction condition parameters [HMIM]Cl obtained the highest allantoin levels on the sixth run of 306.396 μg / g of powder at the ratio of solvents to powders of 10 mL / g, concentrations [HMIM] Cl 1 mol / L ...
Comfrey (Symphytum officinale L.) contains rosmarinic acid which has different pharmacological ac... more Comfrey (Symphytum officinale L.) contains rosmarinic acid which has different pharmacological activities, such as antioxidant and anti-inflammatory activities. However, the medicinal use of comfrey is limited by the hepatotoxic effect of lycopsamine in comfrey, which overshadows the health benefits of rosmarinic acid. Natural deep eutectic solvents (NADES) have a wide range of extraction properties, that provides a new approach to the detoxification of comfrey. In the present study, betaine-based and choline chloride-based NADES were screened for selective extraction of rosmarinic acid over lycopsamine. Ultrasonication was used in conjunction with NADES extraction. The chemical profile of the NADES extracts on antioxidant, anti-inflammatory and hepatotoxic activities were investigated using some chemical reagents. Betaine-urea (1:2 molar ratio, 50% water) obtained the highest content of rosmarinic acid and a low level of lycopsamine (1.934 and 0.018 mg/g, respectively). Betaine-ure...
As the food and beverages industry grows in Indonesia, there also has been an increase in the sof... more As the food and beverages industry grows in Indonesia, there also has been an increase in the soft-drinks production in the society. There are elements often added into the drinks; such as caffeine, artifical sweetener and preservatives,which the content should be monitored. Because, if they are over-used, they will be hazardous to health. The purpose of this research is to obtain the optimum analysis condition for determining the content of saccharin, aspartame, benzoic acid, sorbic acid and caffeine, which are in the soft-drinks, using the reversed phase High-Performance-Liquid-Chromatography (HPLC). In this study, the condition used are Latek 18 column (15 cm x 4.0 mm), mobile phase as a mixture of acetonitrile and acetat buffer pH 5(5:95), flow rate 1,0 ml/minutes and detected by a 254 nm length-wave. The detection limit discovered by this method are for saccharin, benzoic acid, sorbic acid, caffeine and aspartame, respectively, are 0,2 ppm; 0,2 ppm; 0,007 ppm; 0,142 ppm; and 6,5 ppm. Whereas, the quantitative limit for saccharin, benzoic acid, sorbic acid, caffeine and aspartame, respectively, are 0,689 ppm; 0,852 ppm; 0,027 ppm; 0,452 ppm; 25,2 ppm. The calibration curve ranged between 1-60 ppm for saccharin and benzoid acid, 1-40 ppm for caffeine, 0.05-2 ppm for sorbic acid, and 30-100 ppm for aspartame. The investigation has been done for five (5) brands od soft-drinks. The analysis results are sample A contains caffeine 96,66 ppm, sample B
New decahydroacridine-1,8-dione derivatives have been synthesized from 3-aminocyclohex-2-en-1-one... more New decahydroacridine-1,8-dione derivatives have been synthesized from 3-aminocyclohex-2-en-1-one. The compounds were characterized based on spectroscopic data and assessed their antioxidant and anti-inflammatory properties both in-vitro and in-silico. All the compounds exhibited poor in-vitro antioxidant activity but high in-vitro anti-inflammatory activity. An in-silico study using Autodock v 4.2 integrated LigandScout software 4.4.3. against the COX-1 (PBD ID: 1CQE) and COX-2 (PBD ID: 6COX) enzymes indicated that all the compounds could interact with both enzymes. Except for 3c against COX-1, the compounds’ interaction with both enzymes exhibited binding energy lower than diclofenac and curcumin. The results confirm that the compounds have a high potential to be antiinflammatory agents and deserve further development.
HIV-1 (Human immunodeficiency virus type 1) is a member of retrovirus family that could infect hu... more HIV-1 (Human immunodeficiency virus type 1) is a member of retrovirus family that could infect human and causing AIDS disease. AIDS epidemic is one of most destructive diseases in modern era. There were more than 33 million people infected by HIV until 2010. Various studies have been widely employed to design drugs that target the essential enzymes of HIV-1 that is, reverse transcriptase, protease and integrase. In this study, in silico virtual screening approach is used to find lead molecules from the library or database of natural compounds as HIV-1 reverse transcriptase inhibitor. Virtual screening against Indonesian Herbal Database using AutoDock4 performed on HIV-1 reverse transcriptase. From the virtual screening, top ten compounds were mulberrin, plucheoside A, vitexilactone, brucine N-oxide, cyanidin 3-arabinoside, alpha-mangostin, guaijaverin, erycristagallin, morusin and sanggenol N.
International Journal of Pharmacy and Pharmaceutical Sciences, 2016
Objective: This present study was intended to design sustained release tablet containing diclofen... more Objective: This present study was intended to design sustained release tablet containing diclofenac sodium using a matrix of excipient co-processed xanthan gum-crosslinked amylose. Methods: In the previous study, xanthan gum and amylose have been physically and chemically modified by the co-processed and crosslinking method, resulting co-processed excipient xanthan gum-crosslinked amylose are Co-CLA6-XG and Co-CLA12-XG (method A); CL6-Co-A-XG and CL12-Co-A-XG (method B) with each ratio 1:1, 1:2 and 2:1. All excipients had a good swelling index, high viscosity and good gel strength, good characteristics to be used as a matrix for sustained release tablet dosage form. In this study, a tablet with excipient Co-CLA6-XG, Co-CLA12-XG, CL6-Co-A-XG and CL12-Co-A-XG were formulated by direct compression method. The prepared formulations were evaluated for weight variation, thickness, and diameter, hardness, friability, drug content estimation, swelling index, in vitro drug release are within...
We synthesized five new Mannich bases compounds from vanillic acid and evaluated for their antiox... more We synthesized five new Mannich bases compounds from vanillic acid and evaluated for their antioxidant activities using a free-radical DPPH and FRAP methods. The compounds' structures were confirmed based on infrared, proton NMR, carbon NMR, and mass spectra. In this study, the compound 5-(pyrrolidin-1-ylmethyl)vanillic acid (2e) showed the best free-radical scavenger activity, while compound 2-[(diethylamino)methyl]vanillic acid (2c) showed the best as a ferric reductant. Mannich bases enhanced the free-radical scavenger activity but decreasing the ferric reduction potential of the parent compounds. The compounds were found to be moderate antioxidant agents.
Asian Journal of Pharmaceutical and Clinical Research, Oct 1, 2017
Objective: Malaria is a disease that impacts millions of people annually. Among the enzymes, plas... more Objective: Malaria is a disease that impacts millions of people annually. Among the enzymes, plasmepsin is the main enzyme in the plasmodium life cycle that degrades hemoglobin during the erythrocytic phase in the food vacuole. Recently, pharmaceutical industries have been trying to develop therapeutic agents that can cure malaria through the discovery of new plasmepsin inhibitor compounds. One of the developing approaches is the in silico method. Methods: The chosen in silico screening method in this experiment is a structure-based screening using GOLD software and the Indonesian medicinal plants database. Results: From ten in silico screening runs, three of the compounds always ranked in the top ten. These three compounds are trimyristin, cyanidin 3,5-di-(6-malonylglucoside), and isoscutellarein 4'-methyl ether 8-(6"-n-butylglucuronide). Another compound that emerged with high frequency is cyanidin 3,5-di-(6-malonylglucoside). Conclusions: Based on the results obtained from this screening, 11 inhibitor candidates 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)-5glucoside; 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 a GOLD score range from 78.4647 to 98.2836. Two of them, Asp34 and Asp214, bind with all residues in the catalytic site of plasmepsin.
Using heat-induced protein denaturation technique, a series of novel synthesized 1,5-diarylpyrazo... more Using heat-induced protein denaturation technique, a series of novel synthesized 1,5-diarylpyrazole compounds, namely 2-methoxy-4-(1-phenyl-3-methyl-1H-pyrazol-5-yl)phenol (1) and its aminomethyl derivatives (2a-e) were evaluated for their anti-inflammatory potentiality. The structures of the synthesized compounds were elucidated using FTIR, NMR (1H & 13C) and mass spectral data. The study found that the activity of aminomethyl derivatives (2a-e) was higher than that of parent compound 1. In this series, aminomethyl derivatives bearing dimethylamino-methyl, diethylaminomethyl and pyrrolidinomethyl moieties (2a, 2c and 2e, respectively) were more active than diclofenac sodium, which was used as a standard. A study on the structure-activity relationship (SAR) suggested that the activity of aminomethyl moiety of the compound was influenced by its pKa value. Thus, novel compounds act as potential anti-inflammatory agents.
BACKGROUND Coffee used in Indonesia reached 276 thousand tons in 2016 and will be predicted to in... more BACKGROUND Coffee used in Indonesia reached 276 thousand tons in 2016 and will be predicted to increase 8.22 percent to 370 thousand tons in the 2016-2021 period11. The abundant use of coffee produces a by-product, namely coffee skin waste (cascara). In Indonesia, coffee skin is used as animal feed and fertilizer 1. However, the use of cascara in medicinal raw materials and beverages has not been widely used, while cascara can be used as a functional tea useful as an antioxidant 2,3. Coffee skin by-products, namely cascara, have several benefits, namely, can ward off free radicals, with the ability of cascara to ward off free radicals so that cascara can potentially prevent the emergence of cancer cells. Cascara contains active compounds: caffeine 1.3%, chlorogenic acid 2.6%, and caffeic acid 1.6% 4,5. Caffeine compounds found in robusta coffee cascara in addition to having a positive effect, but caffeine also has negative effects if consumed in large quantities, including accelerating heart rate, stimulating the central nervous system, and blood vasodilation 6,7 , so that decaffeination is carried out so that there is a decrease in caffeine levels in robusta coffee cascara. MATERIALS AND METHODS Materials The materials used in this study were robusta coffee cascara derived from Bogor,
Robusta coffee from Malang Regency, East Java is one of the superior products of the largest coff... more Robusta coffee from Malang Regency, East Java is one of the superior products of the largest coffeeproducing region in Indonesia. The coffee has high antioxidants. The component that acts as an antioxidant is the tannin content, and these tannins are also anti-cancer. Using the UV-Vis spectrophotometry method the tannin content in Malang Robusta coffee beans is known and then to measure its ability as an anticancer in-vitro against breast cancer cells using MCF-7. The results showed that the tannin contained in Malang Robusta coffee bean extract was 2.81 % and inhibited MCF-7 at 400 µg/mL, it has potential as an anticancer with an inhibition value of 68.88 %. Therefore, the use of Robusta coffee from Malang at this concentration can be used as an anti-breast cancer agent.
Context: One approach to cancer therapy medication is exploring medicinal plants that contain one... more Context: One approach to cancer therapy medication is exploring medicinal plants that contain one or more compounds specifically targeting cancer cells with fewer side effects. Cascara from coffee fruit (Coffea canephora Pierre ex A.Froehner) is a waste rarely processed but has various chemical contents that can be used in medicine. Aims: To evaluate the in silico and in vitro activity of compounds isolated from ethanolic extract of C. canephora cascara against HeLa and MCF-7 breast cancer cells. Methods: Isolation of the compounds by radial chromatography and thin layer chromatography techniques, and the chemical structures were elucidated by infrared radiation, ultraviolet, nuclear magnetic resonance spectroscopy, and mass spectrometry. In silico study about the compounds binding with the receptor responsibility to cancer (caspases 3 and 9). In vitro study by examining the cytotoxicity of HeLa and MCF-7 cells of the isolated compounds from C. canephora. Results: Four known bioacti...
Tyrosinase is an enzyme that catalyzes melanin biosynthesis. Recently, it has become a popular ta... more Tyrosinase is an enzyme that catalyzes melanin biosynthesis. Recently, it has become a popular target for developing cosmetics as a skin lightening or skin whitening agent, an anti-aging agent, an anti-wrinkle agent, and other therapeutics for skin disorders. Based on the previous reports, many compounds have been developed and designed to be tyrosinase inhibitors, including ferulic acid and cinnamic acid derivatives. However, until now, the use of these compounds in commercial cosmetic products has been limited. It may be due to chemical instability, lipophilicity, and poor efficacy. In this review, we assessed research studies to discuss the structure-activity of ferulic acid and its derivatives, which can contribute to their better efficacy as anti-tyrosinases. Either ferulic acid as a single compound or its hybridization with other cinnamic acid derivatives proved beneficial in designing tyrosinase inhibitors as active functional groups. The structure-activity of the phenyl ring&#39;s substituent improved inhibitory effects on monophenolase activity, especially the halogen substituent. In addition, the alkyl chain length and other functional groups linked, such as amide and acetyl groups, could alter the inhibitory properties, including hydrophobicity, to produce a more stable complex ligand-receptor.
Asam salisilat memiliki aktivitas anti-inflamasi dan antioksidan, namun dapat menimbulkan efek sa... more Asam salisilat memiliki aktivitas anti-inflamasi dan antioksidan, namun dapat menimbulkan efek samping pada saluran cerna. Modifikasi gugus karboksilat senyawa tersebut menjadi turunan amida dapat menjadi solusi untuk mengatasi kekurangannya. Pada penelitian ini dilakukan sintesis senyawa analog salisilamida,2‐hidroksi‐N‐(piridin‐2‐il)benzamida (1) dan turunan basa Mannich-nya (2a-b). Berdasarkan uji aktivitas penghambatan denaturasi protein senyawa sintesis menunjukkan aktivitas antiinflamasi, dengan rentang nilai IC50 = 0.121-0.145 mM. Aktivitas tersebut lebih rendah dibandingkan piroksikam yang digunakan sebagai senyawa standar (IC50 = 0,0073 mM). Hasil penambatan molekuler menunjukkan bahwa rasio afinitas ikatan COX-2/COX-1 dan interaksi ligan semua senyawa hasil sintesis tidak selektif terhadap COX-2.
Tyrosinase is an enzyme that catalyzes melanin biosynthesis. Recently, it has become a popular ta... more Tyrosinase is an enzyme that catalyzes melanin biosynthesis. Recently, it has become a popular target for developing cosmetics as a skin lightening or skin whitening agent, an anti-aging agent, an anti-wrinkle agent, and other therapeutics for skin disorders. Based on the previous reports, many compounds have been developed and designed to be tyrosinase inhibitors, including ferulic acid and cinnamic acid derivatives. However, until now, the use of these compounds in commercial cosmetic products has been limited. It may be due to chemical instability, lipophilicity, and poor efficacy. In this review, we assessed research studies to discuss the structure-activity of ferulic acid and its derivatives, which can contribute to their better efficacy as anti-tyrosinases. Either ferulic acid as a single compound or its hybridization with other cinnamic acid derivatives proved beneficial in designing tyrosinase inhibitors as active functional groups. The structure-activity of the phenyl ring's substituent improved inhibitory effects on monophenolase activity, especially the halogen substituent. In addition, the alkyl chain length and other functional groups linked, such as amide and acetyl groups, could alter the inhibitory properties, including hydrophobicity, to produce a more stable complex ligand-receptor.
We prepared six novel curcumin indazole analogs and confirmed their structures by Fourier transfo... more We prepared six novel curcumin indazole analogs and confirmed their structures by Fourier transform infrared, nuclear magnetic resonance, and mass spectra. Subsequently, their cytotoxicity was tested using the Michigan Cancer Foundation (MCF-7) proliferation assay against the Michigan Cancer Foundation (MCF-7), HeLa, WiDr, and vero cell lines. This study found that the compounds we prepared were more active against WiDr than HeLa and MCF-7. The activity of 3b, 3c, 3d, and 5a against WiDr (colorectal carcinoma) cells was higher than curcumin and tamoxifen. Their selectivity index (SI) indicated that several synthesized compounds showed more selectivity (SI value > 2) than positive controls tamoxifen and doxorubicin (SI value < 2.00). Three compounds (3a, 3b, and 3c) showed high SI against WiDr cells (3.74, 5.27, and 4.39, respectively). Compound 3b produced the highest cytotoxic activity, especially against WiDr cells (IC 50 = 27.20 µM) with excellent selectivity (SI = 5.27). Therefore, the compound should be further developed as an anticancer agent for colorectal carcinoma.
Allantoin is a compound contained in comfrey leaves. This research aims to obtain optimal conditi... more Allantoin is a compound contained in comfrey leaves. This research aims to obtain optimal condition parameters of ionic liquid-ultrasound-assisted extraction (IL-UAE) comfrey leaves to attract allantoin compounds. Comfrey leaves are extracted with eight ionic liquids by ultrasound-assisted extraction (UAE) and screened for allantoin levels. The best ionic liquid from the screening results is optimized response surface methodology (RSM) with Box-Behnken design with three factors and three levels to determine the optimum extraction conditions for allantoin levels. Determination of levels is carried out with TLC densitometry. The results of the IL screening obtained [HMIM]Cl as the best IL in the evaluation of optimization of extraction parameters. The results of optimization of extraction condition parameters [HMIM]Cl obtained the highest allantoin levels on the sixth run of 306.396 μg / g of powder at the ratio of solvents to powders of 10 mL / g, concentrations [HMIM] Cl 1 mol / L ...
Comfrey (Symphytum officinale L.) contains rosmarinic acid which has different pharmacological ac... more Comfrey (Symphytum officinale L.) contains rosmarinic acid which has different pharmacological activities, such as antioxidant and anti-inflammatory activities. However, the medicinal use of comfrey is limited by the hepatotoxic effect of lycopsamine in comfrey, which overshadows the health benefits of rosmarinic acid. Natural deep eutectic solvents (NADES) have a wide range of extraction properties, that provides a new approach to the detoxification of comfrey. In the present study, betaine-based and choline chloride-based NADES were screened for selective extraction of rosmarinic acid over lycopsamine. Ultrasonication was used in conjunction with NADES extraction. The chemical profile of the NADES extracts on antioxidant, anti-inflammatory and hepatotoxic activities were investigated using some chemical reagents. Betaine-urea (1:2 molar ratio, 50% water) obtained the highest content of rosmarinic acid and a low level of lycopsamine (1.934 and 0.018 mg/g, respectively). Betaine-ure...
As the food and beverages industry grows in Indonesia, there also has been an increase in the sof... more As the food and beverages industry grows in Indonesia, there also has been an increase in the soft-drinks production in the society. There are elements often added into the drinks; such as caffeine, artifical sweetener and preservatives,which the content should be monitored. Because, if they are over-used, they will be hazardous to health. The purpose of this research is to obtain the optimum analysis condition for determining the content of saccharin, aspartame, benzoic acid, sorbic acid and caffeine, which are in the soft-drinks, using the reversed phase High-Performance-Liquid-Chromatography (HPLC). In this study, the condition used are Latek 18 column (15 cm x 4.0 mm), mobile phase as a mixture of acetonitrile and acetat buffer pH 5(5:95), flow rate 1,0 ml/minutes and detected by a 254 nm length-wave. The detection limit discovered by this method are for saccharin, benzoic acid, sorbic acid, caffeine and aspartame, respectively, are 0,2 ppm; 0,2 ppm; 0,007 ppm; 0,142 ppm; and 6,5 ppm. Whereas, the quantitative limit for saccharin, benzoic acid, sorbic acid, caffeine and aspartame, respectively, are 0,689 ppm; 0,852 ppm; 0,027 ppm; 0,452 ppm; 25,2 ppm. The calibration curve ranged between 1-60 ppm for saccharin and benzoid acid, 1-40 ppm for caffeine, 0.05-2 ppm for sorbic acid, and 30-100 ppm for aspartame. The investigation has been done for five (5) brands od soft-drinks. The analysis results are sample A contains caffeine 96,66 ppm, sample B
New decahydroacridine-1,8-dione derivatives have been synthesized from 3-aminocyclohex-2-en-1-one... more New decahydroacridine-1,8-dione derivatives have been synthesized from 3-aminocyclohex-2-en-1-one. The compounds were characterized based on spectroscopic data and assessed their antioxidant and anti-inflammatory properties both in-vitro and in-silico. All the compounds exhibited poor in-vitro antioxidant activity but high in-vitro anti-inflammatory activity. An in-silico study using Autodock v 4.2 integrated LigandScout software 4.4.3. against the COX-1 (PBD ID: 1CQE) and COX-2 (PBD ID: 6COX) enzymes indicated that all the compounds could interact with both enzymes. Except for 3c against COX-1, the compounds’ interaction with both enzymes exhibited binding energy lower than diclofenac and curcumin. The results confirm that the compounds have a high potential to be antiinflammatory agents and deserve further development.
HIV-1 (Human immunodeficiency virus type 1) is a member of retrovirus family that could infect hu... more HIV-1 (Human immunodeficiency virus type 1) is a member of retrovirus family that could infect human and causing AIDS disease. AIDS epidemic is one of most destructive diseases in modern era. There were more than 33 million people infected by HIV until 2010. Various studies have been widely employed to design drugs that target the essential enzymes of HIV-1 that is, reverse transcriptase, protease and integrase. In this study, in silico virtual screening approach is used to find lead molecules from the library or database of natural compounds as HIV-1 reverse transcriptase inhibitor. Virtual screening against Indonesian Herbal Database using AutoDock4 performed on HIV-1 reverse transcriptase. From the virtual screening, top ten compounds were mulberrin, plucheoside A, vitexilactone, brucine N-oxide, cyanidin 3-arabinoside, alpha-mangostin, guaijaverin, erycristagallin, morusin and sanggenol N.
International Journal of Pharmacy and Pharmaceutical Sciences, 2016
Objective: This present study was intended to design sustained release tablet containing diclofen... more Objective: This present study was intended to design sustained release tablet containing diclofenac sodium using a matrix of excipient co-processed xanthan gum-crosslinked amylose. Methods: In the previous study, xanthan gum and amylose have been physically and chemically modified by the co-processed and crosslinking method, resulting co-processed excipient xanthan gum-crosslinked amylose are Co-CLA6-XG and Co-CLA12-XG (method A); CL6-Co-A-XG and CL12-Co-A-XG (method B) with each ratio 1:1, 1:2 and 2:1. All excipients had a good swelling index, high viscosity and good gel strength, good characteristics to be used as a matrix for sustained release tablet dosage form. In this study, a tablet with excipient Co-CLA6-XG, Co-CLA12-XG, CL6-Co-A-XG and CL12-Co-A-XG were formulated by direct compression method. The prepared formulations were evaluated for weight variation, thickness, and diameter, hardness, friability, drug content estimation, swelling index, in vitro drug release are within...
We synthesized five new Mannich bases compounds from vanillic acid and evaluated for their antiox... more We synthesized five new Mannich bases compounds from vanillic acid and evaluated for their antioxidant activities using a free-radical DPPH and FRAP methods. The compounds' structures were confirmed based on infrared, proton NMR, carbon NMR, and mass spectra. In this study, the compound 5-(pyrrolidin-1-ylmethyl)vanillic acid (2e) showed the best free-radical scavenger activity, while compound 2-[(diethylamino)methyl]vanillic acid (2c) showed the best as a ferric reductant. Mannich bases enhanced the free-radical scavenger activity but decreasing the ferric reduction potential of the parent compounds. The compounds were found to be moderate antioxidant agents.
Asian Journal of Pharmaceutical and Clinical Research, Oct 1, 2017
Objective: Malaria is a disease that impacts millions of people annually. Among the enzymes, plas... more Objective: Malaria is a disease that impacts millions of people annually. Among the enzymes, plasmepsin is the main enzyme in the plasmodium life cycle that degrades hemoglobin during the erythrocytic phase in the food vacuole. Recently, pharmaceutical industries have been trying to develop therapeutic agents that can cure malaria through the discovery of new plasmepsin inhibitor compounds. One of the developing approaches is the in silico method. Methods: The chosen in silico screening method in this experiment is a structure-based screening using GOLD software and the Indonesian medicinal plants database. Results: From ten in silico screening runs, three of the compounds always ranked in the top ten. These three compounds are trimyristin, cyanidin 3,5-di-(6-malonylglucoside), and isoscutellarein 4'-methyl ether 8-(6"-n-butylglucuronide). Another compound that emerged with high frequency is cyanidin 3,5-di-(6-malonylglucoside). Conclusions: Based on the results obtained from this screening, 11 inhibitor candidates 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)-5glucoside; 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 a GOLD score range from 78.4647 to 98.2836. Two of them, Asp34 and Asp214, bind with all residues in the catalytic site of plasmepsin.
Using heat-induced protein denaturation technique, a series of novel synthesized 1,5-diarylpyrazo... more Using heat-induced protein denaturation technique, a series of novel synthesized 1,5-diarylpyrazole compounds, namely 2-methoxy-4-(1-phenyl-3-methyl-1H-pyrazol-5-yl)phenol (1) and its aminomethyl derivatives (2a-e) were evaluated for their anti-inflammatory potentiality. The structures of the synthesized compounds were elucidated using FTIR, NMR (1H & 13C) and mass spectral data. The study found that the activity of aminomethyl derivatives (2a-e) was higher than that of parent compound 1. In this series, aminomethyl derivatives bearing dimethylamino-methyl, diethylaminomethyl and pyrrolidinomethyl moieties (2a, 2c and 2e, respectively) were more active than diclofenac sodium, which was used as a standard. A study on the structure-activity relationship (SAR) suggested that the activity of aminomethyl moiety of the compound was influenced by its pKa value. Thus, novel compounds act as potential anti-inflammatory agents.
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Papers by Hayun Hayun