• 제목/요약/키워드: Biological screening methods

검색결과 123건 처리시간 0.028초

Biological Screening of Novel Derivatives of Valproic Acid for Anticancer and Antiangiogenic Properties

  • Farooq, Muhammad;El-Faham, Ayman;Khattab, Sherine N.;Elkayal, Ahmed M.;Ibrahim, Mahmoud F.;Taha, Nael Abu;Baabbad, Almohannad;Wadaan, Mohammad A.M.;Hamed, Ezaat A.
    • Asian Pacific Journal of Cancer Prevention
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    • 제15권18호
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    • pp.7785-7792
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    • 2014
  • Background: Valproic acid (VPA) is a potent anticancer and antiangiogenic agent. However, design and synthesis of chemical derivatives with improved antiangiogenic and anticancer activities are still necessary. In this study a library of novel derivatives of VPA was synthesized and tested. Methods: A human liver cancer cell line (HepG2) and a human normal embryonic kidney cell line (HEK 293) were exposed to various concentrations of VPA derivatives for 24 hours and cell viability was checked by MTT colorimetric assay. Anti-angiogenic properties were evaluated in transgenic zebrafish embryos. Results: N-valproylglycine derivatives suppressed survival almost 70% (p value 0.001) in HepG2 cells but only 10-12% in HEK 293 cells (p value 0.133). They also suppressed angiogenic blood vessel formation by 80% when used between $2-20{\mu}M$ in zebrafish embryos. Valproic acid hydrazides showed moderate level of anticancer activity by affecting 30-50% (p value 0.001) of cell viability in HepG2 cells and 8-10% in HEK293 cells (p value 0.034). Conclusion: The majority of compounds in this study showed potent and stronger antiangiogenic and anticancer activity than VPA. They proved selectively toxic to cancer cells and safer for normal cells. Moreover, these compounds inhibited developmental angiogenesis in zebrafish embryos. Based on the fact that liver is a highly vascularized organ, in case of liver carcinoma these compounds have the potential to target the pathological angiogenesis and could be an effective strategy to treat hepatocellular carcinoma.

Pseudomonas aeruginosa KS47에 의한 절삭유의 생물학적 분해 (Biodegradation of Cutting Oil by Pseudomonas aeruginosa KS47)

  • 김란희;이상섭
    • 미생물학회지
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    • 제44권1호
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    • pp.22-28
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    • 2008
  • 본 실험은 생분해가 어려운 절삭유를 단일 균주에 의해 생물학적 처리를 하는 데에 목적이 있다. 절삭유, 절삭폐유로부터 호기 균주 81개를 분리하여 이중 절삭유 분해능이 가장 높은 균주로, 48시간 내에 90.4%를 제거한(초기농도 699.1 mg/L) KS47을 선별하였다. KS47은 형태학적, 생리 화학적, 16S rDNA 염기서열, 그리고 지방산 분석을 통해 Pseudomonas aeruginosa로 동정되었다. P. aeruginosa KS47은 절삭유를 탄소원으로 사용하여 성장 할 수 있었으며, 절삭유 분해시, 최적 분해 조건은 1.5 g/L(wet weight), pH 7.0, $30^{\circ}C$이었다. 최적 조건 하에서 절삭유의 제거능을 본 결과, 1,060 mg/L의 절삭유를 12시간 내에 83.7% 제거함을 확인하였다.

이진탕가미방(二陳湯加味方)의 역류성(逆流性) 식도염(食道炎) 억제효과(抑制效果) (Suppressive Effects of Yijintang-gamibang on Reflux Esophagitis)

  • 최빈혜;곽민아;김대준;변준석
    • 대한한의학회지
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    • 제31권5호
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    • pp.64-81
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    • 2010
  • Objectives: The object of this study was to observe the suppressive effects of Yijintang-gamibang (YJGMB), Yijintang being traditionally used in the Korean Medicine for treating various digestive diseases, on the rat reflux esophagitis (RE) as compared with omeprazole, a well-known proton pump inhibitor. Methods: Three different dosages of YJGMB, 50, 100 and 200 mg/kg, were orally pretreated once a day for 28 days before pylorus and forestomach ligation. Seven groups of 8 rats each were used in the study. Six hrs after pylorus and forestomach ligation, changes to the stomach and esophagus lesion areas, gastric volumes, acid and pepsin outputs, invasive lesion percentages, fundic mucosa, esophageal submucosa and total thicknesses were measured by histomorphometry. The results were compared with omeprazole 10 and 30 mg/kg treated groups in which the effects on RE were already confirmed. Results: As results of pylorus and forestomach ligation, marked increases of esophageal and gastric mucosa lesion areas, gastric volumes, acid outputs, pepsin outputs were observed with histopathological changes of RE, such as hemorrhages, ulcerative lesions and edematous changes on the esophageal and fundic mucosa. However, these pylorus and forestomach ligation induced RE were dose-dependently inhibited by treatment of 50, 100 and 200 mg/kg of YJGMB. YJGMB 50 mg/kg showed similar suppressive effects as 30 mg/kg of omeprazole, but more favorable effects were observed as compared with omeprazole 10 mg/kg. Conclusion: The results suggest that YJGMB showed favorable suppressive effects on the RE induced by pylorus and forestomach ligation. It is therefore expected that YJGMB will show favorable effects on RE as corresponds to the suggestion of traditional Korean medicine. However, more detailed mechanism studies should be conducted in future with the screening of the biological active chemical compounds in herbs.

귀비탕(歸脾湯)이 비소세포 폐암세포(NCI-H520) 이식 마우스에서 악액질 억제에 미치는 영향 (Anticachexic Effects of Kwibi-tang on Non-small Cell Lung Carcinoma, NCI-H520 Xenograft Mice)

  • 손지영;김경순;최해윤;김종대
    • 대한암한의학회지
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    • 제20권2호
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    • pp.23-36
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    • 2015
  • Purpose : The object of this study was to observe anti-cachexic effects of Kwibi-tang extracts (KBTe) on non-small cell lung carcinoma (squamous epithelial carcinoma), NCI-H520, xenograft Balb/c nu-nu nude mice. Methods : Three different dosages of KBTe, 50, 100 and 200 mg/kg were orally administered once a day for 42 days from 11 days after tumor cell inoculation. Six groups, each of 8 mice per group were used in the present study. Changes on the body weight, the epididymal fat weight and serum IL-6 levels were detected with the thicknesses of deposited cervical brown adipose tissue and their mean diameters to monitor the tumor-related anticachexic effects. Results : Deceases on the body weight and gains were also demonstrated in tumor-bearing control with increases of serum IL-6 levels, decreases of epididymal fat pad weight, atrophic changes of cervical brown adipose tissues. These are means that tumor-related cachexia are induced by tumor cell inoculations in the present study. However, these tumor-related cachexia were markedly inhibited by all three different dosages of KBTe treatment as compared with tumor-bearing control. 5-FU showed somewhat deteriorated the tumor-related cachexia in the present study. Conclusion : The results obtained in this study suggest that over 50 mg/kg of KBTe showed favorable anticachexic effects on the NCI-H520 cell xenograft. However, detail mechanism studies should be conducted in future with the screening of the biological active compounds in this herb.

A Putative Transcription Factor pcs1 Positively Regulates Both Conidiation and Sexual Reproduction in the Cereal Pathogen Fusarium graminearum

  • Jung, Boknam;Park, Jungwook;Son, Hokyoung;Lee, Yin-Won;Seo, Young-Su;Lee, Jungkwan
    • The Plant Pathology Journal
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    • 제30권3호
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    • pp.236-244
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    • 2014
  • The plant pathogen Fusarium graminearum causes Fusarium head blight in cereal crops and produces mycotoxins that are harmful to animals and humans. For the initiation and spread of disease, asexual and sexual reproduction is required. Therefore, studies on fungal reproduction contribute to the development of new methods to control and maintain the fungal population. Screening a previously generated transcription factor mutant collection, we identified one putative $C_2H_2$ zincfinger transcription factor, pcs1, which is required for both sexual and asexual reproduction. Deleting pcs1 in F. graminearum resulted in a dramatic reduction in conidial production and a complete loss of sexual reproduction. The pathways and gene ontology of pcs1-dependent genes from microarray experiments showed that several G-protein related pathways, oxidase activity, ribosome biogenesis, and RNA binding and processing were highly enriched, suggesting that pcs1 is involved in several different biological processes. Further, overexpression of pcs1 increased conidial production and resulted in earlier maturation of ascospores compared to the wild-type strain. Additionally, the vegetative growth of the overexpression mutants was decreased in nutrient-rich conditions but was not different from the wild-type strain in nutrient-poor conditions. Overall, we discovered that the pcs1 transcription factor positively regulates both conidiation and sexual reproduction and confers nutrient condition-dependent vegetative growth.

Photoluminescent Graphene Oxide Microarray for Multiplex Heavy Metal Ion Analysis

  • Liu, Fei;Ha, Hyun Dong;Han, Dong Ju;Park, Min Su;Seo, Tae Seok
    • 한국진공학회:학술대회논문집
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    • 한국진공학회 2013년도 제45회 하계 정기학술대회 초록집
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    • pp.281.2-281.2
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    • 2013
  • Since heavy metal ions included in water or food resources have critical effects on human health, highly sensitive, rapid and selective analysis for heavy metal detection has been extensively explored by means of electrochemical, optical and colorimetric methods. For example, quantum dots (QDs), such as semiconductor QDs, have received enormous attention due to extraordinary optical properties including high fluorescence intensity and its narrow emission peaks, and have been utilized for heavy metal ion detection. However, the semiconductor QDs have a drawback of serious toxicity derived from cadmium, lead and other lethal elements, thereby limiting its application in the environmental screening system. On the other hand, Graphene oxide (GO) has proven its superlative properties of biocompatibility, unique photoluminescence (PL), good quenching efficiency and facile surface modification. Recently, the size of GO was controlled to a few nanometers, enhancing its optical properties to be applied for biological or chemical sensors. Interestingly, the presence of various oxygenous functional groups of GO contributes to opening the band gap of graphene, resulting in a unique PL emission pattern, and the control of the sp2 domain in the sp3 matrix of GO can tune the PL intensity as well as the PL emission wavelength. Herein, we reported a photoluminescent GO array on which heavy metal ion-specific DNA aptamers were immobilized, and sensitive and multiplex heavy metal ion detection was performed utilizing fluorescence resonance energy transfer (FRET) between the photoluminescent monolayered GO and the captured metal ion.

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Antibacterial activity of florfenicol composite nanogels against Staphylococcus aureus small colony variants

  • Liu, Jinhuan;Ju, Mujie;Wu, Yifei;Leng, Nannan;Algharib, Samah Attia;Luo, Wanhe
    • Journal of Veterinary Science
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    • 제23권5호
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    • pp.78.1-78.13
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    • 2022
  • Background: Florfenicol might be ineffective for treating Staphylococcus aureus small colony variants (SCVs) mastitis. Objectives: In this study, florfenicol-loaded chitosan (CS)-sodium tripolyphosphate (TPP) composite nanogels were prepared to allow targeted delivery to SCV infected sites. Methods: The formulation screening, the characteristics, in vitro release, antibacterial activity, therapeutic efficacy, and biosafety of the florfenicol composite nanogels were studied. Results: The optimized formulation was obtained when the CS and TPP were 10 and 5 mg/mL, respectively. The encapsulation efficiency, loading capacity, size, polydispersity index, and zeta potential of the optimized florfenicol composite nanogels were 87.3% ± 2.7%, 5.8% ± 1.4%, 280.3 ± 1.5 nm, 0.15 ± 0.03, and 36.3 ± 1.4 mv, respectively. Optical and scanning electron microscopy showed that spherical particles with a relatively uniform distribution and drugs might be incorporated in cross-linked polymeric networks. The in vitro release study showed that the florfenicol composite nanogels exhibited a biphasic pattern with the sustained release of 72.2% ± 1.8% at 48 h in pH 5.5 phosphate-buffered saline. The minimal inhibitory concentrations of commercial florfenicol solution and florfenicol composite nanogels against SCVs were 1 and 0.25 ㎍/mL, respectively. The time-killing curves and live-dead bacterial staining showed that the florfenicol composite nanogels were concentration-dependent. Furthermore, the florfenicol composite nanogels displayed good therapeutic efficacy against SCVs mastitis. Biological safety studies showed that the florfenicol composite nanogels might be a biocompatible preparation because of their non-toxic effects on the renal tissue and liver. Conclusions: Florfenicol composite nanogels might improve the treatment of SCV infections.

네트워크 약리학을 이용한 윤폐환(潤肺丸)의 COPD 치료 효능 및 작용기전 연구 (Network Pharmacology-based Prediction of Efficacy and Mechanism of Yunpye-hwan Acting on COPD)

  • 김민주;양아람;권빛나;김동욱;배기상
    • 대한본초학회지
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    • 제39권3호
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    • pp.37-47
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    • 2024
  • Objectives : Because predicting the potential efficacy and mechanisms of Korean medicines is challenging due to their high complexity, employing an approach based on network pharmacology could be effective. In this study, network pharmacological analysis was utilized to anticipate the effects of YunPye-Hwan (YPH) in treating Chronic obstructive pulmonary disease (COPD). Methods : Compounds and their related target genes of YPH were gathered from the TCMSP and PubChem databases. These target genes of YPH were subsequently compared with gene sets associated with COPD to assess correlation. Next, core genes were identified through a two-step screening process, and finally, functional enrichment analysis of these core genes was conducted using both Gene Ontology (GO) enrichment analysis and Kyoto Encyclopedia of Genes and Genomes (KEGG) Pathways. Results : A total of 15 compounds and 437 target genes were gathered, resulting in a network comprising 473 nodes and 14,137 edges. Among them, 276 genes overlapped with gene sets associated with COPD, indicating a significant correlation between YPH and COPD. Functional enrichment analysis of the 18 core genes revealed biological processes and pathways such as "miRNA Transcription," "Nucleic Acid-Templated Transcription," "DNA-binding Transcription Factor Activity," "MAPK signaling pathway," and "TNF signaling pathway" were implicated. Conclusion : YPH exhibited significant relevance to COPD by modulating cell proliferation, differentiation, inflammation, and cell death pathways. This study could serve as a foundational framework for further research investigating the potential use of YPH in the treatment of COPD.

Depression, sleep quality, and body image disturbances among pregnant women in India: a cross-sectional study

  • Kranti S. Kadam;Aditya R. Anvekar;Vishnu B. Unnithan
    • Journal of Yeungnam Medical Science
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    • 제40권4호
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    • pp.394-401
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    • 2023
  • Background: Pregnancy is associated with a number of physical, emotional, and biological changes that can exacerbate maternal psychological disturbances, such as body image concerns and depression. Sleep disturbances during pregnancy can also have adverse impacts. This study aimed to determine the prevalence of depression, sleep disturbances, and body image concerns among pregnant women. The study also examined the relationship between these factors and pregnancy-related variables, such as bad obstetric history and whether the pregnancies were unplanned. Methods: A cross-sectional study of 146 pregnant patients was conducted at a tertiary care center over 15 months. The patients were administered the Beck Depression Inventory, Pittsburgh Sleep Quality Index, and Body Image Concern Inventory questionnaires. Contingency tables, Fisher exact test, and Spearman correlation were used to identify underlying relationships. Results: The prevalence of depression was 22.6%. Although body image disturbance was noted in only 2.7% of patients, 46.6% had poor sleep quality. Poor sleep was associated with primigravida status. Bad obstetric history and unplanned pregnancy were associated with depression. Depression was found to be significantly correlated with body image disturbances and poor sleep quality. Conclusion: Psychiatric disorders were prevalent during pregnancy. This study highlights the importance of screening for depression in pregnant patients. Counselling and caregiver education can be useful for mitigating psychological disturbances. Management of pregnancies by multidisciplinary teams that include psychiatrists could be immensely useful in improving the pregnancy experiences of patients.

네트워크 약리학 방법을 이용한 위장관 운동성 장애 관련 마늘의 효능 분석 (Analysis of the Effectiveness of Garlic on Gastrointestinal motility disorders using a network pharmacological method)

  • 최나리;김병주
    • 대한한의학방제학회지
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    • 제31권4호
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    • pp.245-252
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    • 2023
  • Objectives : The purpose of this study was to explore the compounds, targets and related diseases of garlic by the approaches of network pharmacology and bioinformatics in traditional chinese medicine. Methods : We investigated components and their target molecules of garlic using SymMap and TCMSP and they were compared with analysis platform. Results : 56 potential compounds were identified in garlic, 26 of which contained target information, and it was found that these 26 compounds and 154 targets interact with each other through a combination of 243 compounds. In addition, Apigenin was linked to the most targeted gene (78) in 26 compounds, followed by Kaempferol (61 genes), Nicotic Acid (14 genes), Geraniol (11 genes), Eee (10 genes), and Sobrol A (9 genes). Among 56 potential compounds, three compounds (Kaempferol, Dipterocarpol, and N-Methyl cytisine) corresponded to the active compound by screening criterion Absorption, Distribution, Metabolism, Excretion (ADME). In addition, 12 compounds in 56 potential compounds were associated with gastrointestinal (GI) motility disorder. Among them, Kaempferol was a compound that met the ADME parameters and the rest were potential compounds that did not meet. Also, Kaempferol was closely related to GI motility disorder, indicating that this Kaempferol could be a candidate for potential medical efficacy. Conclusions : It shows the relationship between the compound of garlic, an herbal supplement, and the biological process associated with GI motility disorder. These results are thought to help develop strategies for treating GI motility disorders.