• Title/Summary/Keyword: active compound

Search Result 968, Processing Time 0.026 seconds

Antibacterial Activity of Salvia Miltiorrhiza against Methicillin-resistant Staphylococcus aureus (丹參의 methicillin 내성 황색포도구균에 대한 효과)

  • Seo, Myung-won;Jeong, Seung-il;Shin, Chol-gyun;Ju, Young-sung;Kim, Hong-jun;Ko, Byoung-seob
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
    • /
    • v.16 no.1
    • /
    • pp.94-99
    • /
    • 2003
  • Objectives : Gram-positive bacteria have became increasing resistant to antibacterial agents, and hence multi-drug-resistant bacterial pathogens are now a major problem in clinical medicine. There is, therefore, a need for new antibacterial agents. In the course of our screening program for potent antibacterial agent from medicinal plants, the extract of Salvia miltiorrhiza (S. miltiorrhiza) showed antibacterial activity against methcillin resistant Staphylococcus aureus (MRSA) and antibiotic-resistant S. aureus. Methods : S. miltiorrhiza was extracted with 80$\%$ EtOH. The extract was suspended in H2O and fractionated successively with hexane chloroform, ethyl acetate, and n-buthanol. The chloroform fraction, which showed the highest antibacterial activity(MICs, 78㎍/ml) against MRSA, was chromatographed on a silica gel column and recycling prep-LC to give the pure antibacterial component. Results and Conclusions : The second fraction among the chloroform soluble portion of an aqueous EtOH extract of S. miltiorrhiza root showed outstanding antibacterial activity against MRSA and antibiotic-resistant S. aureus compared to the other fraction. An active compound was isolated from the second fraction using silica gel column chromatoraphy and recycling prep-LC. Based on these data together with the IH-, 13C-NMR, mass and mp, the active compounds were identified tanshinone Ⅰ, dehydrotanshinone Ⅰ and cryptotanshinone. Among tanshinones, cryptotanshinone and dihydrotanshinone Ⅰ MICs against MRSA and antibiotics-resistant S. aureus were 12.5, 12.5 and 6.3㎍/ml, respectively.

  • PDF

Antimalarial Activity and Phytochemical Profile of Ethanolic and Aqueous Extracts of Bidara Laut (Strychnos ligustrina Blum) Wood

  • MANURUNG, Harisyah;SARI, Rita Kartika;SYAFII, Wasrin;CAHYANINGSIH, Umi;EKASARI, Wiwied
    • Journal of the Korean Wood Science and Technology
    • /
    • v.47 no.5
    • /
    • pp.587-596
    • /
    • 2019
  • This study aimed to determine the antimalarial effect of the Strychnos ligustrina (SLW) wood extracts and to analyze its phytochemicals. The SLW powder samples were macerated with 100% ethanol (E100), 75% ethanol (E75), 50% ethanol (E50), 25% ethanol (E25), and aqueous (A100). The extracts were analyzed by LCMS/MS, and its in-vitro antimalarial activity was tested with Plasmodium falciparum. The results showed that the extract yields of E100, E75, E50, E25, and A100 were 4.3, 5.2, 5.3, 4.7, and 3.6%, respectively. The antimalarial activities of the A100, E25, E50, and E75 extracts were classified as active with $IC_{50}$ values of 38.6, 42.6, 42.9, and $43.7{\mu}g/mL$, respectively. But, the antimalarial activity of the E100 extract was classified as slightly active with $IC_{50}$ values of $87.4{\mu}g/mL$. The dominant compounds contained in the extracts of A100, E25, E50, E75, and E100 was the alkaloid compound, namely brucine with relative concentrations of 24.96, 24.55, 21.33, 11.79, and 11.62%, respectively.

A study on Antibacterial Activity of Samsinhwan Ethanol Extract against MRSA (삼신환(三神丸) 에탄올 추출물(SSH)의 MRSA에 대한 항균활성 연구)

  • Woo, Haksik;Lee, Yeoung Ju
    • Journal of Digital Convergence
    • /
    • v.17 no.8
    • /
    • pp.271-282
    • /
    • 2019
  • The purpose of this study is to identify the antimicrobial effects of SSH(三神丸) and synerggy effects of the existing antibiotics Oxacillin and Ciprofloxacin on MRSA and to identify the mechanisms. In this case, the procedure and method for verifying anti-bacterial activity and active concentration of MARA by measuring the minimum inhibitory concentration (MIC) of the trichin is used to verify the potency and active concentration of MARA, to confirm the potency of the disease by treating antibiotics and trichine ethanol extract in parallel, and to confirm the anti-bacterial effect over time, when the trichine is activated as an anti-bacterial activity to MARA, and a compound. In addition, we hope that this research will not only serve as meaningful data for the development of new drugs to control MARA immunity, but also serve as an opportunity to further accelerate the research and development of antibiotics to overcome resistant strains.

Anti-nociceptive and Anti-inflammatory Properties of Ilex latifolia and its Active Component, 3,5-Di-caffeoyl Quinic Acid Methyl Ester

  • Kim, Joo Youn;Lee, Hong Kyu;Seong, Yeon Hee
    • Natural Product Sciences
    • /
    • v.25 no.1
    • /
    • pp.64-71
    • /
    • 2019
  • The present study was conducted to investigate anti-nociceptive and anti-inflammatory effects of the leaves of Ilex latifolia Thunb (I. latifolia) in in vivo and in vitro. Writhing responses induced by acetic acid and formalin- and thermal stimuli (tail flick and hot plate tests)-induced pain responses for nociception were evaluated in mice. I. latifolia (50 - 200 mg/kg, p.o.) and ibuprofen (100 mg/kg, p.o.), a positive non-steroidal anti-inflammatory drug (NSAID), inhibited the acetic acid-induced writhing response and the second phase response (peripheral inflammatory response) in the formalin test, but did not protect against thermal nociception and the first phase response (central response) in the formalin test. These results show that I. latifolia has a significant anti-nociceptive effect that appears to be peripheral, but not central. Additionally, I. latifolia (50 and $100{\mu}g/mL$) and 3,5-di-caffeoyl quinic acid methyl ester ($5{\mu}M$) isolated from I. latifolia as an active compound significantly inhibited LPS-induced NO production and mRNA expression of the pro-inflammatory mediators, iNOS and COX-2, and the pro-inflammatory cytokines, IL-6 and $IL-1{\beta}$, in RAW 264.7 macrophages. These results suggest that I. latifolia can produce antinociceptive effects peripherally, but not centrally, via anti-inflammatory activity and supports a possible use of I. latifolia to treat pain and inflammation.

Basic network pharmacological analysis of Salvia miltiorrhiza root for further application to an animal stroke model (단삼(丹參)을 뇌졸중 동물모델에 적용하기 위한 기초적인 네트워크 약리학 분석)

  • Choi, Myeongjin;Yang, Wonjin;Lee, Byoungho;Cho, Suin
    • Herbal Formula Science
    • /
    • v.29 no.1
    • /
    • pp.19-31
    • /
    • 2021
  • Objectives : The root of Salvia miltiorrhiza, known as 'Dansam (DS, 丹參)', is used for and treating cardiovascular diseases based on its efficacy of promoting blood circulation and breaking through a blood stasis. In this study, we would like to see if DS could be effectively used for stroke from the perspective of network pharmacology. Methods : The analysis was conducted using Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP) database to derive the main active compounds of DS and identify the mechanism of each compound acting on the human body. The networks between compounds, target protein and disease were expressed through Cytoscape. Protein-protein interaction (PPI) analysis was performed using STRING database. Results : Fifty two active compounds of DS were identified by screening the ingredients of DS through TCMSP. Based on the networks of these compounds with target protein and disease, it can be said that DS might be effective for preventing and treating stroke. PPI result showed that adrenergic receptor has many interactions among proteins, indicating its significance in stroke pathway. Conclusion : In this study, we derived target proteins and target diseases of DS that could be used in study of stroke. However, since it is uncertain if these targets can be controlled by DS extracts or not, we would like to confirm the results with further animal experiments.

In-vitro Antimalarial Investigations and Molecular Docking Studies of Compounds from Trema orientalis L. (blume) Leaf Extract

  • Samuel, Babatunde Bolorunduro;Oluyemi, Wande Michael;Okedigba, Ayoyinka Oluwaseun
    • Natural Product Sciences
    • /
    • v.28 no.2
    • /
    • pp.45-52
    • /
    • 2022
  • The identification of Plasmodium falciparum enoyl acyl-carrier protein reductase (pfENR) is considered as a potential biological target against malaria. Trema orientalis is considered a rich source of phytochemicals useful in malaria treatment. This study evaluated the in-vitro inhibitory activity of the extract and isolated compounds of T. orientalis leaf; the isolated compounds and the analogues of the most active compound were subjected to in-silico molecular docking studies on pfENR. The methanolic extract of T. orientalis was subjected to repeated chromatographic separation which led to the isolation of some compounds. The isolated compounds from the plant were examined for their antimalarial activity using β-hematin inhibition assay. Virtual screening via molecular docking and ADMET studies were conducted to gain insight into the mechanism of binding of ligand and to identify effective pfENR inhibitors. The isolated compounds and the analogues of the most active isolates were gotten from PubChem library for use in docking study. Hexacosanol and β-sitosterol showed inhibition of the β-hematin formation. The docking results showed that hexacosanol, β-sitosterol and the analogues of β-sitosterol displayed binding energy ranging between -6.1 kcal/mol and -11.6 kcal/mol. Sitosterol glucoside has the highest docking score. Some of the ligands showed more binding affinity than known bioactive compounds used as reference. Analogues of β-sitosterol has been shown to be potential inhibitors of pfENR, therefore, the findings from this study suggest that sitosterol glucoside and ergosterol peroxide could act as antimalarial agents after further lead optimisation investigations.

Identifying the Anti-Cancer Effect of Indigo Naturalis in Small Cell Lung Cancer Based on Network Pharmacological Analysis (네트워크 약리학적 분석에 의한 소세포폐암에 대한 청대의 항암기전 연구)

  • Young Hoon, Kim;Woo Jin, Jeong;Gwang Hee, Jeong;Youn Sook, Kim;Won Gun, An
    • Journal of Physiology & Pathology in Korean Medicine
    • /
    • v.36 no.6
    • /
    • pp.229-234
    • /
    • 2022
  • Lung cancer is the leading cause of cancer-related deaths worldwide. Indigo Naturalis (IN) is a dark blue powder obtained by processing leaves or stems of indigo plants, its anticancer effects have been reported in several studies. However, the pharmacological mechanism of IN in small cell lung cancer (SCLC) is not elucidated. In this study, to investigate the anticancer efficacy of IN for SCLC, we presented potential active ingredients, SCLC-related targets, and pharmacological mechanisms of IN that are expected to have anticancer activity for SCLC using a network pharmacological analysis. The phytochemical compounds of IN have been collected through TCMSP, SymMap, or HPLC documents. The active ingredients of IN such as indirubin, indican, isatin, and tryptanthrin were selected through ADME parameters or literature investigations for each compound. Using the Compounds, Disease-Target associations Databases, 124 common targets of IN and SCLC were obtained. Gene Ontology (GO), Kyoto Encyclopedia of Genes and Genomes (KEGG) Pathway enrichment analysis was carried out. GO biological processes are associated with response to xenobiotic stimulus, positive regulation of protein phosphorylation, regulation of mitotic cell cycle, and regulation of apoptotic signaling pathway. KEGG disease pathways included Gastric cancer, Bladder cancer, SCLC, and Melanoma. The main anticancer targets of the IN for SCLC were analyzed in 14 targets, including BCL2, MYC, and TP53. In conclusion, the results of this study based on the network pharmacology of IN can provide important data for the effective prevention and treatment of SCLC.

Gynostemma pentaphyllum extract and its active component gypenoside L improve the exercise performance of treadmill-trained mice

  • Kim, Yoon Hee;Jung, Jae In;Jeon, Young Eun;Kim, So Mi;Hong, Su Hee;Kim, Tae Young;Kim, Eun Ji
    • Nutrition Research and Practice
    • /
    • v.16 no.3
    • /
    • pp.298-313
    • /
    • 2022
  • BACKGROUND/OBJECTIVES: The effectiveness of natural compounds in improving athletic ability has attracted attention in both sports and research. Gynostemma pentaphyllum (Thunb.) leaves are used to make traditional herbal medicines in Asia. The active components of G. pentaphyllum, dammarane saponins, or gypenosides, possess a range of biological activities. On the other hand, the anti-fatigue effects from G. pentaphyllum extract (GPE) and its effective compound, gypenoside L (GL), remain to be determined. MATERIALS/METHODS: This study examined the effects of GPE on fatigue and exercise performance in ICR mice. GPE was administered orally to mice for 6 weeks, with or without treadmill training. The biochemical analysis in serum, glycogen content, mRNA, and protein expressions of the liver and muscle were analyzed. RESULTS: The ExGPE (exercise with 300 mg/kg body weight/day of GPE) mice decreased the fat mass percentage significantly compared to the ExC mice, while the ExGPE showed the greatest lean mass percentage compared to the ExC group. The administration of GPE improved the exercise endurance and capacity in treadmill-trained mice, increased glucose and triglycerides, and decreased the serum creatine kinase and lactate levels after intensive exercise. The muscle glycogen levels were higher in the ExGPE group than the ExC group. GPE increased the level of mitochondrial biogenesis by enhancing the phosphorylation of peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α) protein and the mRNA expression of nuclear respiratory factor 1, mitochondrial DNA, peroxisome proliferator-activated receptor-δ, superoxide dismutase 2, and by decreasing the lactate dehydrogenase B level in the soleus muscle (SOL). GPE also improved PGC-1α activation in the SOL significantly through AMPK/p38 phosphorylation. CONCLUSIONS: These results showed that GPE supplementation enhances exercise performance and has anti-fatigue activity. In addition, the underlying molecular mechanism was elucidated. Therefore, GPE is a promising candidate for developing functional foods and enhancing the exercise capacity and anti-fatigue activity.

Comparative Analysis of Phenolic Compound of Mutant Lines of Sorghum (Sorghum bicolor)

  • Ye-Jin Lee;Baul Yang;Dong-Gun Kim;Sang Hoon Kim;Soon-Jae Kwon;Jae Hoon Kim;Joon-Woo Ahn;Chang-Hyu Bae;Jaihyunk Ryu
    • Proceedings of the Plant Resources Society of Korea Conference
    • /
    • 2022.09a
    • /
    • pp.86-86
    • /
    • 2022
  • Sorghum (Sorghum bicolor) is increasingly important as a biomass crop worldwide. Its genetic diversity provides a large range of biochemical composition suitable for various uses as bioplastics. Phenolic compounds are the main compounds of lignocellulosic residues, which can be used as a source of active components for their use in active packaging materials. In this research, we investigated the total phenolic content (TPC) and the total flavonoid content (TFC) among 60 mutant lines (early heading, high biomass and dwarfness) and their original cultivars. Sixty sorghum mutant lines were developed by treatment with gamma-ray or proton irradiation in 14 sorghum cultivars. The levels of TPC and TFC of 14 original cultivars were ranging from 3.27 to 11.54 mg/100 g and 2.39 to 6.74 mg/100 g, respectively. The TPCs of the mutant lines were ranging from 1.92 to 13.10 mg/100 g with average content of 6.35 mg/100 g. The TFCs of the mutant lines were ranging from 1.72 to 8.30 mg/100 g with average content of 4.20 mg/100 g. Three mutant lines derived from gamma-ray showed significant lower TPC and TFC than those of the original cultivar. While, five mutant lines showed significant higher TPC and TFC. These findings will be useful for the selection of sorghum genotypes with improved phenolic compounds.

  • PDF

Inhibition of Developmental Processes by Flavone in Caenorhabditis elegans and Its Application to the Pinewood Nematode, Bursaphelenchus xylophilus

  • Lee, Yong-Uk;Kawasaki, Ichiro;Lim, Yoongho;Oh, Wan-Suk;Paik, Young-Ki;Shim, Yhong-Hee
    • Molecules and Cells
    • /
    • v.26 no.2
    • /
    • pp.171-174
    • /
    • 2008
  • Flavone (2-phenyl chromone) is a well-known plant flavonoid, but its bioactivity has been little explored. Treatment of Caenorhabditis elegans or C. brissage with flavones induced embryonic and larval lethality that was pronounced in early larval stages. This anti-nematodal effect was also observed in the pinewood nematode, B. xylophilus. $LD_{50}$ values were approximately $100{\mu}M$ for both B. xylophilus and C. elegans. Our results indicate that flavone is an active nematicidal compound that should be further investigated with the aim of developing a potent drug against B. xylophilus.