• Title/Summary/Keyword: leading compound

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Functional roles and mechanisms of ginsenosides from Panax ginseng in atherosclerosis

  • Xue, Qianqian;He, Ningning;Wang, Zhibin;Fu, Xiuxiu;Aung, Lynn Htet Htet;Liu, Yan;Li, Min;Cho, Jae Youl;Yang, Yanyan;Yu, Tao
    • Journal of Ginseng Research
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    • v.45 no.1
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    • pp.22-31
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    • 2021
  • Atherosclerosis (AS) is a leading cause of cardiovascular diseases (CVDs) and it results in a high rate of death worldwide, with an increased prevalence with age despite advances in lifestyle management and drug therapy. Atherosclerosis is a chronic progressive inflammatory process, and it mainly presents with lipid accumulation, foam cell proliferation, inflammatory response, atherosclerotic plaque formation and rupture, thrombosis, and vascular calcification. Therefore, there is a great need for reliable therapeutic drugs or remedies to cure or alleviate atherosclerosis and reduce the societal burden. Ginsenosides are natural steroid glycosides and triterpene saponins obtained mainly from the plant ginseng. Several recent studies have reported that ginsenosides have a variety of pharmacological activities against several diseases including inflammation, cancer and cardiovascular diseases. This review focuses on describing the different pharmacological functions and underlying mechanisms of various active ginsenosides (Rb1,-Rd, -F, -Rg1, -Rg2, and -Rg3, and compound K) for atherosclerosis, which could provide useful insights for developing novel and effective anti-cardiovascular drugs.

Isolation and Synthesis of an Antifungal Metabolite Derived from the Commensal Vaginal Bacterium Dermabacter vaginalis (질 내 공생세균 Dermabacter vaginalis 유래 항진균 대사체의 분리 및 합성)

  • So, Jae Seong;Kwon, Kang Mu;Lee, Munseon;Kim, Dae Keun;Hwang, In Hyun
    • Korean Journal of Pharmacognosy
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    • v.53 no.3
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    • pp.119-124
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    • 2022
  • Vaginal microbiome deeply influences vaginal health via production of messenger molecules. The healthy vaginal pH ranges between 3.5 and 4.5. However, dysbiosis of vaginal microbiome increases the pH level, leading to the incidence of vaginitis. The commensal vaginal bacterium Dermabacter vaginalis-which was isolated from the vaginal fluid of a Korean female-was incubated in acidic and neutral pH to simulate healthy and vaginitis conditions, respectively. The chemical profiles of the two different cultures were compared using HPLC. The compound showing distinctive difference between the two sets of data was presumed to be a chemical messenger, which was identified as cyclo(L-pro-L-met) by analysis of NMR, MS, and specific rotation data. Synthesis was achieved in three steps (overall yield 15%), enabling structure confirmation and antimicrobial evaluation against vaginal pathogens. Cyclo(L-pro-L-met) showed antifungal activity against Candida albicans, a major cause of vulvovaginal candidiasis.

Effect of Oxybenzone (Benzophenone-3) on Rock Bream Oplegnathus fasciatus, Embryo Development (옥시벤존(Benzophenone-3)이 돌돔(Oplegnathus fasciatus)의 배 발생 과정에 미치는 영향)

  • Song, Mihae;Baek, Hea Ja
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.55 no.4
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    • pp.455-460
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    • 2022
  • Oxybenzone (Benzophenone-3; BP-3) is a compound used in sunscreens and enters the oceans due to improper disposal. It is known to disrupt the endocrine signaling in marine organisms, leading to immune and reproductive abnormalities in corals, shellfish and fishes. In this study, we investigated the effects of different concentrations of BP-3 (0, 10, 100 and 1,000 ㎍/L) on the fertilized eggs and hatched larvae of Oplegnathus fasciatus. The morphological changes and hatching and survival rates during embryo development were assessed. In addition, the levels of triiodothyronine (T3) were also measured. The hatched larvae exposed to BP-3 at concentrations of 10 and 100 ㎍/L for 24 h displayed malformation of the tail. After 36 h of exposure to BP-3, spinal deformity was observed at all tested concentrations. The hatching rate was significantly low when exposed to 100 ㎍/L of BP-3. A high levels of T3 was observed when the larvae were exposed to BP-3 at a concentration of 1,000 ㎍/L for 96 h (the end of the experiment). This may be related to increased size of larvae at 1,000 ㎍/L BP-3. In conclusion, our results suggested that BP-3 may interfere with embryo development, resulting in a reduction in hatching rate and malformation of larvae.

First Report of Pectobacterium brasiliense Causing Bitter Melon Soft Rot Disease in Korea

  • Kyoung-Taek Park;Leonid N. Ten;Soo-Min Hong;Chang-Gi Back;Seung-Yeol Lee;Hee-Young Jung
    • Research in Plant Disease
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    • v.29 no.4
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    • pp.452-458
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    • 2023
  • In the Goesan region, located in Chungcheongbuk-do, Korea, a significant outbreak of soft rot infections was documented in August 2021, affecting fruits of Momordica charantia, commonly known as bitter melon or bitter gourd. The symptoms included a noticeable transition to yellowing in the affected fruits, eventually leading to their collapse. The bacterial strain KNUB-09-21 was isolated from the diseased fruits. Molecular analysis, using the sequences of the 16S rRNA region and three housekeeping genes (dnaX, recA, and leuS), along with the results of compound utilization in the API ID 32 GN system, provide strong evidence for the identification of the isolate KNUB-09-21 as Pectobacterium brasiliense. The pathogenicity of strain KNUB-09-21 on M. charantia was confirmed through a controlled inoculation test. Within two days, inoculated fruits displayed soft rot symptoms closely resembling those observed in naturally affected fruits. This is the first report of soft rot on M. charantia in Korea.

Exploring the Potential of Rosemary Derived Compounds (Rosmarinic and Carnosic Acids) as Cancer Therapeutics: Current Knowledge and Future Perspectives

  • Fazila Sirajudeen;Lara J. Bou Malhab;Yasser Bustanji;Moyad Shahwan;Karem H. Alzoubi;Mohammad H. Semreen;Jalal Taneera;Waseem El-Huneidi;Eman Abu-Gharbieh
    • Biomolecules & Therapeutics
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    • v.32 no.1
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    • pp.38-55
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    • 2024
  • Cancer is a global health challenge with high morbidity and mortality rates. However, conventional cancer treatment methods often have severe side effects and limited success rates. In the last decade, extensive research has been conducted to develop safe, and efficient alternative treatments that do not have the limitations of existing anticancer medicines. Plant-derived compounds have shown promise in cancer treatment for their anti-carcinogenic and anti-proliferative properties. Rosmarinic acid (RA) and carnosic acid (CA) are potent polyphenolic compounds found in rosemary (Rosmarinus officinalis) extract. They have been extensively studied for their biological properties, which include anti-diabetic, anti-inflammatory, antioxidant, and anticancer activities. In addition, RA and CA have demonstrated effective anti-proliferative properties against various cancers, making them promising targets for extensive research to develop candidate or leading compounds for cancer treatment. This review discusses and summarizes the anti-tumor effect of RA and CA against various cancers and highlights the involved biochemical and mechanistic pathways.

GC-MS Analysis of Endophytic Bacteria Isolate Acalypha indica L. Compounds as Antibacterial

  • Dwyana Zaraswati;Annisa Andi;Johannes Eva;Wardhani Riuh
    • Mass Spectrometry Letters
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    • v.15 no.3
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    • pp.158-165
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    • 2024
  • Pneumonia is an acute respiratory infection that primarily affects the lungs and is caused by various microorganisms, including viruses, fungi, and bacteria. Klebsiella pneumoniae, a multidrug-resistant (MDR) and extensively drug-resistant (XDR) bacterium, is a leading cause of widespread pneumonia. This study aimed to identify endophytic bacteria from the leaves of Acalypha indica L. and evaluate their antibacterial properties through both in vitro and in silico approaches. The objectives included isolating endophytic bacteria from Acalypha indica L., testing their antibacterial activity against Klebsiella pneumoniae, identifying the selected bacterial isolates using molecular techniques, analyzing their secondary metabolites via gas chromatography-mass spectrometry (GC-MS), and performing in silico molecular docking studies. The study identified BE 4, an endophytic bacterial isolate of Bacillus pumilus, as exhibiting the most potent antibacterial activity against Klebsiella pneumoniae. GC-MS analysis of the ethyl acetate extract of this isolate revealed 1,2-benzenedicarboxylic acid, bis(2-methylpropyl) ester as the primary metabolite component. Furthermore, molecular docking analysis identified two natural compound ligands, 1,2-benzenedicarboxylic acid, diethyl ester (-6.5 kcal/mol), and lilial (-6.2 kcal/mol), as having potential efficacy against drugresistant bacteria responsible for pneumonia. These findings suggest that endophytic bacteria and their bioactive compounds could serve as promising candidates for the development of new treatments against drug-resistant pneumonia.

Solution Phase Photolyses of Substituted Diphenyl Ether Herbicides under Simulated Environmental Conditions (모조(模造) 환경조건하(環境條件下)에서의 치환(置換) Diphenyl Ether 제초제(除草劑)의 광분해(光分解)에 관(關)한 연구(硏究))

  • Lee, Jae-Koo
    • Applied Biological Chemistry
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    • v.17 no.3
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    • pp.149-176
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    • 1974
  • Eight substituted diphenyl ether herbicides and some of their photoproducts were studied in terms of solution phase photolysis under simulated environmental conditions by using a Rayonet photochemical reactor. The test compounds absorbed sufficient light energy at the wavelength of 300 nm to undergo various photoreactions. All the photoproducts were confirmed by means of tlc, glc, ir, ms, and/or nmr spectrometry. The results obtained are summarized as follows: Solution phase photolysis of C-6989: An exceedingly large amount of p-nitrophenol formed strongly indicates the readiness of the ether linkage cleavage of this compound as the main reaction in all solvents used. Photoreduction of nitro to amino group(s) and photooxidation of trifluoromethyl to carboxyl group were recognized as minor reactions. Aqueous photolysis of p-nitrophenol: Quinone(0.28%), hydroquinone (0.66%), and p-aminophenol (0.42%) were confirmed as photoproducts, in addition to a relatively small amount of an unknown compound. The mechanisms of formation of these products were proposed to be the nitro-nitrite rearrangement via $n{\rightarrow}{\pi}^*$ excitation and the photoreduction through hydrogen abstractions by radicals, respectively. Solution phase photolysis of Nitrofen: Photochemical reduction leading to the p-amino derivative was the main reaction in n-hexane. In aqueous solution, the photoreduction of nitro to amino group and hydroxylation predominated over the ether linkage cleavage. Nucleophilic displacement of the nitro group by hydroxide ion and replacement of chlorine substituents by hydroxyl group or, to a lesser extent, hydrogen were also observed as minor reactoins. Solution phase photolysis of MO-338: Photoreduction of the nitro to amino group was marked in the n-hexane solution photolysis. In the aqueous solution, photoreduction of the nitro substituent and hydroxylation were the main reactions with replacement of chlorine substituents by the hydroxyl group and hydrogen, and cleavage of the ether linkage as minor reactions. Photolyses of MC-4379, MC-3761, MC-5127, MC-6063, and MC-7181 in n-hexane and cyclohexane: Photoreduction of the nitro group leading to the corresponding amino derivative and replacement of one of the halogen substituents by hydrogen from the solvent used were the key reactions in each compound. Aqueous photolysis of MC-4379: Cleavage of the ether linkage, replacement of the carboxymethyl by hydroxyl group, hydroxylation, and replacement of the nitro by hydroxy group were prominent with photoreduction and dechlorination as minor reactions. Aqueous photolysis of MC-3761: Cleavage of the ether linkage, replacement of the carboxymethyl by hydroxyl group, and photoreduction followed by hydroxylation were the main reactions. Aqueous photolysis of MC-5127: Replacement of carboxyethyl by hydrogen was predominant with ether linkage cleavage, photoreduction, and dechlorination as minor reactions. It was obvious that the decarboxyethylation proceeded more readily than decarboxymethylation occurring in the other compounds. Aqueous photolysis of MC-6063: Cleavage of the ether linkage and photodechlorination were the main reactions. Aqueous photolysis of MC-7181: Replacement of the carboxymethyl group by hydrogen and monodechlorination were the remarkable reactions. Cleavage of the ether linkage and hydroxylation were thought to be the minor reactions. Aqueous photolysis of 3-carboxymethyl-4-nitrophenol: The photo-induced Fries rearrangement common to aromatic esters did not appear to occur in the carboxymethyl group of this type of compound. Conversion of nitro to nitroso group was the main reaction.

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Removal of Cyanogenic Compounds in Apricot Kernel during Heating Process (가열조리방법을 통한 행인 내 시안화합물의 저감화)

  • Do, Byung-Kyung;Kwon, Hoon-Jeong;Lee, Dong-Ha;Nah, Ahn-Hee;Choi, Youn-Ju;Lee, Sook-Yeon
    • Journal of Food Hygiene and Safety
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    • v.22 no.4
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    • pp.395-400
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    • 2007
  • Apricot Kernel, consumed as herbal medicine, contains amygdalin which generate HCN upon hydrolysis. Dyspnea was reported by ingesting large amount of apricot kernel, and neurological disorders such as tropic ataxic neuropathy or konzo were known as chronic toxicity of amygdalin. Other cyanogen containing plants, including flaxseed and almond, are consumed as food around the world. Moreover, some of them are promoted as functional food, leading to higher consumption, and posing health risk by cyanogenic components. The objective of this study was to find a method for the reduction of the cyanogenic compound, using apricot kernel as a model food. The most effective reduction was obtained by boiling the slices of the kernel for one hour in pH 1 HCl solution, showing 90% removal. However, the common process known to reduce the cyanogen contents, i.e., long incubation at the low temperature, did not show significant change in cyan concentration. Our data contribute to the safety of the plants containing cyanogenic compounds if they were to be developed as foodstuff.

The Characteristic Analysis of Calcareous Deposit Films Formed on Steel Plate by Cathodic Current Process in Marine Environment (해양환경 중 음극전류 프로세스에 의해 강판에 형성된 석회질 피막의 특성 분석)

  • Park, Jun-Mu;Kang, Jae Wook;Choi, In-Hye;Lee, Seung-Hyo;Moon, Kyung-Man;Lee, Myeong-Hoon
    • Journal of Surface Science and Engineering
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    • v.49 no.2
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    • pp.166-171
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    • 2016
  • Cathodic protection is widely recognized as the most cost effective and technically appropriate corrosion prevention methodology for the port, offshore structures, ships. When applying the cathodic protection method to metal facilities in seawater, on the surface of the metal facilities a compound of calcium carbonate($CaCO_3$) or magnesium hydroxide($Mg(OH)_2$) films are formed by $Ca^{2+}$ and $Mg^{2+}$ ions among the many ionic components dissolving in the seawater. And calcareous deposit films such as $CaCO_3$ and $Mg(OH)_2$ etc. are formed by the surface of the steel product. These calcareous deposit film functions as a barrier against the corrosive environment, leading to a decrease in current demand. On the other hand, the general calcareous deposit film is a compound like ceramics. Therefore, there may be some problems such as weaker adhesive power and the longer time of film formation uniting with the base metal. In this study, we tried to determine and control the optimal condition through applying the principle of cathodic current process to form calcareous deposit film of uniform and compact on steel plate. The quantity of precipitates was analyzed, and both the morphology, component and crystal structure were analyzed as well through SEM, EDS and XRD. And based on the previous analysis, it was elucidated mechanism of calcareous deposit film formed in the sacrificial anode type (Al, Zn) and current density (1, 3, $5A/m^2$) conditions. In addition, the taping test was performed to evaluate the adhesion.

Synthesis and antifungal activities of 4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-arylthiazol-5-yl]piperidine derivatives on Phytophthora capsici (4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-arylthiazol-5-yl] piperidine 유도체들의 합성과 고추역병균에 대한 살균활성)

  • Nam, Seok-Woo;Lee, Gyung-Rak;Kim, Tae-Joon;Chung, Bong-Jin;Choi, Won-Sik
    • The Korean Journal of Pesticide Science
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    • v.16 no.1
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    • pp.1-10
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    • 2012
  • Fungicidal activities against phytopathogenic fungi of diarylthiazole compound of 4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-(4-fluorophenyl)thiazol-5-yl]-1-methylpiperidine (I) have been determined to be excellent and compound I was used as the leading compounds in this study. Furthermore, the compound was synthesized by reacting them with five functional groups, 4-fluoro-3-methylphenyl, 4-fluoro-3-chlorophenyl, 4-chloro-2-fluorophenyl, 4-bromo-3-methylphenyl and 2,4-dichlorophenyl groups instead of 4-fluorophenyl group. Also, 2-amino-, 2-(N-ethoxycarbonyl)piperidin-4-yl-, and 2-piperidin-4-yl-thiazole were introduced as the leads instead of 2-N-methylpiperidine-4-yl-thiazol of compound I. VIII-1~VIII-5 and XIII-1~XV-5 compounds were newly synthesized and their structures were confirmed by $^1H$-NMR-spectrum. The fungicidal activities of all the synthesized compounds against Phytophthora capsici were examined using the whole plant method. Among the VIII-1~VIII-5 and XIII-1~XV-5 chemicals, XIV-3 showed the most potent antifungal activity in vivo. While the $EC_{50}$ and $EC_{90}$ values of the commercial fungicide dimethomorph and I were $4.26{\pm}0.02$, $14.72{\pm}0.05$ and $1.01{\pm}0.11$, $6.31{\pm}0.09mM$, those of 4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-(4-chloro-2-fluorophenyl)thiazol-5-yl]-1-methylpiperidine (XIV-3) was $0.98{\pm}0.21$ and $5.85{\pm}0.05mM$. Therefore, XIV-3 can be considered as a viable candidate for the control of plant diseases caused by P. capsici, and further studies will be conducted on the mode of action XIV-3.