Chromolaena odorata Linn leaf extract - Geothermal versus nongeothermal: Phytochemical, antioxidant, and cytotoxicity screenings.

Chromolaena odorata Linn, a popular yet underutilized ethnomedicinal plant, is hypothesized to possess higher bioactive phytoconstituents when it grows in geothermal areas. In this study, the comparison of ethanolic extract from geothermal and nongeothermal C. odorata leaves was carried out based on the phytochemical profile, antioxidant activity, and cytotoxicity. The leaf extracts were produced from a maceration using ethanol 96%, where the products were identified using reagents and gas chromatography-mass spectrometry (GC-MS). Antioxidant activities of both samples were measured based on their 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activities. Cytotoxicity was determined by brine shrimp lethality test using Artemia salina. Phenols were found to be more abundant in geothermal sample based on the qualitative screening and GC-MS analysis (i.e. higher relative abundance of phytol - 3.97%). DPPH antioxidant was higher in geothermal sample than in nongeothermal sample (median inhibitory concentration =13.04 ± 3.35 mg/L vs. 41.09 ± 4.13 mg/L, respectively). Geothermal sample was noncytotoxic (median lethal concentration [LC50] =2139.30 mg/L), whereas the nongeothermal sample had low cytotoxicity (LC50 = 491.48 mg/L). Taken altogether, geothermal C. odorata leaves contain higher bioactive compounds with potent antioxidant activities.

Fatty Acid-Rich Extract from Holothuria atra for Hyperuricemia via Expressions Modulation of GLUT9a and GLUT9b in Rat Model.

An edible sea cucumber Holothuria atra has been hypothesized to have medicinal benefits against hyperuricemia owing to its bioactive compounds, including mono- and poly-unsaturated fatty acids. Herein, we aimed to investigate the fatty acids-rich extract produced from H. atra to treat hyperuricemic rats (Rattus novergicus). The extraction was carried out using n-hexane solvent and then administered to potassium oxonate-induced hyperuricemic rats, with allopurinol acting as a positive control. The extract (50, 100, 150 mg/kg body weight) and allopurinol (10 mg/kg) were administered QD through an oral route using a nasogastric tube. Serum uric acid, creatinine, aspartate aminotransferase (AST) and alanine aminotransferase (ALT), and blood urea nitrogen of the abdominal aortic blood were investigated. Our results suggested that the extract was rich in polyunsaturated (arachidonic acid) and monounsaturated fatty acids (oleic acid), in which its administration of 150 mg/kg could significantly reduce serum uric acid (p < 0.001), AST (p = 0.001), and ALT (p = 0.0302). The anti-hyperuricemic activity could be associated with the modulation of GLUT9 by the H. atra extract. In conclusion, the n-hexane extract from H. atra is a potential serum uric acid-lowering agent targeting GLUT9, where further investigations are crucially warranted.

Ethanolic Extract from Limonia acidissima L. Fruit Attenuates Serum Uric Acid Level via URAT1 in Potassium Oxonate-Induced Hyperuricemic Rats.

A high prevalence of hyperuricemia among adult and older adult populations has intrigued the development of its therapy based on natural products. Our objective was to investigate the antihyperuricemic activity of the natural product from Limonia acidissima L. in vivo. The extract was obtained through the maceration of L. acidissima fruits using an ethanolic solvent and was tested for its antihyperuricemic activity against potassium oxonate-induced hyperuricemic rats. Serum uric acid, creatinine, aspartate aminotransferase (AST), alanine aminotransferase (ALT), and blood urea nitrogen (BUN) were observed before and after the treatment. Expression of urate transporter 1 (URAT1) was also measured using a quantitative polymerase chain reaction. Antioxidant activity based on a 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging assay, along with total phenolic content (TPC) and total flavonoid content (TFC), were measured. Herein, we present the evidence of the serum uric acid lowering effect of the L. acidissima fruit extract along with improved AST and ALT (p < 0.01). The reduction of serum uric acid was in accordance with the decreasing trend of URAT1 (1.02 ± 0.05-fold change in the 200 mg group), except in a group treated with 400 mg/kg body weight extract. At the same time, BUN increased significantly in the 400 mg group (from 17.60 ± 3.286 to 22.80 ± 3.564 mg/dL, p = 0.007), suggesting the renal toxicity of the concentration. The IC50 for DPPH inhibition was 0.14 ± 0.02 mg/L with TPC and TFC of 143.9 ± 5.24 mg GAE/g extract and 390.2 ± 3.66 mg QE/g extract, respectively. Further studies should be carried out to prove this correlation along with the safe concentration range of the extract.

Cytotoxicity and phytochemical profiles of Phyllanthus emblica stem barks with in silico drug-likeliness: Focusing on antidiabetic potentials.

Out of numerous reported medicinal plants, Phyllanthus emblica has been reported to possess a strong antidiabetic potential and other pharmacological effects. This research aimed to identify the phytoconstituents in the extracts of P. emblica stem barks and hypothesize their antidiabetic potentials based on in silico drug-likeliness. Simplicia of P. emblica powder was sequentially macerated at room temperature (24 h) using n-hexane, ethyl acetate, and methanol solvents. Phytochemical profiles of the extract were investigated qualitatively using reagents, followed by gas chromatography-mass spectrometry (GC-MS) analysis. All phytocompounds were then analyzed for their pharmacological properties and predicted bioactivities on molinspiration. Cytotoxicity of each extract was evaluated using the brine shrimp lethality test. As many as 18 compounds (from GC-MS), were identified in all extract samples from P. emblica stem barks. Based on in silico drug-likeliness, methanol extract contained the most potentially bioactive compounds (16α-hydroxycleroda-3,13 (14) Z-dien-15,16-olide; 14-. beta.-H-pregna; and isochiapin B). Isochiapin B was revealed as the only compound that had no violation of the rule of five. All three compounds could hypothetically contribute to the antidiabetic activity of the methanol extract from P. emblica stem barks by inhibiting diabetes-related enzymes and interacting with nuclear receptors. Moderate cytotoxicity of ethyl acetate and methanol extract, respectively, further suggests their bioactivities.

Green Synthesis and Antimicrobial Activities of Silver Nanoparticles Using Calotropis gigantea from Ie Seu-Um Geothermal Area, Aceh Province, Indonesia.

Herein, we report our success synthesizing silver nanoparticles (AgNPs) using aqueous extracts from the leaves and flowers of Calotropis gigantea growing in the geothermal manifestation Ie Seu-Um, Aceh Besar, Indonesia. C. gigantea aqueous extract can be used as a bio-reductant for Ag+→Ag0 conversion, obtained by 48h incubation of Ag+, and the extract mixture in a dark condition. UV-Vis characterization showed that the surface plasmon resonance (SPR) peaks of AgNPs-leaf C. gigantea (AgNPs-LCg) and AgNPs-flower C. gigantea (AgNPs-FCg) appeared in the wavelength range of 410-460 nm. Scanning electron microscopy energy-dispersive X-ray spectrometry (SEM-EDS) revealed the agglomeration and spherical shapes of AgNPs-LCg and AgNPs-FCg with diameters ranging from 87.85 to 256.7 nm. Zeta potentials were observed in the range of -41.8 to -25.1 mV. The Kirby-Bauer disc diffusion assay revealed AgNPs-FCg as the most potent antimicrobial agent with inhibition zones of 12.05 ± 0.58, 11.29 ± 0.45, and 9.02 ± 0.10 mm for Escherichia coli, Staphylococcus aureus, and Candida albicans, respectively. In conclusion, aqueous extract from the leaves or flowers of Calotropis gigantea may be used in the green synthesis of AgNPs with broad-spectrum antimicrobial activities.

Relaxation effects of Eriobotrya japonica toward tracheal smooth muscle via action mechanism on histamine-1 receptor and phosphodiesterase-5 enzyme.

The Eriobotrya japonica leaves have the activity to relax the smooth muscle in the respiratory tract. However, the mechanism of action due to that activity has never been carried out. This study aims to determine the relaxation effects of E. japonica leaves extract in the isolated trachea of the guinea pigs through the inhibition of the histamine-1 (H-1) receptor and the phosphodiesterase-5 (PDE-5) enzyme. The determination of the relaxation effects was carried out by using histamine to contract smooth muscle within the tracheal tract, followed by adding cumulative concentrations of extract. Michaelis-Menten kinetics equation was used to determine the antagonist type of extract toward H-1 receptor. The understanding of mechanism of action of the extract toward PDE-5 enzyme was performed by incubating the smooth muscle using sildenafil. The percentage value of responses, originated from the relaxation effect of the extract toward the trachea was analyzed by using the t-independent test. The result showed that the extract was able to relax the smooth muscle, which was contracted by histamine, and there was a positive correlation between concentration and relaxation effect (P < 0.05; r = 0.973). The extract also antagonized the histamine as a noncompetitive antagonist. The incubation within the trachea with sildenafil demonstrated equal relaxation effect, produced by the extract. It can be concluded that E. japonica extract had relaxation effect within the isolated trachea as antagonist noncompetitive toward H-1 receptor and inhibitor of the PDE-5 enzyme.

Isolation of lupeol acetate from fruit peels of Artocarpus camansi.

The purpose of this research is to find a lupeol acetate from Artocarpus camansi fruit peel. Ethyl acetate extract of A. camansi fruit peel was obtained by maceration process. After the process of fractionation, it results 3 subfractions (A, B, and C). The subfraction B was rechromatographed and yielded B22 pure isolate. Based on data from proton nuclear magnetic resonance, Fourier transform-infrared, and mass spectrometry (MS from gas chromatography-MS), the B22 isolate was suspected as lupeol acetate compound (in this study, the presence of lupeol acetate in the A. camansi fruit peel has been reported for the first time).

Evaluation of cytotoxic activity from Temurui (Murraya koenigii [Linn.] Spreng) leaf extracts against HeLa cell line using MTT assay.

Temurui (Murraya koenigii [Linn.] Spreng) is a local plant of Aceh. The leaves of M. koenigii are used in most of the local foods as spices. Nowadays, cancer is claimed as the second deadly disease in the world where the number of sufferers increases every year. Cervical cancer (HeLa) is one of the most dominant cancers that happen in developing country, including Indonesia. Some chemotherapeutic agents using synthetic drugs have been used to treat cancer, but they are relatively expensive and cause poisoning that limits their use. Based on literatures, M. koenigii serves the potential secondary metabolites that could be developed as anticancer agent. This study aims to evaluate the cytotoxic activity from three extracts of M. koenigii leaves against HeLa cell line, including hexane, ethyl acetate, and methanol. Methodology used included extraction process, phytochemical screening, and cytotoxicity evaluation. The result showed that all the three extracts demonstrated a potent cytotoxic activity for HeLa cancer cells. Hexane and ethyl acetate showed a very strong cytotoxic effect with CD50 values <1 µg/mL, whereas methanol extract showed cytotoxic effect with CD50 value of 2.25 µg/mL. These results prove the potential of M. koenigii as an anticancer agent.

Antimicrobial Activity of Hand Lotion of Flower Mimusops elengi.

BACKGROUND: Aceh is a tropical region that is very many overgrown by various plants that have medicinal properties; one of them is M. elengi. M. elengi flower extract has the main content of triterpene and alcohol, that have antibacterial, antifungal, antioxidant and antineoplastic activity. Extraction of chemical compounds containing essential oils generally uses distillation, and get the small amounts of chemical compounds, while the maceration with n-hexane solvent, producing less active nonpolar compounds against S. aureus bacteria. AIM: Isolating the methanol extract from M. elengi flowers and test its antibacterial and antifungal activity. Furthermore, extracts with active concentrations are made into a lotion. METHODS: Methanol extract from M. elengi flower was characterised by gas chromatography-mass spectrometry, then tested for antibacterial and antifungal, then made into the lotion. The lotion was tested again for its antimicrobial activity, physical and organoleptic properties. RESULTS: The most abundant chemical compounds in an extract of M. elengi based on characterisation with GC-MS is Borneol L; (Bicyclo [2.2.1] heptane-2-ol, 1,7,7-trimethyl, as much as 82%). The methanol extract of M. elengi flower can inhibit the growth of S. aureus bacteria and C. albicans fungi, and also the lotion from methanol extract can inhibit the growth of S. aureus bacteria, but the M. elengi flower extract lotion cannot inhibit the growth of C. albicans fungi. The lotion inhibits the growth of S. aureus bacteria, from a concentration of methanol extract of 8% and 16%. Lotion with 16% methanol extract has 81.33% in activity power compared with positive control. The results of physical and organoleptic properties test, with the concentration of methanol extract of M. elengi 1, 2, 8, and 16%, have pH in the range of 6.6-8 (still in a safe range, 4.5-9 according to SNI 16-4399-1997). The lotion type is m/a, the spreading capacity of the lotion is 18.8 - 39.5 cm2. The power of adhesive at skin ranges from 1 minute 27 seconds to 3 minutes 7 seconds. The viscosity of the lotion ranges from 23,670-24,400 cP, this range is in the range based on SNI 16-4399-1996 (2000-50,000 cP), so the lotion is in a good category. The preferred lotion is at a concentration of 2%, in fragrance. CONCLUSION: Antibacterial activity of the lotion of methanol extract of M. elengi flower against S. aureus bacteria was the best at 16%, but could not inhibit the growth of C. albicans fungi. The most abundant compounds in methanol extract are Borneol L compounds; (Bicyclo [2.2.1] heptane-2-ol, 1,7,7-trimethyl. In general, the physical properties of this lotion meet the requirements of SNI16-4399-1996, SNI 16-4399-1997, and lotions which are preferred at a concentration of 2% in fragrance.