• Advances in Traditional Medicine
• /
• 제5권3호
• /
• pp.240-245
• /
• 2005

The effect of aqueous and alcoholic extract of seeds of Nigella sativa (N. sativa) was studied on the spontaneous movements of the whole worm (w.w) preparation and nerve muscle (n.m) complex of Setaria cervi (S. cervi). Both the extracts caused inhibition of spontaneous movements of the w.w and n.m complex characterized by initial stimulation followed by irreversible paralysis, with the exception that aqueous extract produced a partially reversible paralysis of w.w preparation. Lesser concentration of both the extracts was required to inhibit the movements of n.m complex than the w.w. Suggesting a cuticular permeability barrier. The lethal concentration $50\;(LC_{50})$ and lethal concentration $90\;(LC_{90})$ were 30 and 55 ng/ml for aqueous and 45 and 60 ng/ml for alcoholic extracts respectively.

• Archives of Pharmacal Research
• /
• 제25권5호
• /
• pp.643-646
• /
• 2002

The succinic semialdehyde dehydrogenase (SSADH) inhibitory component was isolated from the EtOAc fraction of Lactuca sativa through repeated column chromatography; then, it was identified as phytol, a diterpenoid, based on the interpretation of several spectral data. Incubation of SSADH with the phytol results in a time-dependent loss of enzymatic activity, suggesting that enzyme modification is irreversible. The inactivation followed pseudo-first-order kinetics with the second-rate order constant of $6.15{\times}10^{-2}mM^{-1}min^{-1}.$ Complete protection from inactivation was afforded by the coenzyme $NAD^{+}$, whereas substrate succinic semialdehyde failed to prevent the inactivation of the enzyme; therefore, it seems likely that phytol covalently binds at or near the active site of the enzyme. It is postulated that the phytol is able to elevate the neurotransmitter GABA levels in central nervous system through its inhibitory action on one of the GABA degradative enzymes, SSADH.

• Advances in Traditional Medicine
• /
• 제4권1호
• /
• pp.53-59
• /
• 2004

The effect of aqueous and alcoholic extract of the leaves of Ocimum. sanctum was studied on the spontaneous movements of the whole worm (w.w) preparation and nerve muscle (n.m.) complex of Setaria cervi (S. cervi) and on the survival of microfilariae (m.f.) in vitro. Both the extracts caused inhibition of the spontaneous motility of the w.w. and n.m. complex of S. cervi characterized by initial stimulation followed by reversible paralysis, aqueous extract at a higher concentration showed immediate effect and irreversible paralysis. The concentration required to inhibit the movements of n.m. complex was $1/4^{th}$ for aqueous and $1/3^{rd}$ for alcoholic extract compared to that for the w.w., suggesting a cuticular permeability barrier. On the m.f. the lethal concentration (LC 50 and LC 90) were 35 and 50 ng/ml for aqueous whereas, 60 and 85 ng/ml for alcoholic extracts respectively.

• 한국해양바이오학회지
• /
• 제12권2호
• /
• pp.99-107
• /
• 2020

Osteoarthritis (OA) is an inflammatory degenerative joint disease that is accompanied by irreversible joint cartilage destruction. Recently, the antioxidant effects of Carpomitra costata, which is a type of brown algae, have been reported, but their effects on OA have not been investigated. In this study, the anti-osteoarthritic effect of the ethanol extract of C. costata (EECC) on SW1353 human chondrocytes was studied. Results showed that EECC significantly attenuated the interleukin-1β (IL-1β)-induced release of pro-inflammatory mediators, including prostaglandin E2 and nitric oxide (NO), as well as expressions of cyclo-oxygenase-2 and inducible NO synthase. EECC also inhibited the IL-1β-induced expressions of matrix metalloproteinase-1, -3, and -13 in SW1353 chondrocytes, which reduced their extracellular secretion. In addition, the oxidative stress induced by IL-1β was confirmed to be blocked by EECC due to the inhibition of reactive oxygen species generation. Moreover, EECC suppressed IL-1β-mediated translocation of nuclear factor-kappa B (NF-κB) from cytosol into the nucleus and the degradation of IκB-α, which indicates that EECC exhibits anti-inflammatory effects by inhibiting the NF-κB signaling pathway. These results are the first to demonstrate the anti-inflammatory activities of C. costata extracts in chondrocytes, thus suggesting that this algae extract may be used in the treatment of OA.

• Restorative Dentistry and Endodontics
• /
• 제24권1호
• /
• pp.187-199
• /
• 1999

Bone remodeling is characterized by the continuing processes of osteoblast-mediated bone formation and osteoclast-mediated bone resorption. Bone metabolism is tightly regulated at the local level by networks of hormones, cytokines, and other factors. In pathological conditions of bone remodeling, including osteoporosis and periodontal diseases, inflammatory cytokines and local mediators are responsible for enhancement of osteoclast resorption and inhibition of repair at the sites of bone resorption. TNF-${\alpha}$ is a pleiotropic hormone with actions on the differentiation, growth, and functional activities of normal and malignant cells from numerous tissues. TNF-${\alpha}$ has been proposed as a local mediator of the control of bone turnover in situations of chronic inflammation, and it has been assumed that the local source of TNF-${\alpha}$ is the monocyte in the adjacent bone marrow or the local circulation. TNF-${\alpha}$ is a potent inducer of bone resorption. TNF-${\alpha}$ is known to induce the activation of apoptotic signaling pathway, which leads to the apoptosis of bone cells. We demonstrated that treatment of murine osteoblastic MC3T3E1 cells with TNF-${\alpha}$ decreases proliferation as well as alkaline phosphatase (ALP) activity in a dose depenent manner. In addition, TNF-${\alpha}$ increases osteoclast-like cell formation in $1{\alpha}$, 25(OH)2D3 or PGE2-treated bone marrow cell culture. When cells were cultured in TNF-${\alpha}$ free ${\alpha}$-MEM, this inhibitory effect of ALP activity was reversible up to 10 ng/ml TNF-${\alpha}$, in contrast, at the 20 ng/ml TNF-${\alpha}$, irreversible. In this concentration, TNF-${\alpha}$ may induce apoptosis in MC3T3E1 cells. In this study, TNF-${\alpha}$ induces apoptosis resulting in chromosomal DNA fragmentation, preceded by JNK/SAPKs and caspase-3 activation. Our present results show that JNK/SAPKs and caspase-3 are activated by TNF-${\alpha}$, suggesting that the JNK/SAPKs and caspase-3 participate in the bone resorption, associated with apoptosis.

• Journal of Microbiology and Biotechnology
• /
• 제19권12호
• /
• pp.1628-1634
• /
• 2009

Small heat shock proteins (sHSPs) function as molecular chaperones that protect cells against environmental stresses. In the present study, the genes of hsp17.6 and hsp17.7, cytosolic class I sHSPs, were cloned from a tropical plant, Ageratina adenophorum. Their C-terminal domains were highly conserved with those of sHSPs from other plants, indicating the importance of the C-terminal domains for the structure and activity of sHSPs. The recombinant HSP17.6 and HSP17.7 were applied to determine their chaperone function. In vitro, HSP17.6 and HSP17.7 actively participated in the refolding of the model substrate citrate synthase (CS) and effectively prevented the thermal aggregation of CS at $45^{\circ}C$ and the irreversible inactivation of CS at $38^{\circ}C$ at stoichiometric levels. The prior presence of HSP17.7 was assumed to suppress the thermal aggregation of the model substrate CS. Therefore, this report confirms the chaperone activity of HSP17.6 and HSP17.7 and their potential as a protectant for active proteins.

• Journal of Ginseng Research
• /
• 제29권2호
• /
• pp.100-106
• /
• 2005

The number of reporting the effects on ginseng's physiological, pharmacological, and behavioral effects has been increased every year. Major active components of Panax ginseng, are the ginsenosides, which are mainly triterpenoid dammarane derivatives. 3-Nitropropionic acid (3-NP) is blown to induce cellular energy deficit and oxidative stress related neurotoxicity via an irreversible inhibition of the mitochondrial enzyme succinate dehydrogenase (SDH). Intraperitoneal injection of 3-NP produces striatal degeneration. Aged animals was more vulnerable to 3-NP than young animal. We used three different ages of 5-, 8-, and 26-week-old rats. 3-NP alone treatment induced striatal lesion and increased lesion volume with age-dependent manner in 5-, 8-, and 26-week-old rats by $30.2{\pm}5.8$, $v$, and $51.3{\pm}8.4mm^3$, respectively. However, pretreatment of GTS (100 mg/kg/day) before 3-NP reduced striatal lesion in 5-,8-, and 26-week-old rats by $3.15{\pm}6.1$, $8.89{\pm}1.9$, and $27.3{\pm}5.6mm^3$, respectively. Pretreatment of GTS also significantly increased survival rate in 5-week-old rats (3-NP alone: GTS +3-NP = $40.4{\pm}6.3$: $72.5{\pm}9.5\%$) than 8-week-old rats (3-NP alone: GTS + 3-NP : $13.5{\pm}5.2\%$ : $45.1{\pm}3.1\%$). In 26-week-old rats, 3-NP alone treated group died on day 18, whereas GTS +3-NP-treated group prolonged lifespan to 30 days. Thus, pretreatment of GTS before administration of 3-NP extended lifespan in all ages. The present results indicate that aged animals are more vulnerable to 3-NP and GTS pretreatment protected 3-NP-induced striatal damage in different ages of animals.

• ALGAE
• /
• 제35권2호
• /
• pp.201-212
• /
• 2020

The inflammatory bowel diseases (IBD) including ulcerative colitis and Crohn disease are characterized by chronic inflammation throughout the gastrointestinal tract. The prevalence of IBD has been increasing worldwide, and has sometimes led to irreversible impairment of gastrointestinal structure and functions. In the present study, we identified a new sulfoquinovosylmonoacylglycerols (SQMG) (1) together with two known SQMGs (2 and 3) regulating intestinal inflammation from the brown alga Turbinaria ornata. The anti-inflammatory properties of two bioactive SQMGs, 1 and 2 were evaluated using an in vitro co-culture system consisting of human epithelial Caco-2 cells and PMA (phorbol 12-myristate 12-acetate)-differentiated THP-1 macrophages. Treatment with 1 or 2 inhibited the production nitric oxide and prostaglandin E₂ induced by lipopolysaccharide and interferon γ challenge. The expressions of inducible nitric oxide synthase and cyclooxygenase 2 were markedly down-regulated in response to inhibition of nuclear factor κB translocation to nucleus. These findings suggest the potential use of the brown alga T. ornata and its biologically active metabolites SQMGs as pharmaceutical adjuvants in the treatment of inflammation-related diseases, including IBD.

• Journal of Ginseng Research
• /
• 제22권2호
• /
• pp.140-146
• /
• 1998

It was founded that an X-compound is contained in extracts from the root of old red ginseng (6RG) compared with that from the root of 4-year old red ginseng(4RG). Both water extract and petroleum ether extract (PEII) from 6RG or 4RG inhibited the release of [$^{3}H$]-serotonin induced by platelet activating factor (PAF; 40 ng/ml). Water extract and PEll from 6RG Inhibited potently PAF-induced [$^{3}H$]-serotonin release compared with those from 4RG. X-compound out of both water extract and PEll from 6RG inhibited the release of [$^{3}H$]-serotonin inducted by collagen (100 $\mu\textrm{g}$/ml) or thrombin(20 U/ml). X-compound had a synergistic effect with water extract from 4RG on collagen-and thrombin-induced [3H] -serotonin release out of human platelets. The concentration(IC50) of X-compound that require to inhibit 50% of [$^{3}H$]-serotonin-release was 3.25 $\mu\textrm{g}$/ml, and it is inferred that maximum concentration of X-compound that inhibits the release of [$^{3}H$]-serotonin is 10 $\mu\textrm{g}$/ml. Because thrombosis is resulted mainly from the irreversible aggregations which are intimately related with the serotonin release and migraine is also caused when serotonin is released, it is inferred that water extract, PEII and X-compound from 6RG have antithrombosis and antimigrainous functions by inhibiting the release of serotonin from human platelets.

• Journal of Microbiology and Biotechnology
• /
• 제25권8호
• /
• pp.1299-1306
• /
• 2015

This study aims to investigate the mechanism of action of the cinnamon bark essential oil (CB), when used singly and also in combination with piperacillin, for its antimicrobial and synergistic activity against beta-lactamase TEM-1 plasmid-conferred Escherichia coli J53 R1. Viable count of bacteria for this combination of essential oil and antibiotic showed a complete killing profile at 20 h and further confirmed its synergistic effect by reducing the bacteria cell numbers. Analysis on the stability of treated cultures for cell membrane permeability by CB when tested against sodium dodecyl sulfate revealed that the bacterial cell membrane was disrupted by the essential oil. Scanning electron microscopy observation and bacterial surface charge measurement also revealed that CB causes irreversible membrane damage and reduces the bacterial surface charge. In addition, bioluminescence expression of Escherichia coli [pSB1075] and E. coli [pSB401] by CB showed reduction, indicating the possibility of the presence of quorum sensing (QS) inhibitors. Gas-chromatography and mass spectrometry of the essential oil of Cinnamomum verum showed that trans-cinnamaldehyde (72.81%), benzyl alcohol (12.5%), and eugenol (6.57%) were the major components in the essential oil. From this study, CB has the potential to reverse E. coli J53 R1 resistance to piperacillin through two pathways; modification in the permeability of the outer membrane or bacterial QS inhibition.