• Title/Summary/Keyword: Antifungal compounds

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Synthesis, Spectroscopic, and Biological Studies of Chromium(III), Manganese(II), Iron(III), Cobalt(II), Nickel(II), Copper(II), Ruthenium(III), and Zirconyl(II) Complexes of N1,N2-Bis(3-((3-hydroxynaphthalen-2-yl)methylene-amino)propyl)phthalamide (N1,N2-bis(3-((3-hydroxynaphthalen-2-yl)methylene-amino)propyl)phthalamide의 크롬(III), 망간(II), 철(III), 코발트(II), 니켈(II), 구리(II), 루테늄(III) 및 산화 지르코늄(II) 착물에 대한 합성과 분광학 및 생물학적 연구)

  • Al-Hakimi, Ahmed N.;Shakdofa, Mohamad M.E.;El-Seidy, Ahemd M.A.;El-Tabl, Abdou S.
    • Journal of the Korean Chemical Society
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    • v.55 no.3
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    • pp.418-429
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    • 2011
  • Novel chromium(III), manganese(II), iron(III), cobalt(II), nickel(II), copper(II), ruthenium(III), and zirconyl(II) complexes of $N^1,N^2$-bis(3-((3-hydroxynaphthalen-2-yl)methylene-amino)propyl)phthalamide ($H_4L$, 1) have been synthesized and characterized by elemental, physical, and spectral analyses. The spectral data showed that the ligand behaves as either neutral tridentate ligand as in complexes 2-5 with the general formula $[H_4LMX_2(H_2O)]{\cdot}nH_2O$ (M=Cu(II), Ni(II), Co(II), X = Cl or $NO_3$), neutral hexadentate ligand as in complexes 10-12 with the general formula $[H_4LM_2Cl_6]{\cdot}nH_2O$ (M=Fe(III), Cr(III) or Ru(III)), or dibasic hexadentate ligand as in complexes 6-9 with the general formula $[H_2LM_2Cl_2(H_2O)_4]{\cdot}nH_2O$ (M = Cu(II), Ni(II), Co(II) or Mn(II), and 13 with general formula $[H_4L(ZrO)_2Cl_2]{\cdot}8H_2O$. Molar conductance in DMF solution indicated the non-ionic nature of the complexes. The ESR spectra of solid copper(II) complexes 2, 5, and 6 showed $g_{\parallel}$ >g> $g_e$, indicating distorted octahedral structure and the presence of the unpaired electron in the $N^1,N^2$ orbital with significant covalent bond character. For the dimeric copper(II) complex $[H_2LCu_2Cl_2(H_2O)_4]{\cdot}3H_2O$ (6), the distance between the two copper centers was calculated using field zero splitting parameter for the parallel component that was estimated from the ESR spectrum. The antibacterial and antifungal activities of the compounds showed that, some of metal complexes exhibited a greater inhibitory effect than standard drug as tetracycline (bacteria) and Amphotricene B (fungi).

Induction of Apoptosis and Antitumor Activity by Stichoposide D through the Generation of Ceramide in Human Leukemia Cells (Stichoposide D의 백혈병 세포주에서 세라마이드 생성을 통한 세포 사멸 유도 및 항암 작용)

  • Park, Eun-Seon;Yun, Seung-Hoon;Shin, Sung-Won;Kwak, Jong-Young;Park, Joo-In
    • Journal of Life Science
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    • v.22 no.6
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    • pp.760-771
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    • 2012
  • Marine triterpene glycosides are physiologically active natural compounds isolated from sea cucumbers(holothurians). It was demonstrated that they have a wide range of biological activities, including antifungal, cytotoxic, and antitumor effects. A previous study showed that stichoposide C (STC) isolated from Thelenota anax induces apoptosis through generation of ceramide by activation of acid sphingomyelinase (SMase) and neutral SMase in human leukemia cells. In this study, we investigated whether STD, a structural analog of STC, can induce apoptosis and examined the molecular mechanisms for its activity. It was found that STC and STD induce apoptosis in a dose- and time-dependent manner and lead to the activation of caspase-8, mitochondrial damage, activation of caspase-9, and activation of caspase-3 in K562 and HL-60 cells. STC activates acid SMase and neutral SMase, which results in the generation of ceramide. Specific inhibition of acid SMase or neutral SMase partially blocked STC-induced apoptosis, but not STD-induced apoptosis. In contrast, STD generates ceramide through the activation of ceramide synthase. Specific inhibition of ceramide synthase partially blocked STD-induced apoptosis, but not STC-induced apoptosis. Moreover, STC and STD markedly reduced tumor growth of HL-60 xenograft tumors and increased ceramide generation in vivo. These results indicate that STC and STD can induce apoptosis and have antitumor activity through the different molecular mechanisms, because they have a different sugar residue attached to aglycones. Thus, these results suggest that their actions are affected by a sugar residue attached to aglycones and they can be used as anticancer agents in the treatment of leukemia.

Evaluations on Deodorization Effect and Anti-oral Microbial Activity of Essential Oil from Pinus koraiensis (잣나무 정유의 소취효과 및 구강균에 대한 항균활성 평가)

  • Hwang, Hyun Jung;Yu, Jung-Sik;Lee, Ha Yeon;Kwon, Dong-Joo;Han, Woong;Heo, Seong-Il;Kim, Sun Young
    • Korean Journal of Plant Resources
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    • v.27 no.1
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    • pp.1-10
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    • 2014
  • Essential oils of various plants have been known for potential biological effects such as antibacterial, antifungal, spasmolytic, antiplasmodial activities and insect-repellent property. Recently, the essential oils have attracted considerable interest in oral disease therapy. This essential oil has been known as being effective on easing sick house syndrome, giving forest aroma therapy effect and acting as repellent against pest. The essential oil of Pinus koraiensi, a native plant from Hongcheon-gun, Gangwon-do, was obtained by hydrodistillation. In light of its medicinal importance, in this study its composition, antibacterial activity and the reducing effect of offensive odor have been analyzed. The composition of essential oil was determined by GC and GC-MS. We have identified 14 compounds, of which 1R-${\alpha}$-pinene (19.38 %), 3-carene (10.21 %), camphene (9.82 %), limonene (9.00 %), bicyclo[2,2,1] heptan-2-ol (8.76 %) and ${\beta}$-phellandrene (7.98 %) were the main components. Essential oils from P. koraiensis, Chamaecyparis obtusa, Abies holophylla and Pinus densiflora were compared in terms of alleviating effect of malodors caused from formaldehyde, ammonia, trimethylamine and methylmercaptan. P. koraiensis essential oil was found to decrease the amounts of ammonia and trimethylamine by 75.17 % and 77.36 %, respectively. Antibacterial activity against Streptococcus mutans and Streptococcus sobrinus, which were known as oral cavity inducer, was investigated using the paper disc agar diffusion method. The inhibition zone was observed against S. mutans (5.97 mm) and S. sobrinus (1.40 mm), respectively. P. koraiensis essential oil shown effective deodorization and inhibitory activity against oral cavity in this study might be potential material in oral sanitary industry.