Publications by authors named "Fadlina Chany Saputri"

9 Publications

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Inhibition of pancreatic elastase and by leaves extract and its constituents.

J Pharm Bioallied Sci 2020 Jul-Sep;12(3):317-323. Epub 2020 Jul 18.

Department of Phytochemistry, Faculty of Pharmacy, Universitas Indonesia, Depok, Indonesia.

Objective: Elastases are protease enzymes, which mainly hydrolyze proteins of the connective tissue, so they have a significant impact on human disease. is one of the species found in Indonesian mountains, and it has potential as an elastase inhibitor. The objective of this research was to examine the elastase inhibitor activity of leaves and to dock different ligands of its constituents against target protein of Porcine Pancreatic Elastase (PPE) receptor.

Method: Dried leaves powder of was extracted using Soxhlet apparatus with -hexane, ethyl acetate, and methanol. The extract was evaporated, and elastase inhibitor activity was determined using PPE with the quercetin used as control positive. Selected nine constituents of were evaluated on the docking behavior of elastase receptor using Protein-Ligand ANT System (PLANTS) computational software with PPE enzyme with Protein Data Bank (PDB) file 1BRU.

Result: The methanol extract showed significantly inhibited elastase with IC50 186.13 μg/mL, but ethyl acetate extract showed weak activity, and -hexane extract did not show any activity. Docking studies and binding free energy calculations and hydrogen bonding with some amino acids revealed that ellagic acid showed the least binding energy for the target enzyme.

Conclusion: This research has opened new insights into understanding that constituents of methanol extract are potential inhibitors against elastase, and suggested the active compound is ellagic acid.
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http://dx.doi.org/10.4103/jpbs.JPBS_271_19DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7574744PMC
July 2020

Simultaneous Natural Deep Eutectic Solvent-Based Ultrasonic-Assisted Extraction of Bioactive Compounds of Cinnamon Bark and Sappan Wood as a Dipeptidyl Peptidase IV Inhibitor.

Molecules 2020 Aug 23;25(17). Epub 2020 Aug 23.

Graduate Program of Herbal Medicine, Faculty of Pharmacy, Universitas Indonesia, Depok, West Java 16424, Indonesia.

Cinnamon bark () and sappan wood () have been reported to be beneficial for Type-2 Diabetes Mellitus (T2DM) and the combination is commonly used by Indonesian herbal industries. In the present study, the simultaneous extraction of bioactive compounds from both plants was conducted using natural deep eutectic solvent (NADES), their content analyzed using high-performance liquid chromatography (HPLC), and their dipeptidyl peptidase IV (DPP IV) inhibitory activity evaluated. An additional in silico molecular docking analysis was conducted to ensure their activity. The results showed that NADES (with a composition of choline chloride-glycerol) extraction from cinnamon and sappan wood had DPP IV inhibitory activity of 205.0 and 1254.0 µg/mL, respectively. Brazilin as a marker substance from sappan wood was responsible for the DPP IV inhibitory activity, while none of the marker substances chosen for cinnamon bark (-cinnamaldehyde, coumarin, and -cinnamic acid) were found to have significant DPP IV inhibitory activity. These results were confirmed by molecular docking conducted in brazilin, -cinnamaldehyde, coumarin, and -cinnamic acid.
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http://dx.doi.org/10.3390/molecules25173832DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7504365PMC
August 2020

Pharmacokinetic Herb-Drug Interaction between Calyces Aqueous Extract and Captopril in Rats.

Evid Based Complement Alternat Med 2020 17;2020:5013898. Epub 2020 Jun 17.

Laboratory of Bioavailability and Bioequivalency, Faculty of Pharmacy, Universitas Indonesia, Kampus UI, Depok 16424, Indonesia.

L. (Malvaceae) is a traditional medicinal herb widely consumed as a beverage ("hibiscus tea"), and its global popularity is expanding due to health benefits such as blood pressure and cholesterol control. Previous studies showed that is coadministered with antihypertensives and antihyperlipidemics, thus predisposing herb-drug interactions. We investigated the pharmacokinetic interaction between L. aqueous extract and captopril, a frequently prescribed antihypertensive. In this study, chemical profile of L. aqueous extract was identified using HPLC system equipped with a DAD detector at 360 nm and 520 nm. The male Sprague Dawley rats were divided into two groups of six rats. Group I received a single dose of captopril suspension (4.5 mg/200 g body weight (BW) orally (p.o.)) while group II received L. aqueous extract (60 mg/200 g BW; p.o.) daily for two weeks prior to the same captopril dose. Multiple blood samples were collected at predetermined times after captopril administration and the plasma concentration was analyzed using ultrahigh-pressure liquid chromatography-tandem mass spectrometry. Chemical profiling of the L. aqueous extract showed that the extract contains chlorogenic acid, myricetin 3-arabinogalactoside, 5-O-caffeoylshikimic acid, quercetin 3-rutinoside, delphinidin 3-sambubioside, and cyanidin 3-sambubioside. Ingestion of the extract significantly reduced the captopril area under the curve (AUC) (0.1745 (0.1254-0.2429)), AUC0 (0.1734 (0.1232-0.2442))], and peak plasma concentration (0.2119 (0.1337-0.3359)) (geometric mean ratio of the coadministration group to the captopril group (90% CI)). The geometric mean ratios were falling outside the 90% CI of 0.8-1.25 bioequivalent range. Conversely, L. extract increased the apparent total body clearance (Cl/F, 0.0257 ± 0.0115 vs. 0.1418 ± 0.0338 mL/h·kg) and the apparent volume of distribution (Vd/F, 0.0541 ± 0.0226 vs. 0.3205 ± 0.0790 mL/kg). This study indicated that coadministration of L. aqueous extract could change the pharmacokinetic profile of captopril; therefore, its coadministration should be avoided.
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http://dx.doi.org/10.1155/2020/5013898DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7317316PMC
June 2020

Optimization of choline chloride-glycerol based natural deep eutectic solvent for extraction bioactive substances from barks and heartwoods.

Heliyon 2019 Dec 9;5(12):e02915. Epub 2019 Dec 9.

Department of Pharmacognosy and Phytochemistry, Faculty of Pharmacy, Universitas Indonesia, Kampus UI Depok 16424 West Java Indonesia.

Indonesian cassia ( Blume) is commonly used as a condiment. It reportedly contains a number of major phytochemical constituents such as trans-cinnamaldehyde and coumarin. Sappan wood () is a native plant of Southeast Asia that contains brazilin, a widely known red pigment. This study aimed to determine the optimal extraction conditions using a choline chloride-glycerol (ChCl-glycerol)-based natural deep eutectic solvent (NADES) to obtain greater trans-cinnamaldehyde and brazilin levels from Indonesian cassia and sappan wood. The powders of Indonesian cassia and sappan wood were extracted using ChCl-glycerol-based NADES varied at three different levels: ratio of ChCl to glycerol, ratio of powder to NADES, and the amount of water in NADES. All variables were designed using the Box-Behnken design of response surface methodology to provide 15 extraction conditions. The extraction was performed using ultrasonication-assisted extraction for 30 and 50 min for Indonesian cassia and sappan wood, respectively. Determination of the active compound contents was performed using a high-performance liquid chromatography system equipped with a UV-VIS detector at λmax = 280 nm. The optimization results revealed that the highest levels of trans-cinnamaldehyde, coumarin, and brazilin in NADES extracts were 1907.32, 1735.68, and 368.67 μg/ml, respectively, whereas the lowest levels of these compounds were 453.59, 616.76, and 74.21 μg/ml, respectively. The maximal levels exceeded those obtained using a conventional extraction method, in which 5000 μg/ml Indonesian cassia reflux extract contained only 108.45 μg/ml trans-cinnamaldehyde. Similarly, 1000 μg/ml sappan wood contained only 124.64 μg/ml brazilin. ChCl-glycerol-based NADES was suitable for extracting active compounds from Indonesian cassia and sappan wood; moreover, this solvent is more effective than organic ethanolic coventional solvent.
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http://dx.doi.org/10.1016/j.heliyon.2019.e02915DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6909081PMC
December 2019

Effects of Calyces Aqueous Extract on the Antihypertensive Potency of Captopril in the Two-Kidney-One-Clip Rat Hypertension Model.

Evid Based Complement Alternat Med 2019 17;2019:9694212. Epub 2019 Jul 17.

Laboratory of Bioavailability and Bioequivalency, Faculty of Pharmacy, Universitas Indonesia, Kampus UI Depok 16424, Indonesia.

aqueous extract (HS) is often used as complementary therapy for hypertension. However, some studies have shown that coadministration with a conventional antihypertensive drug can affect drug potency. We compared the effects of HS plus captopril (CAP) coadministration to HS and CAP administration alone on blood pressure and renin-angiotensin-aldosterone system (RAAS) biomarkers in the rat two-kidney-one-clip (2K1C) model of hypertension. Male Sprague Dawley rats were randomly divided into seven groups (n=6/group), a normal control (SHAM) group, and six 2K1C groups. In 2K1C animals, hypertension was induced using a stainless microclip (inner diameter of 0.20 mm). Four weeks after 2K1C surgery, blood pressure was significantly higher than in the SHAM group. Then, model rats were randomly divided into negative control (2K1C, no treatment), positive control (4.5 mg captopril/200 g body weight [BW] orally [p.o.]), HS alone (30 mg/200 g BW; p.o.), and 3 co-treatment groups receiving HS (15, 30, or 60 mg/200 g BW; p.o.) plus 4.5 mg/200 g BW captopril. The treatments were performed for two weeks. Blood pressure was significantly reduced by all the drug treatments to near the level of SHAM controls. Plasma renin level, serum angiotensin converting enzyme (ACE) activity, and plasma angiotensin II level were also significantly elevated in the 2K1C group compared to the SHAM group. Both serum ACE activity and plasma angiotensin II level were significantly reduced to near SHAM group levels by all the drug treatments. aqueous extract alone can reduce blood pressure. This extract appears could be used as a supplement with captopril but may not provide any additional benefit.
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http://dx.doi.org/10.1155/2019/9694212DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6662455PMC
July 2019

Potential Gastroprotective Activity of Rice Bran ( L.) Extracted by Ionic Liquid-Microwave-Assisted Extraction against Ethanol-Induced Acute Gastric Ulcers in Rat Model.

Sci Pharm 2018 Sep 7;86(3). Epub 2018 Sep 7.

Laboratory of Pharmacognosy-Phytochemistry, Faculty of Pharmacy, Universitas Indonesia, Depok 16424, Indonesia.

The presence of gamma-oryzanol in rice bran oil can be 10⁻20-fold higher than tocopherol and tocotrienol. Gamma-oryzanol has various pharmacological properties. The objective of this study was to evaluate the effectiveness of rice bran extract as a gastroprotective in reducing lesions in ethanol-induced acute gastric ulcer models in rat, using the ionic liquid-microwave-assisted extraction (IL-MAE) method. Rice bran extract was obtained using the IL-MAE method with ionic liquid (IL), 1-butyl-3-methylimidazolium tetrafluoroborate [BMIM]BF₄ (concentration 0.7 M), and a ratio of solid/liquid of 15 g/mL, 15 min extraction time, and 10% microwave power. The rats were pretreated with rice bran extract at different doses (100, 200, and 400 mg/kg body weight; BW) for seven days and subsequently exposed to acute gastric lesions induced by 80% ethanol. Omeprazole (36 mg/kg BW) was used as a standard anti-ulcer drug. The ulcer index, gastric juice acidity, and mucus levels were measured to assess the degree of gastroprotection. The results showed that the oral administration of rice bran extract at a dose of 400 mg/kg BW significantly inhibited the development of ulcer formation by 66.75% and reduced gastric acid levels. Moreover, gamma oryzanol and omeprazole protected the gastric mucosa from ethanol-induced gastric lesions by increasing the level of gastric mucus. Rice bran extract is effective as a gastroprotective therapy sourced from natural ingredients in treating the incidence of gastric ulcers. Most likely, this is related to gamma oryzanol as a bioactive compound contained in rice bran ( L.).
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http://dx.doi.org/10.3390/scipharm86030035DOI Listing
September 2018

Correlation between Chemical Composition of Curcuma domestica and Curcuma xanthorrhiza and Their Antioxidant Effect on Human Low-Density Lipoprotein Oxidation.

Evid Based Complement Alternat Med 2012 26;2012:438356. Epub 2012 Nov 26.

Drug and Herbal Research Center, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300 Kuala Lumpur, Malaysia.

The antioxidant activity of the curcuminoids of Curcuma domestica L. and C. xanthorrhiza Roxb. and eight compounds which are prevalent constituents of their rhizome oils were investigated in an effort to correlate human low-density lipoprotein (LDL) antioxidant activity with the effect of the herbs and their components. The antioxidant activity was examined using thiobarbituric acid reactive substances (TBARSs) assay with human LDL as the oxidation substrate. The methanol extracts and rhizome oils of C. xanthorrhiza and C. domestica showed strong inhibitory activity on copper-mediated oxidation of LDL. Curcumin, demethoxycurcumin, and bisdemethoxycurcumin, isolated from the methanol extracts of both plants, exhibited stronger activity than probucol (IC(50) value 0.57 μmol/L) as reference, with IC(50) values ranging from 0.15 to 0.33 μmol/L. Xanthorrhizol, the most abundant component (31.9%) of the oil of C. xanthorrhiza, showed relatively strong activity with an IC(50) value of 1.93 μmol/L. The major components of C. domestica, ar-turmerone (45.8%) and zerumbone (3.5%), exhibited IC(50) values of 10.18 and 24.90 μmol/L, respectively. The high levels of curcuminoids in the methanol extracts and xanthorrhizol, ar-turmerone and zerumbone in the oils, and in combination with the minor components were responsible for the high LDL antioxidant activity of the herbs.
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http://dx.doi.org/10.1155/2012/438356DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3519093PMC
December 2012

Benzophenones and xanthones from Garcinia cantleyana var. cantleyana and their inhibitory activities on human low-density lipoprotein oxidation and platelet aggregation.

Phytochemistry 2012 Aug 26;80:58-63. Epub 2012 May 26.

Drug and Herbal Research Center, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300 Kuala Lumpur, Malaysia.

Three benzophenones, 2,6,3',5'-tetrahydroxybenzophenone (1), 3,4,5,3',5'-pentahydroxybenzophenone (3) and 3,5,3',5'-tetrahydroxy-4-methoxybenzophenone (4), as well as a xanthone, 1,3,6-trihydroxy-5-methoxy-7-(3'-methyl-2'-oxo-but-3'-enyl)xanthone (9), were isolated from the twigs of Garcinia cantleyana var. cantleyana. Eight known compounds, 3,4,5,3'-tetrahydroxy benzophenone (2), 1,3,5-trihydroxyxanthone (5), 1,3,8-trihydroxyxanthone (6), 2,4,7-trihydroxyxanthone (7), 1,3,5,7-tetrahydroxyxanthone (8), quercetin, glutin-5-en-3β-ol and friedelin were also isolated. The structures of the compounds were elucidated by spectroscopic methods. The compounds were investigated for their ability to inhibit low-density lipoprotein (LDL) oxidation and platelet aggregation in human whole blood in vitro. Most of the compounds showed strong antioxidant activity with compound 8 showing the highest inhibition with an IC₅₀ value of 0.5 μM, comparable to that of probucol. Among the compounds tested, only compound 4 exhibited strong inhibitory activity against platelet aggregation induced by arachidonic acid (AA), adenosine diphosphate (ADP) and collagen. Compounds 3, 5 and 8 showed selective inhibitory activity on platelet aggregation induced by ADP.
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http://dx.doi.org/10.1016/j.phytochem.2012.05.003DOI Listing
August 2012

Inhibitory activities of compounds from the twigs of Garcinia hombroniana Pierre on human low-density lipoprotein (LDL) oxidation and platelet aggregation.

Phytother Res 2012 Dec 15;26(12):1845-50. Epub 2012 Mar 15.

Drug and Herbal Research Center, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300 Kuala Lumpur, Malaysia.

The methanol extract of the twigs of Garcinia hombroniana, which showed strong LDL antioxidation and antiplatelet aggregation activities, was subjected to column chromatography to obtain 3,5,3',5'-tetrahydroxy-4-methoxybenzophenone, 1,7-dihydroxyxanthone and eight triterpenoids, garcihombronane B, D, E and F, friedelin, glutin-5-en-3β-ol, stigmasterol and lupeol. The structures of the compounds were elucidated by spectroscopic methods. The compounds were evaluated for their ability to inhibit copper-mediated LDL oxidation and arachidonic acid (AA)-, adenosine diphosphate (ADP)-, collagen-induced platelet aggregation in vitro. Among the compounds tested, 3,5,3',5'-tetrahydroxy-4-methoxybenzophenone and 1,7-dihydroxyxanthone showed strong inhibitory activity on LDL oxidation with half-maximal inhibitory concentration (IC(50)) values of 6.6 and 1.7 µM, respectively. 3,5,3',5'-Tetrahydroxy-4-methoxybenzophenone exhibited strong activity on AA-, ADP- and collagen-induced platelet aggregation with IC(50) values of 53.6, 125.7 and 178.6 µM, respectively, while 1,7 dihydroxyxanthone showed significant and selective inhibitory activity against ADP-induced aggregation with IC(50) value of 5.7 µM. Of the triterpenoids tested, garcihombronane B showed moderate activity against LDL oxidation and garcihombronane D and F showed selective inhibition on ADP-induced platelet aggregation.
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http://dx.doi.org/10.1002/ptr.4667DOI Listing
December 2012