Osman, Mohamed E.;El-nasr, Amany A. Abo;Hussein, Hagar M;Hamed, Moaz M
Microbiology and Biotechnology Letters
/
v.50
no.2
/
pp.255-269
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2022
Actinomycetes isolated from marine habitats represent a promising source of bioactive substances. Here, we report on the isolation, identification, productivity enhancement and application of the bioactive compounds of Streptomyces qinglanensis H4. Eighteen marine actinomycetes were isolated and tested for resistance to seven bacterial diseases. Using 16S rRNA sequencing analysis (GenBank accession number MW563772), the most powerful isolate was identified as S. qinglanensis. Although the strain produced active compound(s) against a number of Gram-negative and Gram-positive bacteria, it failed to inhibit pathogenic fungi. The obtained inhibition zones were 22.0 ± 1.5, 20.0 ± 1, 16.0 ± 1, 12.0 ± 1, 22.0 ± 1 and 24.0 ± 1 mm against Bacillus subtilis ATCC 6633, Escherichia coli ATCC 19404, Enterococcus faecalis ATCC 29212, Pseudomonas aeruginosa ATCC 9027, Candida albicans ATCC 10231 and Staphylococcus aureus ATCC6538, respectively. To maximize bioactive compound synthesis, the Plackett-Burman design was used. The productivity increased up to 0.93-fold, when S. qinglanensis was grown in optimized medium composed of: (g/l) starch 30; KNO3 0.5; K2HPO4 0.25; MgSO4 0.25; FeSO4·7H2O, 0.01; sea water concentration (%) 100; pH 8.0, and an incubation period of 9 days. Moreover, the anticancer activity of S. qinglanensis was tested against two different cell lines: HepG2 and CACO. The inhibition activities were 42.96 and 57.14%, respectively. Our findings suggest that the marine S. qinglanensis strain, which grows well on tailored medium, might be a source of bioactive substances for healthcare companies.
Objectives : Oryeong-san was composed of Alismatis Rhizoma, Atractylodis Rhizoma Alba, Poria Sclerotium, Polyporus, Cinnamomi Cortex, and known to have hundreds of chemical compounds. The aim of this study was to screen chemical compounds constituting Oryeong-san with the drug-likeness and oral bioavailability from the analysis of their physicochemical properties. Methods : A list of chemical compounds of Oryeong-san was obtained from TM-MC(database of medicinal materials and chemical compounds in Northeast Asian traditional medicine). To remove redundant compounds, the SMILES (Simplified Molecular Input Line Entry System) strings of each compound were identified. All of the physicochemical properties for the compounds were calculated using the DruLiTo(Drug Likeness Tool). Drug-likeness was estimated by QED(Quantitative Estimate of Druglikeness) and OB(Oral bioavailability) was checked based on the Veber's rules. Results : A total of 475 compounds were obtained by eliminating duplication among 544 compounds of 5 medicinal materials. Analysis of the physicochemical properties revealed that the most common values were MW(molecular weight) 200~300 g/mol, ALOGP(octanol-water partition coefficient) 1~2, HBA(number of hydrogen bond acceptors) 0~1, HBD(number of hydrogen bond donors) 0, PSA(polar surface area) 0~50 angstrom, ROTB(number of rotatable bonds) 1, AROM(number of aromatic rings) 0, and ALERT(number of structural alerts) 1. QED had 93% of the values between 0.2 and 0.7, and OB had 90% of the value of TRUE. Conclusions : We in this paper screened the candidate active compounds of Oryeong-san using the QED and Veber's rules. In the future, we will use the screening results to analyze the mechanism of Oryeong-san based on systems pharmacology.
BACKGROUND/OBJECTIVES: A variety of immunomodulators can improve the efficacy of low-dose chemotherapeutics. Active hexose correlated compound (AHCC), a mushroom mycelia extract, has been shown to be a strong immunomodulator. Whether AHCC could enhance the antitumor effect of low-dose 5-fluorouracil (5-FU) via regulation of host immunity is unknown. MATERIALS/METHODS: In the current study Hepatoma 22 (H22) tumor-bearing mice were treated with PBS, 5-FU ($10mg{\cdot}kg^{-1}{\cdot}d^{-1}$, i.p), or AHCC ($360mg{\cdot}kg^{-1}{\cdot}d^{-1}$, i.g) plus 5-FU, respectively, for 5 d. $CD^{3+}$, $CD^{4+}$, $CD^{8+}$, and NK in peripheral blood were detected by flow cytometry. ALT, AST, BUN, and Cr levels were measured by biochemical assay. IL-2 and $TNF{\alpha}$ in serum were measured using the RIA kit and apoptosis of tumor was detected by TUNEL staining. Bax, Bcl-2, and TS protein levels were measured by immunohistochemical staining and mRNA level was evaluated by RT-PCR. RESULTS: Diet consumption and body weight showed that AHCC had no apparent toxicity. AHCC could reverse liver injury and myelosuppression induced by 5-FU (P < 0.05). Compared to mice treated with 5-FU, mice treated with AHCC plus 5-FU had higher thymus index, percentages of $CD^{3+}$, $CD^{4+}$, and NK cells (P < 0.01), and ratio of $CD^{4+}$/$CD^{8+}$ (P < 0.01) in peripheral blood. Radioimmunoassay showed that mice treated with AHCC plus 5-FU had the highest serum levels of IL-2 and $TNF{\alpha}$ compared with the vehicle group and 5-FU group. More importantly, the combination of AHCC and 5-FU produced a more potent antitumor effect (P < 0.05) and caused more severe apoptosis in tumor tissue (P < 0.05) compared with the 5-FU group. In addition, the combination of AHCC and 5-FU further up-regulated the expression of Bcl-2 associated X protein (Bax) (P < 0.01), while it down-regulated the expression of B cell lymphoma 2 (Bcl-2) (P < 0.01). CONCLUSIONS: These results support the claim that AHCC might be beneficial for cancer patients receiving chemotherapy.
Journal of the Korean Society of Food Science and Nutrition
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v.41
no.4
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pp.456-461
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2012
The leaves of $Stevia$$rebaudiana$ are well-known in Japan, Korea, and China as a natural sweetener. Medicinal uses of this plant originated in Paraguay and Brazil in the form of aqueous decoctions of the leaves used as a contraceptive agent and for the treatment of hyperglycemia. In the present study, the antioxidant, anti-hypertension, and anti-inflammatory activities of $S.$$rebaudiana$ extracts are investigated for their use in food. The biologically-active compound was isolated and purified from $S.$$rebaudiana$. The isolated compound was identified as austroinulin ($C_{20}H_{34}O_3$; molecular weight 322) by mass, IR spectrophotometry, 1D, and 2D-NMR. Austroinulin was characterized as a diterpenoid possessing a 3-methylpenta-2,4-dienyl at C-9. When subjected to an inflammatory mediator inhibitory assay from lipopolysaccharide (LPS)-activated macrophages, the austroinulin inhibited the enhanced production of nitric oxide (NO) and inducible nitric oxide synthase (iNOS) expression (10 ${\mu}g$/mL=67.9 and 45.1%, respectively). This was significant and dose-dependent. The results suggest that austroinulin from $S.$$rebaudiana$ inhibited the NO and iNOS in RAW 264.7 cells.
Panax ginseng has been extensively used in the traditional oriental medicine as a restorative, tonic and Prophylactic agent. Recently, several reports regarding to anticancer effects of Panax ginseng has accumulated. These studies emphasized the fact that the anticancer activities might be due to a glycoside group called ginsenoside or pan.u saponin which has a water soluble characteristic. However, the authors and collaborates demonstrated that a highly lipid soluble component in extract of Panax ginseng roots contains a considerable cytotoxic activities against marine leukemic cells (L1210, P388) and human censer cells (HRT-18, HT-29, HCT48). This study was devised to observe the cytotoxic activities of Petroleum-ether extract of Panax giuseng roots (crude GBD and its Partially Purified fraction from silicic acid column chromatography (7 : 3 GX) against sarcoma-180 (5-180) and Walker carcinosar- coma 256 (Walker 256) in vivo, and murine leukemic Lymphocytes (L1210) and human rectal cancer cells (HRT-18) and human colon cancer cells (HT-29 and HCT48) in vitro. Each cell-line was cultured in medium containing serial concentration of the crude GX or 7 : 3 GX in vitro. A highly lipid soluble compound in the extract of Panax ginseng root was cytocidal to murine leukemic cells and human colon and rectal cancer cells in vitro. In the meantime, ginseng saponin derivatives did not have cytotoxic effects at its corresponding concentration. The growth rates of the cancer cells in medium containing ginseng extracts were inhibited gradually to a significant degree roughly in proportion to the increase of the extract concentration. The cytotoxic activity of 7 : 3 GX was about 3 times more potent than that of crude GX, one unit of cytotoxic activity against L1210 cells being equivalent to 2.54 Ug and 058 Ug for the crude GX and 7 : 3 GX, respectively. The Ri value of the active compound on silica- gel thin layer chromatography with petroleum-ether/ethyl ether/acetic acid mixture (90 : 10 : 1, v/v/v) as a developing so lvent was 053. While, the Panaxydol and Panaxynol as active compounds were purified from Petroleum-ether extract of Panax ginseng root by Drs. Ahn and Kim, and author found out that the one unit of cytotoxic activity of the Panaxydol and Panaxynol against L1210 cells being equivalent to 056 Ug and 0.3918 respectively. The survival times of mice inoculated with S-180 cells were extended about 1.5 to 2 times by the 7 : 3 GX treatment compared with their control group. The significantly decreased hemoglobin values of rats after inoculation with Walker 256 were recovered to normal range by oral administration of the crude Gt The synthetic levels of protein, DNA and RNA in human colon and rectal cancer cells were significantly diminished by treatment with the crude GX, which can explain a part of the origin of its anticancer activity.
Park, Yong Dae;Kang, Min Ah;Lee, Hyo Jung;Jin, Chang Hyun;Choi, Dae Seong;Kim, Dong Sub;Kang, Si-Yong;Byun, Myung Woo;Jeong, Il Yun
Journal of Radiation Industry
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v.3
no.1
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pp.13-18
/
2009
In earlier investigations, seeds of Perilla frutescens(L.) Britt. cv. Chookyoupjaso were irradiated with 200 Gy gamma ray to generate mutagenesis. The aim of this study is to investigate the effects of a hexane extract from Perilla frutescens (L.) Britt. cv. Chookyoupjaso mutant 45 on the actions of anti-inflammatory activity on inducible nitric oxide synthase, and an identification of the major active compound. The hexane extract from P. frutescens exhibited activity of inhibition of a NO production ($IC_{50}$, $295.1{\mu}g\;ml^{-1}$). The hexane extract was further divided into subfractions by silica-gel chromatogarphy. Inhibition of the NO production by various fractions was assayed in LPS-stimulated RAW 264.7 cells. Among the seven fractions, the 5th fraction was the most effective ($IC_{50}$, $19.5{\mu}g\;ml^{-1}$). The 5th fraction suppressed the expression of protein of iNOS in LPS-induced RAW 264.7 cells, and GC/MS analyses showed that isoegomaketone is a major bio-active compound in the 5th fraction. The result indicated that isoegomaketone has a good potential to be developed as an anti-inflammation agent.
Journal of the Society of Cosmetic Scientists of Korea
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v.45
no.2
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pp.117-129
/
2019
In this study Anti-inflammatory activity was investigated for the extract of Prunus pendula for. ascendens (Makino) Ohwi by monitoring nitric oxide (NO) production in LPS-stimulated RAW 264.7 murine macrophage cells. The P. pendula ethyl acetate (EtOAc) fraction showed to decrease the NO synthesis by 76.3% at $100{\mu}g/mL$ concentration. The inhibition occurred in a dose-dependent manner without causing cell toxicity. The EtOAc fraction also inhibited the production of $PGE_2$, $IL-1{\beta}$, IL-6 and expression of iNOS, COX-2 protein in dose-dependent manner. From the phytochemical study to isolate the active constituents, five known compounds were identified, which are ursolic acid (1), prunasin (2), methyl p-coumarate (3), kaempferol (4), astragalin (5). All of the compounds 1 - 5 were isolated for the first time from the P. pendula. Among the isolates, the flavonoids 4 and 5 were verified to inhibit NO production with high efficiency. These results suggested that extract of P. pendula leaves could be useful as anti-inflammatory agents in pharmaceutical or cosmetic applications.
HK shiitake mushroom mycelium (HKSMM), containing 14% β-glucan, is a health functional food ingredient approved individually for liver health by the Ministry of Food and Drug Safety. The immune-enhancing efficacy of a 50% aqueous ethanol extract of HKSMM (designated HKSMM50) was studied in Jurkat cells activated with concanavalin A (ConA). Active hexose correlated compound (AHCC) was used as a positive control. ConA-activated Jurkat cells were treated with HKSMM50 (0, 25, 50, 100 ㎍ g/ml) or AHCC (100 ㎍ g/ml), and cultured for 3 and 6 hours. The nuclear factor of activated T cells (NFAT) protein content in the cytosol and the nucleus was measured by Western blotting. Interleukin-2 (IL-2), interferon-gamma (IFN-γ), and cyclooxygenase-2 (COX-2) were determined using enzyme-linked immunosorbent assay (ELISA) kits. HKSMM50 lowered NFAT content in the cytosol, but elevated NFAT content in the nucleus. The IL-2 and IFN-γ productions were elevated. Meanwhile, both COX-2 activity and apoptosis were suppressed. The efficacy of the AHCC treatment showed similar to those of HKSMM50 treatments. These results indicate that the HKSMM50 exhibited immune-enhancing effects in ConA-treated Jurkat cells by activation of NFAT protein, and suggest that HKSMM could be used as a health functional food ingredient to improve immune functions in humans.
Pepper mild mosaic virus(PMMoV) and Cucumber mosaic virus (CMV) are important pathogens in various vegetable crops worldwide. We have found that hot water extract of Phellinus linteus mycelium strongly inhibit PMMoV and CMV infection. Based on these results, the inhibitor named as 'PLM-WE1' formulated from extract of Phellinus linteus mycelium was tested for its inhibitory effects on PMMoV and CMV infection to each local lesion host plant (Nicotiana glutinosa: PMMoV, Chenopodium amaranticolor: CMV). Pretreatment effect of PLM-WE1 against infections of each virus (PMMoV and CMV) to local host plant was measured to be 99.2% to PMMoV and 80.3% to CMV, and its permeability effect was measured to be 45.0% to PMMoV and 41.9% to CMV. Duration of inhibitory activity of PLM-WE1 against PMMoV infection on N. glutinosa was maintained for 3 days at 75% inhibition level and CMV infection on C. amaranticolor maintained for 3 days at 62% inhibition level. Inhibitory effects on systemic host plants of PLM-WE1 were measured to be 75~85% to PMMoV and 75% to CMV. Under electron microscope, PMMoV particles were not denatured or aggregated by mixing PLM-WE1. It is suggested that the mode of action of PLM-WE1 differ from that of inactivation due to the aggregation of viruses. The methanol extract of P. linteus mycelium was sequentially partitioned with haxane, ethyl acetate, BuOH and $H_2O$. The $H_2O$ fraction was showed high activity than the other fractions. The active compound was isolated with a partial acid hydrolysis, fractional precipitation with ethanol. The inhibitory effect of the precipitate isolated from 70% ethanol fraction was 99.1% to PMMoV and 88.0% to CMV. The structure of isolated compound was determined by $^1H$-NMR and $^{13}C$-NMR. This compound was identified as a polysaccharide consisting alpha or beta-glucan.
Journal of the Korean Society of Food Science and Nutrition
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v.21
no.4
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pp.353-366
/
1992
This study was devised to purify the compound from tuna that have cytotoxic activities against various cancer cell lines and to observe its immunopotentiating activities. The cytotoxic compound was partially purified 277 fold, from petroleum ehter extract (crude extract) of tuna by silicic acid column chromatography (fraction D) and thin layer chromatography (Spot I). Cytotoxic activity was monitored using human colon cancer cell, HCT-48. The active compound (Spot I) was composed of seven materials which are fatty acids of four kinds ($C_{14:0},\;C_{16:0},\;C_{17:1},\;and\;C_{18:0}$) and unknown three fat materials. The active compound has cytotoxic activities against various cancer cell lines, that is, murine leukemic lymphocytes (L1210, P388) and human rectal (HRT-18) and colon cancer cells (HCT-48, HT-29). The patterns of size distribution of HCT-48 cells in the medium containing tuna extract were shifted to direction of the small size region. Also, the microscopic shape of HCT-48 cells were shrinked and distracted. The number of plaque forming cell and immunoglobin fraction of serum protein obtained from tuna-treated mice were increased, but natural killer cell activity was not affected.
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