scholarly journals Biological Activities of Euphorbia peplus Leaves Ethanolic Extract and the Extract Fabricated Gold Nanoparticles (AuNPs)

Molecules ◽  
2019 ◽  
Vol 24 (7) ◽  
pp. 1431 ◽  
Author(s):  
Hamed A. Ghramh ◽  
Khalid Ali Khan ◽  
Essam H. Ibrahim
Keyword(s):  
Antimicrobial Activity ◽  
Gold Nanoparticles ◽  
Hela Cells ◽  
Hepg2 Cells ◽  
Biological Activities ◽  
Inhibitory Effect ◽  
Mosquito Larvae ◽  
Inhibitory Effects ◽  
Euphorbia Peplus ◽  
Dose Dependent

Euphorbia peplus leaves extract (EpExt) and gold nanoparticles (AuNPs) phytofabricated with extract (EpExt-AuNPs) were investigated for biological activities. EpExt and EpExt-AuNPs were screened for: (i) anticancer activity against Hela and HepG2 cell lines; (ii) antimicrobial activity; (iii) hemolytic activity; (iv) cytotoxic or stimulatory effects; and (v) insecticidal activity. AuNPs (size 50 nm) were synthesized. (i) EpExt had a stimulatory effect (51.04%) on Hela cells and an inhibitory effect (−12.83%) on HepG2 cells while EpExt-AuNPs showed inhibitory effects (−54.25% and −59.64% on Hela and HepG2 cells respectively). (ii) Antimicrobial activity of EpExt-AuNPs was significantly higher (ranged from 11.67 mm to 14.33 mm) than that of EpExt (ranged from 5.33 mm to 6.33 mm). (iii) Both EpExt and EpExt-AuNPs displayed 100% hemolysis. (iv) A dose-dependent inhibitory effect of EpExt was observed (ranged from −48.5% to −92.1%), which was greater than that of EpExt-AuNPs (ranged from −32.1% to −69.1%) (v) EpExt-AuNPs was more lethal against mosquito larvae with lethal concentration (LC50) value (202.692 ppm) compared to EpExt (1430.590 ppm). In conclusion, EpExt-AuNPs were inhibitory against HepG2 and Hela cells, while EpExt inhibited HepG2 but stimulated Hela cells. EpExt-AuNPs had antimicrobial effects. EpExt showed dose-dependent inhibitory effects on splenic cells. EpExt-AuNPs were lethal against mosquito larvae.

scholarly journals Synthesis of Gold Nanoparticles (AuNPs) Using Ricinus communis Leaf Ethanol Extract, Their Characterization, and Biological Applications

Nanomaterials ◽  
2019 ◽  
Vol 9 (5) ◽  
pp. 765 ◽  
Author(s):  
Hamed A. Ghramh ◽  
Khalid Ali Khan ◽  
Essam H. Ibrahim ◽  
William N. Setzer
Keyword(s):  
Antimicrobial Activity ◽  
Gold Nanoparticles ◽  
Cell Viability ◽  
Red Blood Cells ◽  
Hela Cells ◽  
Blood Cells ◽  
Hepg2 Cells ◽  
Ricinus Communis ◽  
Inhibitory Effects ◽  
Splenic Cells

The purpose of this study was to explore the collective biological properties of Ricinus communis ethanol leaf extract (RcExt) and extract-fabricated gold nanoparticles (RcExt-AuNPs). AuNPs were synthesized using RcExt. Fingerprint data of the biochemicals putatively found in RcExt were obtained using gas chromatography–mass spectrometry (GC-MS/MS) and high-performance liquid chromatography/ultraviolet-visible (HPLC/UV-VIS) analyses. RcExt-AuNPs were characterized by UV-Vis spectroscopy, scanning electron microscopy (SEM), and Fourier- transform infrared radiation (FTIR) spectroscopy. Cytotoxic activity on the Hela and HepG2 tumor cell lines was tested through cell viability, antimicrobial activity against bacterial and fungal pathogens through a well diffusion assay, hemolytic activity on red blood cells through absorbance reading, and stimulatory/inhibitory effects on splenic cells by cell viability. AuNPs of 200 nm size were synthesized. GC-MS/MS analysis revealed 12 peaks and HPLC/UV-VIS analysis resulted in 18, 13, and five peaks at the wavelengths of 220, 254, and 300 nm, respectively. Cytotoxicity screening revealed that RcExt had stimulatory effects (6.08%) on Hela cells and an inhibitory effect (−28.33%) on HepG2 cells, whereas RcExt-AuNPs showed inhibitory effects (−58.64% and −42.74%) on Hela and HepG2 cells, respectively. Antimicrobial activity of RcExt-AuNPs against tested pathogens was significantly higher (average diameters of inhibition zones were higher (ranging from 9.33 mm to 16.33 mm)) than those of RcExt (ranging from 6.00 mm to 7.33 mm). RcExt and RcExt-AuNPs showed 4.15% and 100% lytic effects, respectively. Inhibitory effects on splenic cells for RcExt-AuNPs were observed to be significantly higher (−30.56% to −72.62%) than those of RcExt (−41.55% to −62.25%) between concentrations of 25 to 200 µg/mL. RcExt-AuNPs were inhibitory against HepG2 and Hela cells, while RcExt inhibited HepG2 but stimulated Hela cells. RcExt-AuNPs showed comparatively more antimicrobial activity. RcExt was safe while RcExt-AuNPs harmful to red blood cells (RBCs). RcExt and RcExt-AuNPs showed inhibitory effects on splenic cells irrespective of dose.

Inhibitory Effects of Indomethacin on Implantation and its Related Phenomena

1996 ◽  
Vol 24 (4) ◽  
pp. 358-362 ◽  
Author(s):  
K Kanayama ◽  
H Osada ◽  
K Nariai ◽  
T Endo
Keyword(s):  
Birth Rate ◽  
Inhibitory Effect ◽  
High Rate ◽  
Control Group ◽  
Corpora Lutea ◽  
Response Relationship ◽  
Inhibitory Effects ◽  
Dose Response Relationship ◽  
Dose Dependent ◽  
Implantation Period

The dose-response relationship for the inhibitory effect of indomethacin on implantation and continuance of pregnancy was examined in four groups of rabbits administered with indomethacin (2.5, 5.0, 7.5 and 10.0 mg/kg) during the implantation period and compared with a control group. Implanted fetuses and corpora lutea were counted by laparotomy, and the number of offspring born was noted. The inhibitory effect of indomethacin on implantation was found to be dose–dependent, and the birth rate decreased in the indomethacin groups compared with the control group. As a result, even where implantation had been achieved, death of the implanted fetuses occurred at a high rate in rabbits administered with indomethacin during the implantation period.

Discovery of a Novel Small-Molecule Interleukin-6 Inhibitor through Virtual Screening Using Artificial Intelligence

2021 ◽  
Vol 18 ◽  
Author(s):  
Yoshiaki Sato ◽  
Ikuo Kashiwakura ◽  
Masaru Yamaguchi ◽  
Hironori Yoshino ◽  
Takeshi Tanaka ◽  
...  
Keyword(s):  
Artificial Intelligence ◽  
Small Molecule ◽  
Interleukin 6 ◽  
Inflammatory Diseases ◽  
Biological Activities ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Cell Functions ◽  
Dependent Cell ◽  
Dose Dependent

Background: Interleukin-6 (IL-6) is a multifunctional cytokine involved in various cell functions and diseases. Thus far, several IL-6 inhibitors, such as, humanized monoclonal antibody have been used to block excessive IL-6 signaling causing autoimmune and inflammatory diseases. However, anti-IL-6 and anti-IL-6 receptor monoclonal antibodies have some clinical disadvantages, such as a high cost, unfavorable injection route, and tendency to mask infectious diseases. While a small-molecule IL-6 inhibitor would help mitigate these issues, none are currently available. Objective: The present study evaluated the biological activities of identified compounds on IL-6 stimulus. Methods: We virtually screened potential IL-6 binders from a compound library using INTerprotein’s Engine for New Drug Design (INTENDD®) followed by the identification of more potent IL-6 binders with artificial intelligence (AI)-guided INTENDD®. The biological activities of the identified compounds were assessed with the IL-6-dependent cell line 7TD1. Results: The compounds showed the suppression of IL-6-dependent cell growth in a dose-dependent manner. Furthermore, the identified compound inhibited expression of IL-6-induced phosphorylation of signal transducer and activator of transcription 3 in a dose-dependent manner. Conclusion: Our screening compound demonstrated an inhibitory effect on IL-6 stimulus. These findings may serve as a basis for the further development of small-molecule IL-6 inhibitors.

scholarly journals Inhibition of Liver Tumor Cell Metastasis by Partially Acetylated Chitosan Oligosaccharide on A Tumor-Vessel Microsystem

Marine Drugs ◽  
2019 ◽  
Vol 17 (7) ◽  
pp. 415 ◽  
Author(s):  
Bolin Jing ◽  
Gong Cheng ◽  
Jianjun Li ◽  
Zhuo A. Wang ◽  
Yuguang Du
Keyword(s):  
Tumor Cells ◽  
Liver Tumor ◽  
Hepg2 Cells ◽  
Tumor Metastasis ◽  
Inhibitory Effect ◽  
Chitosan Oligosaccharide ◽  
Inhibitory Effects ◽  
Tumor Vessel ◽  
Destructive Effect ◽  
Cell Metastasis

Chitooligosaccharides (COS), the only cationic oligosaccharide in nature, have been demonstrated to have anti-tumor activity. However, the inhibitory effects of COS on different stages of tumor metastasis are still unknown, and it is not clear what stage(s) of tumor metastasis COS targeted. To study the inhibitory effects of a new partially acetylated chitooligosaccharide (paCOS) with fraction of acetylation (FA) 0.46 on each phase of liver cancer cell metastasis, a dynamic tumor-vessel microsystem undergoing physiological flow was leveraged. paCOS (FA = 0.46) significantly inhibited proliferation of HepG2 cells through vascular absorption on the chip, and inhibited migration of HepG2 cells by inhibiting the formation of pseudopod in liver tumor cells. It was also found that paCOS at 10 μg/mL had a stronger inhibitory effect on liver tumor cells invading blood vessels than that of paCOS at 100 μg/mL, and paCOS at 100 μg/mL, which had a significant destructive effect on tumor vascular growth and barrier function. Moreover, paCOS reduced the number of liver tumor cells adhering onto the surface of HUVECs layer after 3 h of treatment. Therefore, the results revealed that paCOS had considerable potential as drugs for anti-tumor metastasis.

scholarly journals Inhibitory Effect and Mechanism of Arctium lappa Extract on NLRP3 Inflammasome Activation

2018 ◽  
Vol 2018 ◽  
pp. 1-10 ◽  
Author(s):  
Young-Kyu Kim ◽  
Sushruta Koppula ◽  
Do-Wan Shim ◽  
Eun-Jung In ◽  
Su-Bin Kwak ◽  
...  
Keyword(s):  
Nlrp3 Inflammasome ◽  
Biological Activities ◽  
Inhibitory Effect ◽  
Inflammasome Activation ◽  
Inhibitory Effects ◽  
Arctium Lappa ◽  
Nlrp3 Inflammasome Activation ◽  
Anti Inflammatory ◽  
Underlying Mechanisms ◽  
Peritonitis Model

Arctium lappa (A. lappa), Compositae, is considered a potential source of nutrition and is used as a traditional medicine in East Asian countries for centuries. Although several studies have shown its biological activities as an anti-inflammatory agent, there have been no reports on A. lappa with regard to regulatory role in inflammasome activation. The purpose of this study was to investigate the inhibitory effects of A. lappa extract (ALE) on NLRP3 inflammasome activation and explore the underlying mechanisms. We found that ALE inhibited IL-1β secretion from NLRP3 inflammasome activated bone marrow derived macrophages but not that secreted by NLRC4 and AIM2 inflammasomes activation. Mechanistic studies revealed that ALE suppressed the ATPase activity of purified NLRP3 and reduced mitochondrial reactive oxygen species (mROS) generated during NLRP3 activation. Therefore, the inhibitory effect of ALE on NLRP3 inflammasome might be attributed to its ability to inhibit the NLRP3 ATPase function and attenuated the mROS during inflammasome activation. In addition, ALE significantly reduced the LPS-induced increase of plasma IL-1β in mouse peritonitis model. These results provide evidence of novel anti-inflammatory mechanisms of A. lappa, which might be used for therapeutic applications in the treatment of NLRP3 inflammasome-associated inflammatory disorders.

scholarly journals Inhibition of Wool Growth in Merino Sheep following Administration of Mouse Epidermal Growth Factor and a Derivative

1982 ◽  
Vol 35 (2) ◽  
pp. 163 ◽  
Author(s):  
GPM Moore ◽  
BA Panaretto ◽  
D Robertson
Keyword(s):  
Growth Factor ◽  
Epidermal Growth Factor ◽  
Dose Level ◽  
Fibre Production ◽  
Inhibitory Effect ◽  
Inhibitory Effects ◽  
Parent Molecule ◽  
Wool Growth ◽  
Epidermal Growth ◽  
Dose Dependent

The present study investigates the effects of dosage and different modes of delivery of mouse epidermal growth factor (EG F) on the production of breaks in the fleece and on wool growth in Merino wethers. Subcutaneous infusions of EGF of ~O� 25 mg kg- o.75 for 7-28 h resulted in a dose-dependent total or partial inhibition of wool production 2-4 weeks later. A complete break appeared in the fleece that was shed. Lower doses had lesser inhibitory effects on wool growth: the fleece was not shed but bore a zone of weakness, termed an incomplete break. Inclusion of the glucocorticoid analogue dexamethasone in the infusate did not alter the action of EGF on the fleece. Although a higher plane of nutrition increased the rate of fibre production, it did not alter the extent of inhibition of wool growth by EGF. Infusion of a peptide from EGF, which lacked eight of the C-terminal amino acids (EGFl _ 45), was as effective as the parent molecule in inhibiting wool growth. EGF administered as a single subcutaneous injection was less reliable as a method for producing breaks in the fleece. Of seven wethers that received EGF at a dose level between 0�27 and 0�32 mg kg- o. 7 5, only three shed their fleeces. The remainder either developed incomplete breaks in the wool or were not affected. Administration of EGF at a dose level of 0�56 mg kg- 0. 7 5 via a rumen tube to one sheep had no discernible inhibitory effect on wool growth.

Effect of Norcantharidin on N-acetyltransferase Activity in HepG2 Cells

2001 ◽  
Vol 29 (01) ◽  
pp. 161-172 ◽  
Author(s):  
Lii-Tzu Wu ◽  
Jing-Gung Chung ◽  
Jung-Chou Chen ◽  
Wei Tsauer
Keyword(s):  
Hepatocellular Carcinoma ◽  
Hepg2 Cell ◽  
Hepg2 Cells ◽  
High Performance ◽  
Inhibitory Effect ◽  
The Other ◽  
Dependent Manner ◽  
Hepg2 Cell Line ◽  
Aminobenzoic Acid ◽  
Dose Dependent

The inhibition of arylamine N-acetyltransferase (NAT) activity by norcantharidin (NCTD), the demethylated form of cantharidin, in human hepatocellular carcinoma HepG2 cells was investigated. By using high performance liquid chromatography, NAT activity on acetylation of 2-aminofluorene (AF) and p-aminobenzoic acid (PABA) were examined. Two assay system were performed, one with cellular cytosols, the other with intact HepG2 cell suspensions. The NAT activity in HepG2 cell line was inhibited by norcantharidin in a dose-dependent manner in both types of examined systems: i.e. the greater the concentration of norcantharidin in the reaction, the greater the inhibition of NAT activities. This report is the first to show that norcantharidin has an inhibitory effect on NAT activity in HepG2 cell.

scholarly journals Synthesis, characterization, biological activities, and catalytic applications of alcoholic extract of saffron (Crocus sativus) flower stigma-based gold nanoparticles

2021 ◽  
Vol 10 (1) ◽  
pp. 230-245
Author(s):  
Fahad A. Alhumaydhi ◽  
Ibrahim Khan ◽  
Abdur Rauf ◽  
Muhammad Nasimullah Qureshi ◽  
Abdullah S. M. Aljohani ◽  
...  
Keyword(s):  
Gold Nanoparticles ◽  
Biological Activities ◽  
Inhibitory Effect ◽  
Biological Properties ◽  
Crocus Sativus ◽  
Alcoholic Extract ◽  
X Ray ◽  
Vis Spectroscopy

Abstract Currently, nanotechnology is gaining massive attention compared to conventional methods as the biosynthesis of plant-based nanoparticles is considered safe, effective, and ecofriendly. Therefore, keeping in view the importance of nanotechnology, the present study was designed to synthesize, characterize, and evaluate the biological effectiveness of saffron stigma-based gold nanoparticles (SS-AuNPs) for their in vitro and in vivo biological properties. These gold nanoparticles were characterized by UV–Vis spectroscopy, Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), energy-dispersive X-ray spectroscopy (EDX), and X-ray diffraction (XRD). The highest antibacterial effect was observed by the saffron extract against Escherichia coli (22 mm). SS-AuNPs significantly inhibited the activity of enzyme urease (54.98%) and CA-II (64.29%). However, the nonsignificant inhibitory effect was observed in the case of α-chymotrypsin. Maximum analgesic (84.98%) and antiinflammatory (88.98%) effects were observed for SS-AuNPs (10 mg/kg). Similarly, SS-AuNPs demonstrated a significant (P < 0.01) sedative effect at all tested doses.

Surfactant-associated protein inhibits phospholipid secretion from type II cells

1987 ◽  
Vol 63 (2) ◽  
pp. 692-698 ◽  
Author(s):  
W. R. Rice ◽  
G. F. Ross ◽  
F. M. Singleton ◽  
S. Dingle ◽  
J. A. Whitsett
Keyword(s):  
Pulmonary Surfactant ◽  
Lung Surfactant ◽  
Inhibitory Effect ◽  
Heat Denaturation ◽  
Type Ii Cells ◽  
Dependent Manner ◽  
Type Ii ◽  
Inhibitory Effects ◽  
Dose Dependent

Secretion of [3H]phosphatidylcholine ([3H]PC) from isolated rat pulmonary type II epithelial cells was inhibited by the surfactant-associated protein of Mr = 35,000 (SAP-35) purified from canine lung surfactant. SAP-35 inhibited [3H]PC secretion in a dose-dependent manner and significantly inhibited basal, phorbol ester, beta-adrenergic, and P2-purinergic agonist-induced [3H]PC secretion. SAP-35 significantly inhibited [3H]PC secretion from 1 to 3 h after treatment. The IC50 for inhibition of [3H]PC secretion by canine SAP-35 was 1–5 X 10(-6) g/ml and was similar for inhibition of both basal and secretagogue-stimulated release. Heat denaturation of SAP-35, addition of monoclonal anti-SAP-35 antibody, reduction and alkylation of SAP-35, or association of SAP-35 with phospholipid vesicles reversed the inhibitory effect on secretagogue-induced secretion. Inhibitory effects of SAP-35 were observed 3 h after cells were washed with buffer that did not contain SAP-35. Although SAP-35 enhanced reassociation of surfactant phospholipid with isolated type II cells, its inhibitory effect on secretion of [3H]PC did not result from stimulation of reuptake of secreted [3H]PC by type II cells. The inhibition of phospholipid secretion by SAP-35 was also not due to inhibition of PC or disaturated PC synthesis by SAP-35. SAP-35, the major phospholipid-associated protein in pulmonary surfactant, is a potent inhibitor of surfactant secretion from type II cells in vitro and may play an important role in homeostasis of surfactant in the alveolar space.

Human Recombinant Activin-A Modulates the Steroidogenesis of Cultured Bovine Adrenocortical Cells

1992 ◽  
Vol 132 (3) ◽  
pp. R1-R4 ◽  
Author(s):  
Y. Nishi ◽  
M. Haji ◽  
S. Tanaka ◽  
T. Yanase ◽  
R. Takayanagi ◽  
...  
Keyword(s):  
Inhibitory Effect ◽  
Activin A ◽  
Dependent Manner ◽  
Cortisol Secretion ◽  
Inhibitory Effects ◽  
Aldosterone Secretion ◽  
Adrenocortical Cells ◽  
Adrenal Steroidogenesis ◽  
Direct Inhibitory Effect ◽  
Dose Dependent

ABSTRACT The effect of human recombinant activin-A on adrenal steroidogenesis was studied in cultured bovine adrenocortical cells. Activin-A significantly reduced cortisol output from ACTH (10nmol/l)-stimulated adrenocortical cells incubated for 24 hours in a dose-dependent manner (10, 100 and 500ng activin-A /ml suppressed cortisol secretion by 19, 33 and 40%), although no significant effect was observed in the case of 3 h incubation. Dehydroepiandrosterone (DHEA) secretion from ACTH-stimulated adrenocortical cells incubated for 24 h was also decreased by the addition of activin-A in a dose-dependent manner. (10, 100 and 500ng activin-A /ml suppressed DHEA secretion by 22, 56 and 58%). These inhibitory effects of activin-A (100ng/ml) on cortisol and DHEA secretion were partially blocked by the addition of follistatin / FSH-Suppressing Protein (200ng/ml). In contrast, activin-A treatment resulted in no significant decrease in aldosterone secretion. There were no significant effects of activin-A on basal secretions of cortisol, DHEA or aldosterone from adrenocortical cells. These results suggest that activin-A has a direct inhibitory effect on ACTH-stimulated bovine adrenocortical steroidogenesis.

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