• Title/Summary/Keyword: synthesis of natural product

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Novel Benzoylurea Derivatives as Potential Antitumor Agents; Synthesis, Activities and Structure-Activity Relationships

  • Hwang, Ki-Jun;Park, Kyung-Ho;Lee, Chong-Ock;Kim, Beom-Tae
    • Archives of Pharmacal Research
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    • v.25 no.6
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    • pp.781-785
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    • 2002
  • A series of pyrazoloxyphenyl benzoyl urea derivatives was designed and synthesized for cytotoxic evaluation as potential antitumor agents. The synthetic compounds were evaluated for in vitro cytotoxicity against five human tumor cell lines, including A-549, SKOV-3, SK-MEL-2, XF-498 and HCT-15. Among others, compound 11 exhibited 50∼100 times greater antitumor activities than the commercial product, Cisplatin.

Enhancing the Effect of Aronia Extract on Hyaluronic Acid Synthesis through Liposome Formation

  • Youn, Young Han
    • Journal of People, Plants, and Environment
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    • v.23 no.4
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    • pp.465-473
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    • 2020
  • Background and objective: Aronia melanocarpa, called black chokeberry, is a natural product belonging to the family rosaceae, and is known to contain polyphenolic antioxidants including cyanidin-3-galactoside, cyanidin-3-arabinoside, cyanidin-3-xyloside, and cyanidin-3-glucoside Because of the abundance of anthocyanins, Aronia has been studied to be used in various industries. Methods: Aronia melanocarpa extract was treated 24 hours a day to RAW 264.7 cells with inflammations induced by LPS. After extracting total RNA, the amount of inflammatory cytokine expression was measured using RT-PCR. After processing the Aronia liposome using Aronia extract and the layer-by-layer electrostatic deposition method in keratinocyte cells at the same time, we checked the synthesis of Hyaluronic acid enhanced through the formation of Aronia liposome using ELISA. Results: The treatment of Aronia extract in inflammation-induced RAW 264.7 cells conducted to check the anti-inflammatory efficacy of Aronia extract inhibited inflammatory cytokines including TLR4, TNF-α, IL-1β, COX-2, and iNOS and increased the mRNA expression of HAS2 genes related to moisturizing. Based on the anti-inflammatory and moisturizing effect of Aronia extract, the Aronia liposome technology was introduced to Aronia extract to produce Aronia liposome. Conclusion: The liposome formation of Aronia extract is expected to be used as a functional material in treating various inflammatory skin diseases by controlling the moisture content of the corneocytes by increasing the expression rate of genes associated with the synthesis of hyaluronic acid, while retaining the efficacy of its components.

Inhibitory Effects of Plant Extracts on Tyrosinase Activity and Melanin Synthesis

  • Park, Hyen-Joo;Park, Kwang-Kyun;Hwang, Jae-Kwan;Chung, Won-Yoon;Lee, Seung-Eun;Lee, Sang-Kook
    • Natural Product Sciences
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    • v.16 no.2
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    • pp.133-139
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    • 2010
  • In order to develop a new skin whitening agent, approximately 100 plant extracts were evaluated for their inhibitory activities against melanin biosynthesis in cultured mouse melanocyte melan-a cells. As a result, seven extracts exhibited over 50% inhibition of melanin synthesis compared to control at a concentration of $20\;{\mu}g/ml$. In particular, Aster ageratoides Turcz. var. ageratoides (branch, root, aerial, flower; $IC_{50}$ = 17.3, 6.1, 13.6, $12.9\;{\mu}g/ml$, respectively) and Physalis alkekengi var. francheti (leaf, unripen fructus, aerial; $IC_{50}$ = 6.5, 28.3, $23.9\;{\mu}g/ml$) markedly inhibited melanin synthesis. In addition, tyrosinase activity was monitored by the measurement of dopachrome formation from the oxidation of L-3,4-dihydroxyphenylalanine. Extracts of A. ageratoides Turcz. var. ageratoides (flower) and P. alkekengi var. francheti (leaf) showed the most potent tyrosinase inhibitory activity. These plants might be the potential candidate sources in the development of novel skin-whitening products.

Effect of Ethanolic Extracts Mixed with Grains and Fallopia multiflora on Melanogenesis (곡물과 적하수오를 혼합한 에탄올 추출물이 멜라닌 합성에 미치는 영향)

  • Lee, Eunbeen;Kim, Moon-Moo
    • Journal of Life Science
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    • v.29 no.4
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    • pp.461-469
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    • 2019
  • The aim of this study was to investigate the effect of a mixture of ethanol extracts of Black oryzasativa, Sesamum indicum, Oryza sativa, Rhynchosia Nulubilis, and Polygoni multiflori radix (MIXEE) on melanogenesis to develop a natural product for black hair growth. An accumulation of hydrogen peroxide ($H_2O_2$) in hair follicles, which reduces melanin synthesis, is responsible for hair graying. In the present study, MIXEE showed scavenging activity against DPPH radicals and reducing power. In addition, it reduced the cellular $H_2O_2$ level, indicating that it could inhibit oxidation and promote melanin synthesis, which was decreased by $H_2O_2$. On the other hand, it did not affect tyrosinase activity in vitro but promoted the turnover of L-DOPA into melanin. MIXEE promoted melanin synthesis at the cellular level in B16F1 cells. Furthermore, MIXEE increased the expression levels of superoxide dismutase 2 (SOD2) and SOD3 in western blot analysis. In addition, MIXEE increased the expression levels of tyrosinase-related protein (TRP)-2, which promoted melanin synthesis from L-DOPA. The results suggested that MIXEE could promote melanogenesis. Therefore, MIXEE may have potential as a natural product for promotion of melanin production and reversal of gray hair to black hair.

Plant cell culture strategies for the production of natural products

  • Ochoa-Villarreal, Marisol;Howat, Susan;Hong, SunMi;Jang, Mi Ok;Jin, Young-Woo;Lee, Eun-Kyong;Loake, Gary J.
    • BMB Reports
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    • v.49 no.3
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    • pp.149-158
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    • 2016
  • Plants have evolved a vast chemical cornucopia to support their sessile lifestyles. Man has exploited this natural resource since Neolithic times and currently plant-derived chemicals are exploited for a myriad of applications. However, plant sources of most high-value natural products (NPs) are not domesticated and therefore their production cannot be undertaken on an agricultural scale. Further, these plant species are often slow growing, their populations limiting, the concentration of the target molecule highly variable and routinely present at extremely low concentrations. Plant cell and organ culture constitutes a sustainable, controllable and environmentally friendly tool for the industrial production of plant NPs. Further, advances in cell line selection, biotransformation, product secretion, cell permeabilisation, extraction and scale-up, among others, are driving increases in plant NP yields. However, there remain significant obstacles to the commercial synthesis of high-value chemicals from these sources. The relatively recent isolation, culturing and characterisation of cambial meristematic cells (CMCs), provides an emerging platform to circumvent many of these potential difficulties.

A Refining of Natural Diatomite and Synthesis of SiC Powder (규조토 정제 및 탄화규소 분말합성)

  • Pai, Chul-Hoon
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.18 no.3
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    • pp.312-319
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    • 2017
  • For high value-added applications of natural blue diatomite, the physical refining process and synthesis of SiC from refined diatomite were investigated. Approximately 30 percent Fe ($Fe_2O_3$) in raw blue diatomite was removed by a particle sieve separation process; the Fe composition for 325 mesh down powder was approximately 2 percent. Although a wet and/or dry magnetic separation process had some influence on the separation and/or refining of Fe composition, the Fe composition in the non-magnetic by-product was approximately 2 percent. Water leaching separation was effective in removing the Fe composition; approximately 40 percent of the Fe in raw blue diatomite was removed. The synthesis of ${\beta}$-SiC by a carbothermal reduction of the $SiO_2$ in the refined diatomite using carbon (graphite, carbon black), the effects of an acid-treatment on removing the Fe, and the specific surface area for the synthesized powder were also investigated. The impurities were mostly eliminated and the specific surface area was increased to $52.5m^2/g$.

The Effect of Oligosaccharides on Ethylene Production in Mung Bean (Vigna radiata W.) Hypocotyl Segments

  • Choy, Yoon-Hi;Lee, Dong-Hee;Lee, June-Seung
    • Journal of Plant Biology
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    • v.39 no.4
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    • pp.295-300
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    • 1996
  • The physiological effects of oligogalacturonic acid (OGA:D. P. 6-7), a product of acid hydrolysis of polygalacturonic acid (PGA), on ethylene biosynthesis in mung bean (Vigna radiata W.) hypocotyl segments was studied. Among PGA, OGA and monogalacturomic acid (MGA), only OGA stimulated ethylene production in mung bean hypocotyl segments, and the most effective concentraton of OGA was 50$\mu\textrm{g}$/mL. Time course data indicated that this stimulatiion effect of OGA appeared after 90 min incubation period and continued until 24 h. When indol-3-acetic acid (IAA) and 1-aminocyclopropane-1-carboxylic acid (ACC) were treated with OGA to investigate the mechanism of OGA on ethylene production, they did not show synergistic effects on ethylene production. The stimulation of ethylene production by OGA was due to the increase of in vivo ACC synthase activity, but OGA treatment had no effect of in vivo ACC oxidase activity. The effect of aminoethoxy vinyl glycine (AVG) and Co2+, the inhibitor of ethylene synthesis, was siminished a little by the OGA, but the treatment of Ca2+, known to increase ACC, with OGA did not increase the ethylene production, this effect seems to be specific for Ca2+ because other divalent cation, Mg2+, did not show the inhibition of OGA-indyuced ethylene production. It is possible that the OGA adopts a different signal transduction pathway to the ethylene bioxynthesis.

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Biogenic Nano-Synthesis; towards the Efficient Production of the Biocompatible Gold Nanoparticles

  • Ghodake, Gajanan;Eom, Chi-Yong;Kim, Si-Wouk;Jin, Eon-Seon
    • Bulletin of the Korean Chemical Society
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    • v.31 no.10
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    • pp.2771-2775
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    • 2010
  • We present a rapid biogenic method for the production of nanoscale gold particles using pear extract. The formation and stability of pear-derived gold nanoparticles (Pear-AuNPs) were monitored by ultraviolet-visible spectroscopy. Their morphology, elemental composition and crystalline phase were determined by transmission electron microscopy, energy-dispersive X-ray spectroscopy and selected area electron diffraction. The average core size of crystalline Pear-AuNPs was in the range of $10{\pm}5\;nm$ and the observed morphology was spherical. The X-ray photoelectron spectrum showed a strong peak for the pure 'Au' phase. The circular dichroism spectrum indicated the natural capping ability of the pear extract, which generated peptide-gold nanoparticles. These nanoparticles were stable in aqueous solution for two months. A cell viability assay of Pear-AuNPs showed biocompatibility with human embryonic kidney 293 cells. Accordingly, this eco-friendly process for the bio-mimetic production of Pear-AuNPs is nontoxic in nature; consequently, it will find potential application in nano-biotechnology.

Discrimination of biological and artificial nicotine in e-liquid

  • Hyoung-Joon Park;Heesung Moon;Min Kyoung Lee;Min Soo Kim;Seok Heo;Chang-Yong Yoon;Sunyoung Baek
    • Analytical Science and Technology
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    • v.36 no.1
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    • pp.22-31
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    • 2023
  • As the use of e-liquid cigarettes is rapidly increasing worldwide, it multiplies the potential risk undisclosed to the health of non- and smokers. To reduce the hazard, each country has its own set of regulations for controlling e-liquids. In Korea, the narrow definition of tobacco makes it difficult and have been steadily occurring tax evasion exploiting the difference in natural and artificial nicotine. Therefore, it is very important to distinguish source of nicotine for their regulation. To find biochemical discriminant markers, this study established analysis methods based on high-performance liquid chromatography coupled with diode array detector (HPLC-DAD) and high-performance liquid chromatography coupled with triple Quadrupole mass spectrometry (HPLC-MS/MS) for nicotine enantiomers and tobacco alkaloids targeted using the difference in pathways of nicotine biosynthesis and chemical synthesis. The method was validated by experimenting linearity (R2 > 0.999), recovery (80.99-108.41 %), accuracy (94.11-109.73 %) and precision (0.04-8.27 %). Then, the results for discrimination of the nicotine obtained from analysis of 65 commercial e-liquid products available in Korean market was evaluated. The method successfully applied to the e-liquids and one sample labelled 'synthetic nicotine' for tax exemption was found to contain a natural nicotine product. This method can be used to determine whether an e-liquid product uses natural or artificial nicotine and monitor non-taxable e-liquid products. The method is more scientific than the existing one, which relies only on field evidence.

The Study of Plate Powder Coated Nano Sized ZnO Synthesis and Effect of Sensory Texture Improvement (나노 ZnO 입자가 코팅된 판상 분체의 합성과 사용감 증진 효과에 대한 연구)

  • Jin-Hwa , Lee;Ju-Yeol, Han;Sang-Gil, Lee;Hyeong-Bae, Pyo;Dong-Kyu, Lee
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.30 no.2
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    • pp.173-180
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    • 2004
  • Nano sized ZnO particle as 20-30nm applies for material, pigments, rubber additives, gas sensors, varistors, fluorescent substance as well as new material such as photo-catalyst, sensitizer, fluorescent material. ZnO with a particle size in the range 20-30nm has provided to be an excellent UV blocking material in the cosmetics industry, which can be used in sunscreen product to enhance the sun protection factor and natural makeup effect. But pure ZnO particles application limits for getting worse wearing feeling. We make high-functional inorganic-composite that coated with nano-ZnO on the plate-type particle such as sericite, boron nitride and bismuthoxychloride. In this experiment, we synthesized composite powder using hydrothermal precipitation method. The starting material was ZnCl$_2$ Precipitation materials were used hexamethylenetetramine(HMT) and urea. We make an experiment with changing as synthesis factors that are concentrations of starting material, precipitation materials, nuclear formation material, reaction time, and reaction temperature. We analyzed composite powder's shape, crystallization and UV-blocking ability with FE-SEM, XRD, FT-IR, TGA-DTA, In vitro SPF test. The user test was conducted by product's formulator. In the results of this study, nanometer sized ZnD was coated regardless of the type of plate-powder at fixed condition range. When the coated plate-powders were applied in pressed powder product, the glaze of powder itself decreased, but natural make-up effect, spreadability, and adhesionability were increased.