In our search for natural soluble epoxide hydrolase (sEH) inhibitors from plants, an extract of the dried whole plants of Euphorbia supina Rafin was found to significantly inhibit sEH activity in vitro. Phytochemical investigation of E. supina resulted in isolation of 17 compounds (1
Euphorbia ; Euphorbiaceae ; Inhibitory Concentration 50 ; Phenol ; Triterpenes

A new L-isoascorbic acid derivative epi-leptosphaerin (1) and two known compounds leptosphaerin (2), and verongamine (3) were isolated from sponges of the orders Verongida and Thorectidae. Compounds 1 and 2 are most likely of sponge-associated fungal origin. In the present study, isolated compounds were investigated for their inhibition of soluble epoxide hydrolase (sEH), which is considered a promising target for the management of pain, inflammation, and comorbidities associated with diabetes. Compound 3, verongamine, displayed weak inhibitory activity against sEH with an IC50 value 51.5 +/- 1.0 microM.
Comorbidity ; Inflammation ; Inhibitory Concentration 50 ; Porifera

Green tea, the leaves of Camellia sinsneis (Theaceae), is generally acknowledged as the most consumed beverage with multiple pharmacological functions including antioxidant activity. This study was performed to analyze the effect of extraction conditions of green tea on its antioxidant effects using DPPH assay. Three extraction factors such as extraction solvent (EtOH, 0 – 100%), extraction time (3 – 15 min) and extraction temperature (10 – 70℃) were analyzed and optimized extraction condition for antioxidant activity of green tea extract (GTE) was determined using response surface methodology with three-level-three-factor Box-Behnken design (BBD). Regression analysis showed a good fit of data and the optimal conditions of extraction were found to be 57.7% EtOH, 15 min and 70℃. Under this condition, antioxidant activity of experimental data was 88.4% which was almost fit to the ideal value of 88.6%. As epigallocatechin gallate (EGCG) is known for the major ingredient for antioxidant activity of green tea, we investigated the effect of EGCG on antioxidant activity of GTE. EGCG showed antioxidant activity with the IC50 value of 4.2 µg/ml and a positive correlation was observed between EGCG content and the antioxidant activity of GTE with R2 = 0.7134. Interestingly, however, GTE with 50 – 70% antioxidant activity contain less than 1.0 µg/ml of EGCG, which is much lower than IC50 value of EGCG. Therefore, we suppose that EGCG together with other constituents contribute to antioxidant activity of GTE. Taken together, these results suggest that green tea is more beneficial than EGCG alone for antioxidant ability and optimal extraction condition of green tea will be useful for the development of food and pharmaceutical applications.
Antioxidants ; Beverages ; Camellia ; Inhibitory Concentration 50 ; Tea

Phytochemical investigation from the stem bark of Beilschmiedia pulverulenta resulted in the isolation of five lignans, (+)-yangambin (1), (+)-sesartemin (2), (+)-excelsin (3), (+)-sesamin (4), and (+)-syringaresinol (5), together with lupeol (6), lupenone (7), β-sitosterol (8), and β-sitostenone (9). Their structures were established by the analysis of their spectroscopic (1D and 2D NMR) and spectrometric (MS) data, as well as by comparison with those reported in the literature. The isolated lignans were tested for their anticholinesterase (AChE: acetylcholine esterase and BChE: butyryl cholineesterase) and anti-inflammatory (COX-2: cyclooxygenase-2 and LOX: lipoxygenase) activities. All the isolated lignans (1 – 5) exhibited significant inhibition activities in AChE/BChE and COX-2/LOX assays with IC50 values ranging from 168.8 – 504.2 µM and 21.0 – 59.4 µM, respectively.
Acetylcholine ; Cyclooxygenase 2 ; Inhibitory Concentration 50 ; Lignans

Phytochemical investigation of the aerial components of Ducrosia ismaelis Asch. led to the isolation of six known compounds, psoralen (1), isopsoralen (2), cnidioside A (3), (-)-syringaresinol-O-beta-D-glucopyranoside (4), (E)-plicatin B (5), trilinolein (6). The chemical structures of these compounds were elucidated from spectroscopic data and by comparison of these data with previously published results. The antioxidant, anti-osteoporotic and cardiovascular related activities of the isolated compounds were assessed using oxygen radical absorbance capacity (ORAC), reducing capacity, tartrate-resistant acid phosphatase (TRAP), and soluble epoxide hydrolase (sEH) inhibitory activity assays. Compounds (3-5) showed potent peroxyl radical-scavenging capacities with ORAC values of 11.06 +/- 0.39, 7.98 +/- 0.10, and 13.99 +/- 0.06 Trolox equivalent (TE) at concentrations of 10 microM, respectively. Only compounds 4 and 5 was able to significantly reduce Cu2+ ions, with a reduction value of 9.06 +/- 0.32 and 4.61 +/- 0.00 microM Trolox Equivalent (TE) at a concentration of 10 microM. Compound 5 at 10 microM exhibited a potent inhibitory effect on osteoclastic TRAP activity with a TRAP value of 86.05 +/- 6.55% of the control. Compounds 1, 3 and 5 potently inhibited sEH activity with IC50 values of 41.6 4.9, 16.0 1.1, and 49.0 5.7 microM, respectively.
Acid Phosphatase ; Apiaceae ; Ficusin ; Inhibitory Concentration 50 ; Ions ; Osteoclasts ; Oxygen

Chemical investigation of the fermentation broth of a Soft Coral-Derived fungus Pestalotiopsis sp., led to the isolation of a new phthalide derivative, pestalotiolide A (1), three known analogues (2, 3 and 4), along with 5'-O-acetyl uridine (5) first isolated as a natural product. The structure of the new compound (1) was established by comprehensive spectroscopic analysis and chemical methods. Compounds 1
Fermentation ; Fungi ; Inhibitory Concentration 50 ; Ribavirin ; Structure-Activity Relationship ; Uridine

This study investigated in vitro antioxidant activity of Sonchus oleraceus L. by extraction solvent, which were examined by reducing power, hydroxyl radical-scavenging activity(HRSA) and 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assays. 70% MeOH extract had the greatest reducing power while EtOH extract had the greatest HRSA. The antioxidant activity of S. oleraceus extracts was concentration dependent and its IC50 values ranged from 47.1 to 210.5 microgram/ml and IC50 of 70% MeOH, boiling water and 70% EtOH extracts were 47.1, 52.7 and 56.5 microgram/ml, respectively. 70% MeOH extract of S. oleraceus contained the greatest amount of both phenolic and flavonoid contents. The extracts tested had greater nitrite scavenging effects at lower pH conditions. The cytotoxic activity showed that EtOH extract had the best activity against the growth of stomach cancer cell. These results suggest that S. oleraceus extract could be used as a potential source of natural antioxidants.
Antioxidants ; Hydrogen-Ion Concentration ; Inhibitory Concentration 50 ; Phenol ; Sonchus* ; Stomach Neoplasms ; Water

Pentacyclic triterpenes, mainly, asiatic acid, madecassic acid, asiaticoside, and madecassoside are the active constituents of Centella asiatica. A pentacyclic triterpene enriched C. asiatica extract (PRE) was prepared and standardized to contain a total pentacyclic triterpenes not less than 65% w/w. This work was focused on determination of antiinflammatory, antioxidant, and tyrosinase inhibitory activities of PRE and its stability. The PRE exhibited a satisfactory nitric oxide inhibitory effect, with an IC50 value of 64.6 µg/mL. In addition, the PRE inhibited tyrosinase enzyme activity with an IC50 value of 104.8 µg/mL. In contrast, the PRE possessed only weak antioxidant activity. The PRE was stable over a period of four months when stored as a dried powder but only in a well-closed container protected from light at 4 °C. An aqueous alcoholic solution of the PRE was stable at pH values of 5.8 and 7.0, but was not stable at a pH of 8.2. Preparations of the PRE in an aqueous solution should be performed in acidic or neutral conditions.
Alcoholics ; Centella ; Humans ; Hydrogen-Ion Concentration ; Inhibitory Concentration 50 ; Monophenol Monooxygenase ; Nitric Oxide ; Pentacyclic Triterpenes

Betulinic acid (BA), a natural pentacyclic triterpene found in many medicinal plants is known to have various biological activity including tumor suppression and anti-inflammatory effects. In this study, the cell-death induction effect of BA was investigated in BV-2 microglia cells. BA was cytotoxic to BV-2 cells with IC50 of approximately 2.0 μM. Treatment of BA resulted in a dose-dependent chromosomal DNA degradation, suggesting that these cells underwent apoptosis. Flow cytometric analysis further confirmed that BA-treated BV-2 cells showed hypodiploid DNA content. BA treatment triggered apoptosis by decreasing Bcl-2 levels, activation of capase-3 protease and cleavage of PARP. In addition, BA treatment induced the accumulation of p62 and the increase in conversion of LC3-I to LC3-II, which are important autophagic flux monitoring markers. The increase in LC3-II indicates that BA treatment induced autophagosome formation, however, accumulation of p62 represents that the downstream autophagy pathway is blocked. It is demonstrated that BA induced cell death of BV-2 cells by inducing apoptosis and inhibiting autophagic flux. These data may provide important new information towards understanding the mechanisms by which BA induce cell death in microglia BV-2 cells.
Apoptosis* ; Autophagy ; Cell Death* ; DNA ; Inhibitory Concentration 50 ; Microglia* ; Plants, Medicinal

Anticancer effect of methanol extract of Caesalpinia sappan L. on oral carcinoma (KB) and osteosarcoma (HOS) cells were investigated in this study. In order to elucidate the anticancer mechanism of Caesalpinia sappan L, we analyzed telomerase inhibitory effect of the methanol extract of Caesalpinia sappan L. In addition we prepared 5 fraction samples according to its polarity differences and analyzed anticancer effects on oral carcinoma and osteosarcoma cells. Following results are obtained in this study. 1. 50% cell proliferation inhibitory value (IC50) of the methanol extract of Caesalpinia sappan L. against oral carcinoma (KB) cells and osteosarcoma (HOS) cells were 9.0 microgram/ml and 10.9 microgram/ml, respectively. 2. The methanol extract of Caesalpinia sappan L. showed inhibitory effect of telomerase which is required for cancer cell immortality. Therefore, it seems that the anticancer effect of methanol extract of Caesalpinia sappan is at least partially due to telomerase inhibitory effect. 3. Five fraction samples were prepared according to its polarity and 88.7% of ingredient of total methanol extract was transferred to ethylacetate fraction. Thin layer chromatography analysis showed that dichloromethane fraction contained ingredient with relatively high polarity and ethylacetate fraction contained similar ingredient found in total methanol extract. 4. Anticancer effect was observed in n-hexane, dichloromethane, and ethylacetate fractions. The highest anticancer effect was found in dichloromethane fraction which had IC50 value of 4.4 and>4.0 microgram/ml against oral carcinoma (KB) cells and osteosarcoma (HOS) cells, respectively.
Caesalpinia* ; Cell Proliferation ; Chromatography, Thin Layer ; Inhibitory Concentration 50 ; Methanol ; Methylene Chloride ; Osteosarcoma* ; Telomerase