PRODUCTION OF LOVASTATIN AND SULOCHRIN BY Aspergillus terreus USING SOLID STATE FERMENTATION

Lovastatin is an anti-cholesterol agent that was produced by Aspergillus terreus using solid state fermentation (SSF). During this fermentation process, sulochrin is also produced as an unwanted co-metabolite. However, our previous result showed that sulochrin had potential as antidiabetes because it is an inhibitor agent of α-glucosidase. In this paper, we reported our observation on lovastatin and sulochrin production pattern in relation with inhibitor α-glucosidase activity during eleven days fermentation of A. terreus koji (SSF) ethyl acetate extract. Koji obtained from solid state fermentation with rice as the substrate and incubated at room temperature, sample is taken daily for eleven day (D-1 to D-11). Lovastatin and sulochrin production was measured by Liquid Chromatography- Mass Spectrometer based on their molecular weight m/z 404.5 and 332.3 respectively. The inibitory activity is measured by inhibition model of koji extract against α-glucosidase (EC 3.2.1.20) from Saccharomyces cereviceae. The results show that lovastatin production was started on the day 2 (0.04 mg/g) and achieving the optimal production on day 7 (11.46 mg/g), while sulochrin production was started on day 4 (0.60 mg/g) and keep produced until the end of fermentation period at Day 11 (3.11 mg/g). Koji extract was started to show inhibitory to α-glucosidase activity on Day 5 (IC50= 23.34 μg/mL) and keep showed activity until Day 11 (IC50=3.33 μg/mL). These results suggest that inhibitory activity of koji extract to α- glucosidase activity have relation with sulochrin biosynthesis production.Keywords: α-glucosidase inhibitor, Aspergillus terreus, lovastatin, SSF, sulochri

Antimigratory Activity of Brazilin-Containing Fraction from Caesalpinia sappan L. on MDAMB-231 Cells

Caesalpinia sappan is studied for several biological activities. The aim of this research is to determine the cytotoxic and antimigratory activities of Caesalpinia sappan active fraction in combination with cisplatin on human TNBC cells (MDA-MB-231). Caesalpinia sappan heartwood was extracted with methanol. Then, several fractions of the methanol extract were obtained by using a liquid-liquid extraction method followed by column chromatography. The cytotoxicity was determined using MTT assay. Synergistic effects were analyzed by calculating the combination index (CI). Migration was examined using wound-healing assay. Levels of MMP2 activity were determined with gelatin zymography assay. The results showed that most of the fractions included in this study exhibited cytotoxic effects against MDA-MB-231 cells, and C fraction demonstrated the highest cytotoxic activity of all fractions. The combination of C-cisplatin revealed a synergistic inhibitory effect on MDA-MB-231 cell growth (CI<1). Furthermore, C fraction, alone and in combination with cisplatin, inhibited migration of MDA-MB-231 and suppressed MMP2 activity. The C fraction isolated from Caesalpinia sappan increased the cytotoxic and antimigratory activities of cisplatin on MDA-MB-231 cells. Based on these findings, the potential of Caesalpinia sappan to act as a supportive agent in metastatic TNBC treatment with cisplatin warrants further exploration

Revelation of New Compound from Ethanolic Extract of Fragaria x ananassa var. Lembang

Fragaria x ananassa (strawberry) is a subtropical plant that can adapt well in tropical highlands. Fragaria x ananassa have been widely used to cope with health problems. The active compound component of secondary metabolites contained in Fragaria x ananassa has the potential as an antioxidant. This research is done to isolate secondary metabolites from extract of Fragaria x ananassa fruits. Extract Fragaria x ananassa was produced by maceration using ethanol as the solvent. Separation and isolation compound were carried out using Vacuum Liquid Chromatography (VLC) and Gravity Column Chromatography (GCC) guided by Thin Layer Chromatography (TLC) using hexane: ethyl acetate (3:7) as the eluent. The flavonoid compound was determined by the total content of phenolic and flavonoid in extract of Fragaria x ananassa fruits. The results of total phenolic content and total flavonoid content were 0.1130 mg/g and 0.0112 mg/g, respectively. The alkaloid compound was determined by Dragendorff testing. The elucidation of the structure by Fourier Tansform Infrared (FTIR), Nuclear Magnetic Resonance (NMR), and Liquid Chromatography Mass Spectrometry (LCMS) showed that the active compound contained in the secondary metabolite of extract ethanol from Fragaria x ananassa is 3-Cyclopentyl-5-(1-hydroxyethyl)-1,6-dihydro-7H-pyrazolo[4,3- d]pyrimidin-7-one.Keywords: Fragaria x ananassa extract, flavonoid, alkaloid, total phenolic and flavonoid content, FTIR, NMR, LCMS

Synthesis of (6-Methoxy-2,5-dinitro-quinoline-4-yl)-(5-vinyl-1-aza-bicyclo[2.2.2]oct-2-yl)-methanol) and In Vitro Assay Against Plasmodium falciparum 3D7

Quinine, a naturally happening alkaloid initially utilized for the treatment of muscle cramps, is currently most usually utilized to treat malaria. Symptoms of poisonous quinine, called Cinchonism, include wooziness, tinnitus (ringing in the ears), blurred vision, nausea, vomiting, serious adverse reaction to excessive quinine use, vision impairment and deafness. This research aimed to obtain more polar quinine derivatives using reactions with sulfuric acid and nitric acid to reduce toxicity. The reactions were performed analogously to the procedures reported in the literature. The characterization of reaction products utilizing proton (1H) and carbon-13 (13C) nuclear magnetic resonance (NMR) spectroscopy showed that the reaction using reagents led to nitration of the quinoline ring with the yields of 7.09 %. The IC50 value of >10.000 μg/mL was obtained from the antimalarial test against Plasmodium falciparum 3D7. The IC50 values proved that the synthesis products (6-Methoxy-2,5-dinitro-quinoline-4-yl)-(5- vinyl-1-aza-bicyclo[2.2.2]oct-2-yl)-methanol) was not potential for malaria treatment

Andrographolide undergoes modification after illumination by blue laser in the presence of sodium bicarbonate

1384-1387Andrographolide is the marker compound of Andrographis paniculata (Kalmegh), a herb that constitutes many traditional Asian remedies. In the present photochemical approach to modify its 12-en-14-hydroxyl moiety into 13-enone, a methanol solution of andrographolide has been illuminated with blue laser for 6 hours in the presence of sodium bicarbonate. After the illumination, it has been discovered that the 12-en-14-hydroxyl moiety undergoes modification into the 11-enone

In Vitro Antidiabetic Activities of Extract and Isolated Flavonoid Compounds from <i>Artocarpus altilis</i> (Parkinson) Fosberg

The antidiabetic activity test through a mechanism of inhibition of α-glucosidase enzyme was studied against ethanol, n-hexane, ethyl acetate and n-butanol fractions of ethanol extract of Artocarpus altilis (Parkinson) Fosberg (Moraceae) leaves and four flavonoid compounds isolated from ethyl acetate extracts of A. altilis. Ethyl acetate fraction has strongest antidiabetic activity compared to ethanol, n-hexane, and n-butanol fractions with IC50values5.98,6.79, 440.18and14.42μg/mL, respectively. Four flavonoid compounds (1-(2,4-dihydroxyphenyl)-3-[8-hydroxy-2-methyl-2-(4-methyl-3-pentenyl)-2H-1-benzopyran-5-yl]-1-propanone (AC-31), 2-geranyl-2',3,4,4'-tetrahydroxy dihydrochalcone (AC-51), 8-geranyl-4',5,7-trihydroxyflavone (AC-33) andcyclocommunol (AA-3), have been isolated from ethylacetate fraction. AC-31 was the strongest antidiabetic compound compared to AC-51, AC-33 and cyclocommunolwithIC50values are 15.73, 24.41,49.49,and72.20μg/mL. Kineticstudies of AC-31 using Lineweaver-Burk method showed that inhibition mechanism of enzymeα-glucosidase was anon-competitivetype

Andrographolide undergoes modification after illumination by blue laser in the presence of sodium bicarbonate

Andrographolide is the marker compound of Andrographis paniculata (Kalmegh), a herb that constitutes many traditional Asian remedies. In the present photochemical approach to modify its 12-en-14-hydroxyl moiety into 13-enone, a methanol solution of andrographolide has been illuminated with blue laser for 6 hours in the presence of sodium bicarbonate. After the illumination, it has been discovered that the 12-en-14-hydroxyl moiety undergoes modification into the 11-enone.

Isolation and activity test of antioxidant, antibacterial, and cytotoxic compounds from the stem bark of Aglaia foveolata Pannell

Aglaia foveolata Pannell (A. foveolata) is a type of plant that has many benefits, including the skin, leaves, roots, and seeds as medicinal ingredients. The potential of this plant is inseparable from the content of various bioactive compounds. This study aims to isolate, characterize the active compound from the stem bark of A. foveolata and test its activity as an antioxidant with the ABTS method, cytotoxic (MCF-7 cancer cells) with the MTT method, and antibacterial (bacterial strains ATCC and MDR) with the MIC. There are four isolated compounds obtained, namely (1) 17,24-epoxy-25-hydroxybaccharan-3-one, (2) β-stigmasterol glucoside, (3) Eichlerianic acid, and (4) 17,24-epoxy-25 -hydroxy-3- oxobaccharan-21-oic acid, which is a class of triterpenoid and steroid compounds. The best activity as an antioxidant was compound 3 (25.68 µg/mL); cytotoxic activity against MCF-7 cells namely compound 4 (94.59 µg/mL); antibacterial activity against ATCC strains: (1) P. aeruginosa namely compound 3 (29.4 µg/mL), (2) E. coli, (3) S. aureus, (4) B. subtilis for compounds 1, 2, and 4 have the same activity (62.5 µg/mL) while compound 3 was not active; MDR bacterial strains: (1) P. aeruginosa namely compound 4 (62.5 µg/mL), (2) E. coli namely compound 3 (62.5 µg/mL), (3) S. aureus namely compound 4 (62 .5 µg/mL), (4) B. subtilis namely compound 4 (62.5 µg/mL) and (5) K. pneumoniae namely compound 1 (125 µg/mL)

Mechanism, Adsorption kinetics and applications of carbonaceous adsorbents derived from black liquor sludge

Pretreatment processes in second generation bioethanol production produce a lignin-based black liquor. Polyaluminum chloride (PACl) was employed to treat black liquor using coagulation, in which the generated sludge was converted to a carbonaceous adsorbent. The bioethanol black liquor sludge-based carbonaceous adsorbent (BBLS-CA) was characterized physically, and its adsorption mechanism, kinetics, and ability to absorb methylene blue (MB) were evaluated. Additional studies revealed the performance of BBLS-CA to treat peat water and landfill leachate. The results demonstrate that BBLS-CA decolorized a 100 mg/l solution of MB by 98% within 30 min. MB components reclaimed from BBLS-CA reveal the presence of NH2, substituted and p-disubstituted benzene rings, and =CH2, suggesting that physical and chemical mechanisms are operative during adsorption. Isotherm analysis reveals that adsorption equilibrium followed the Langmuir model and exhibited pseudo second-order kinetic behavior. BBLS-CA adsorbed 100% iron and manganese; and remediated 72% color and 67% COD in peat water, as well as 57% COD in landfill leachate. This report highlights a by-product from black liquor sludge that can be applied to the removal of wastewater pollutants. Further, the development of method is required to obtain activated carbon which fulfills standard properties of activated carbon