Background: The extract of Adenostemma lavenia (L.) O. Kuntze leaves has anti-inflammatory activities and is used as a folk medicine to treat patients with hepatitis and pneumonia in China and Taiwan. The diterpenoid ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic acid (11αOH-KA) is the major ingredient in the extract and has wide-spectrum biological activities, such as antitumor and antimelanogenic activities, as well as anti-inflammatory activity. However, the physical and biological properties of this compound as an antioxidant or antiaging agent have not been reported yet. Methods: In addition to in vitro assays, we monitored antioxidative and antiaging signals in Schizosaccharomyces pombe (yeast) and mouse melanoma B16F10 cells. Results: A. lavenia water and chloroform fractions showed antioxidant properties in vitro. The A. lavenia extracts and 11αOH-KA conferred resistance to H2O2 to S. pombe and B16F10 cells and extended the yeast lifespan in a concentration-dependent manner. These materials maintained the yeast mitochondrial activity, even in a high-glucose medium, and induced an antioxidant gene program, the transcriptional factor pap1+ and its downstream ctt1+. Accordingly, 11αOH-KA activated the antioxidative transcription factor NF-E2-related factor 2, NRF2, the mammalian ortholog of pap1+, in B16F10 cells, which was accompanied by enhanced hemeoxygenase expression levels. These results suggest that 11αOH-KA and A. lavenia extracts may protect yeast and mammalian cells from oxidative stress and aging. Finally, we hope that these materials could be helpful in treating COVID-19 patients, because A. lavenia extracts and NRF2 activators have been reported to alleviate the symptoms of pneumonia in model animals.
Phytochemical investigation of the acetone extract of Macaranga javanica leaves afforded three new prenylated 9,10-dihydrophenanthrenes, macajavanicins A-C (1-3). Structures of these compounds were elucidated mainly by NMR and mass spectral data. Along with compounds 1-3, two known prenylated dihydrostilenes, laevifolins A and B (4, 5), were also isolated. The presence of these new 9,10-dihydrophentanthrene derivatives is the first time in the genus Macaranga, and its chemo taxonomic significances are briefly discussed. The antibacterial properties of compounds 1-5 against eight pathogenic bacteria are also described.
This study reports the optimization of the preparation of etoricoxib (ETX)-loaded low molecular weight of chitosan (LMWC) nanoparticles (ETX-LMWC-NPs) by ionic gelation method with sodium tripolyphosphate (TPP) as cross-linking agent. The independent variables (LMWC/TPP mass ratio, LMWC, and poloxamer 188 concentration) were formulated and optimized using response surface methodology (RSM) Box-Behnken design (BBD) with three levels for each factor. Size of particles, polydispersity index (PDI), and encapsulation efficiency was investigated as the dependent variable. ETX-LMWC-NPs were characterized by particle size analyzer, scanning electron microscope, UV-Vis spectrophotometry, and Fourier transforms infrared spectroscopy. The ETX-LMWC-NPs have an average particle size of 259.91 nm, a PDI of 0.041, and encapsulation efficiency of 51.25%. ETX-LMWC-NPs are spherical and have a spectrum at wavenumber 1656 cm-1 and 718 cm-1, respectively, indicating the presence of C=N and C-Cl originating from the ETX compound. The ETX release profile at pH 1.2 and 6.8 mediums approach the Korsmeyer-Peppas model. ETX released pH 1.2 did not differ significantly from free ETX with a maximum 10-12% release. ETX release at pH 6.8 had a maximum release of 21% and showed a 19% increase in dissolution rate than free ETX. The ETX-LMWC-CSNPs prepared by optimum formula (2.65 % LMWC, 5.5 LMWC/TPP mass ratio, and 1 mg/mL) showed stable monodispersity nanoparticles and easily soluble in water.
Tumbuhan Asteraceae dilaporkan mengandung metabolit sekunder tinggi yang aktif sebagai antioksidan. Senyawa antioksidan juga digunakan untuk mencegah penuaan/reaksi glikasi. Penelitian ini bertujuan menentukan aktivitas antioksidan dan antiglikasi 7 tumbuhan Asteraceae. Daun Adenostema lavenia, Ageratum conyzoides, Dichrocephala integrifolia, Galinsoga parvifolia, Synedrella nodiflora, Mikania micrantha, dan Sphagneticola trilobata masing-masing diekstraksi menggunakan air. Ekstrak kemudian ditentukan kandungan total fenol, flavonoid, dan aktivitas antioksidan menggunakan metode 1,1-difenil-2-pikrilhidrazil (DPPH) dan 2,2’-azino-bis(3 ethylbenzothiazoline-6-sulfonic acid (ABTS), serta aktivitas antiglikasi. Ekstrak dengan kadar total fenolik dan flavonoid tertinggi adalah ekstrak M. micrantha. Ekstrak A. lavenia memiliki aktivitas antioksidan terhadap DPPH tertinggi dengan nilai IC50 sebesar 121,82 μg/mL dan A. conyzoides tertinggi terhadap ABTS dengan kapasitas sebesar 4,51 mg trolox ekivalen (TE)/g ekstrak. Aktivitas antiglikasi tertinggi pada ekstrak G. parvifolia sebesar 90,67% yang tidak berbeda nyata dengan ekstrak A. lavenia (87,87%) dan S. trilobata (87,38%). Secara keseluruhan ekstrak A. lavenia dan S. trilobata baik dikembangkan sebagai antioksidan dan antiglikasi.
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