• Title/Summary/Keyword: Pharmaceutical compound

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2-O-digalloyl-1,3,4,6-tetra-O-galloyl-β-D-glucose isolated from Galla Rhois suppresses osteoclast differentiation and function by inhibiting NF-κB signaling

  • Ihn, Hye Jung;Kim, Tae Hoon;Kim, Kiryeong;Kim, Gi-Young;Jeon, You-Jin;Choi, Yung Hyun;Bae, Jong-Sup;Kim, Jung-Eun;Park, Eui Kyun
    • BMB Reports
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    • v.52 no.6
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    • pp.409-414
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    • 2019
  • Natural compounds isolated from medicinal herbs and plants have immense significance in maintaining bone health. Hydrolysable tannins have been shown to possess a variety of medicinal properties including antiviral, anticancer, and anti-osteoclastogenic activities. As a part of a study on the discovery of alternative agent against skeletal diseases, we isolated a hydrolysable tannin, 2-O-digalloyl-1,3,4,6-tetra-O-galloyl-${\beta}$-D-glucose (DTOGG), from Galla Rhois and examined the effect on osteoclast formation and function. We found that DTOGG significantly inhibited receptor activator of nuclear factor-${\kappa}B$ ligand (RANKL)-induced osteoclast differentiation by downregulating the expression of the key regulator in osteoclastogenesis as well as osteoclast-related genes. Analysis of RANKL/RANK signaling revealed that DTOGG impaired activation of $I{\kappa}B{\alpha}$ and p65 in the nuclear factor kappa-lightchain-enhancer of activated B cells (NF-${\kappa}B$) signaling pathway. Furthermore, DTOGG reduced bone resorbing activity of osteoclasts, compared to the vehicle-treated control. These results suggest that DTOGG could be a useful natural compound to manage osteoclast-mediated skeletal diseases.

4,4'-Diaponeurosporene from Lactobacillus plantarum subsp. plantarum KCCP11226: Low Temperature Stress-Induced Production Enhancement and In Vitro Antioxidant Activity

  • Kim, Mibang;Jung, Dong-Hyun;Seo, Dong-Ho;Park, Young-Seo;Seo, Myung-Ji
    • Journal of Microbiology and Biotechnology
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    • v.31 no.1
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    • pp.63-69
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    • 2021
  • Carotenoids, which have biologically beneficial effects and occur naturally in microorganisms and plants, are pigments widely applied in the food, cosmetics and pharmaceutical industries. The compound 4,4'-diaponeurosporene is a C30 carotenoid produced by some Lactobacillus species, and Lactobacillus plantarum is the main species producing it. In this study, the antioxidant activity of 4,4'-diaponeurosporene extracted from L. plantarum subsp. plantarum KCCP11226 was examined. Maximum carotenoid content (0.74 ± 0.2 at A470) was obtained at a relatively low temperature (20℃). The DPPH radical scavenging ability of 4,4'-diaponeurosporene (1 mM) was approximately 1.7-fold higher than that of butylated hydroxytoluene (BHT), a well-known antioxidant food additive. In addition, the ABTS radical scavenging ability was shown to be 2.3- to 7.5-fold higher than that of BHT at the range of concentration from 0.25 mM to 1 mM. The FRAP analysis confirmed that 4,4'-diaponeurosporene (0.25 mM) was able to reduce Fe3+ by 8.0-fold higher than that of BHT. Meanwhile, 4,4'-diaponeurosporene has been confirmed to be highly resistant to various external stresses (acid/bile, high temperature, and lysozyme conditions). In conclusion, L. plantarum subsp. plantarum KCCP11226, which produces 4,4'-diaponeurosporene as a functional antioxidant, may be a potentially useful strain for the development of functional probiotic industries.

Photostability evaluation of Jawarishe Jalinoos

  • Shahnawaz, Shahnawaz;Rahman, Khaleequr;Sultana, Arshiya;Sultana, Shabiya
    • CELLMED
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    • v.11 no.4
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    • pp.18.1-18.8
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    • 2021
  • Jawarishe Jalinoos (JJ) is an orally used formulation available in semisolid dosage form, prepared with powdered plant materials mixed in honey or sugar syrup. It has many admirable pharmacological effects and used in Unani medicine to treat various acute and chronic disorders since ancient times. The ICH Harmonised Tripartite Guideline stated that photostability testing should be an essential part of stability testing to confirm that light exposure does not result in an unacceptable change in drugs substance and finished products. To date, the effect of light on JJ is not studied, in this study photostability evaluation of JJ was carried out. The test sample was manufactured with genuine ingredients in the in-door pharmacy of the National Institute of Unani Medicine. JJ was packed in two transparent polyethylene terephthalate airtight containers. The first sample was analysed at zero-day and the second sample was placed in a stability chamber subjected to light challenge with an overall illumination of 1.2 million lux hours combined with near ultraviolet energy of 200-watt hours per square meter by using option 2, along with 30±2℃ temperature and relative humidity 70±5%. Analysis of both finished products showed no considerable changes in organoleptic characters. Less than 5% variation was observed in physicochemical parameters. HPTLC fingerprinting showed justifiable variation. Microbial load and specific counts were within the limit prescribed by WHO. As no unacceptable changes were noted in JJ subjecting to light challenge, it is concluded that JJ is a photostable Unani compound formulation.

Effects of Activated Carbon on the Reduction of Benzo(a)pyrene in Artemisia argyi Extract

  • Lee, Sung-Hoon
    • Journal of People, Plants, and Environment
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    • v.23 no.5
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    • pp.537-544
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    • 2020
  • Background and objective: Artemisia argyi has a long history as an effective treatment for various diseases. The detection of environmental pollutant benzo(a)pyrene, a known human carcinogen, in the leaves of Artemisia argyi is cause for concern. For medicinal plant extracts, both a reduction of benzo(a)pyrene as well as the maintained effectiveness of the compound are important. Therefore, in this study, we propose an optimized process for the addition and filtration of activated carbon to reduce benzo(a)pyrene and change the contents of the indicating substance(jaceosidine and eupatilin). Methods: Artemisia argyi EtOH extract containing 36 ppb of benzo(a)pyrene was added to 0.1, 0.5, 1.0, and 1.5% (w/w) of activated carbon for 120 min and filtered using an activated carbon filter 1, 2, 3, and 5 times respectively. The content of benzo(a)pyrene and indicating substances in Artemisia argyi extract were then measured with high performance liquid chromatography (fluorescence and UV detectors). Results: As the amounts of activated carbon powder and filtering cycles increased, the content of benzo(a)pyrene in the Artemisia argyi extract decreased. However, when activated carbon powder 1.5% was added to the extract, and when the activated carbon filter was filtered five times, the results were reduced by 15% and 30~40% respectively. The optimal extraction condition for reducing benzo(a)pyrene was adding 1.5% of activated carbon powder. This resulted in reducing benzo(a)pyrene by 83% and indicating substances by about 4%. Conclusions: Here we present a process for reducing benzo(a)pyrene in Artemisia argyi extract using activated carbon to reduce toxicity and minimize the loss of active ingredients. This approach has potential application within a manufacturing process of various medicinal plant extracts.

Identification of 1,3,6,8-Tetrahydroxynaphthalene Synthase (ThnA) from Nocardia sp. CS682

  • Purna Bahadur Poudel;Rubin Thapa Magar;Adzemye Fovennso Bridget;Jae Kyung Sohng
    • Journal of Microbiology and Biotechnology
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    • v.33 no.7
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    • pp.949-954
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    • 2023
  • Type III polyketide synthase (PKS) found in bacteria is known as 1,3,6,8-tetrahydroxynaphthalene synthase (THNS). Microbial type III PKSs synthesize various compounds that possess crucial biological functions and significant pharmaceutical activities. Based on our sequence analysis, we have identified a putative type III polyketide synthase from Nocardia sp. CS682 was named as ThnA. The role of ThnA, in Nocardia sp. CS682 during the biosynthesis of 1,3,6,8 tetrahydroxynaphthalene(THN), which is the key intermediate of 1-(α-L-(2-O-methyl)-6-deoxymannopyranosyloxy)-3,6,8-trimethoxynaphthalene (IBR-3) was characterized. ThnA utilized five molecules of malonyl-CoA as a starter substrate to generate the polyketide 1,3,6,8-tetrahydroxynaphthalene, which could spontaneously be oxidized to the red flaviolin compound 2,5,7-trihydroxy-1,4-naphthoquinone. The amino acid sequence alignment of ThnA revealed similarities with a previously identified type III PKS and identified Cys138, Phe188, His270, and Asn303 as four highly conserved active site amino acid residues, as found in other known polyketide synthases. In this study, we report the heterologous expression of the type III polyketide synthase thnA in S. lividans TK24 and the identification of THN production in a mutant strain. We also compared the transcription level of thnA in S. lividans TK24 and S. lividans pIBR25-thnA and found that thnA was only transcribed in the mutant.

Newly identified maltol derivatives in Korean Red Ginseng and their biological influence as antioxidant and anti-inflammatory agents

  • Jeong Hun Cho;Myoung Chong Song;Yonghee Lee;Seung-Taek Noh;Dae-Ok Kim;Chan-Su Rha
    • Journal of Ginseng Research
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    • v.47 no.4
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    • pp.593-603
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    • 2023
  • Background: Korean Red Ginseng is a major source of bioactive substances such as ginsenosides. Efficacy of red ginseng extract (RGE), which contains not only saponins but also various non-saponins, has long been studied. In the water-soluble component-rich fraction of RGE (WS), a byproduct generated in the process of extracting saponins from the RGE, we identified previously unidentified molecules and confirmed their efficacy. Methods: The RGE was prepared and used to produce WS, whose components were isolated sequentially according to their water affinity. The new compounds from WS were fractionized and structurally analyzed using nuclear magnetic resonance spectroscopy. Physiological applicability was evaluated by verifying the antioxidant and anti-inflammatory efficacies of these compounds in vitro. Results: High-performance liquid chromatography confirmed that the obtained WS comprised 11 phenolic acid and flavonoid substances. Among four major compounds from fractions 1-4 (F1-4) of WS, two compounds from F3 and F4 were newly identified in red ginseng. The analysis results show that these compound molecules are member of the maltol-structure-based glucopyranose series, and F1 and F4 are particularly effective for decreasing oxidative stress levels and inhibiting nitric oxide secretion, interleukin (IL)-1β and IL-6, and tumor necrosis factor-α. Conclusion: Our findings suggest that a few newly identified maltol derivatives, such as red ginseng-derived non-saponin in the WS, exhibit antioxidant and anti-inflammatory effects, making them viable candidates for application to pharmaceutical, cosmetic, and functional food materials.

Evaluation of Cell Based Anti-oxidation Assay of Functional Components Derived from Domestic Major Potato Varieties

  • Jung Hwan Nam;Su Young Hong;Su Jeong Kim;Hwang Bae Sohn;Yul Ho Kim;Kyung Tea Lee;Soo jin Park;Jae Kwon Lee
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2020.08a
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    • pp.75-75
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    • 2020
  • Potatoes were first introduced outside the Andes region four centuries ago, and have become an integral part of much of the world's food. Potatoes were first introduced into Europe in the 16th century and Korea in the early 19th century. Potatoes have a short growing season, high production per unit area, relatively strong environmental adaptability, and are cultivated in more than 130 countries around the world. It is the world's fourth-largest crop, following rice, wheat, bean and maize. In the nutritional aspects, potatoes contain abundant vitamins and minerals, as well as an assortment of phytochemicals such as carotenoids and natural phenols. Due to the high content of potato functional compounds, it has known that potatoes are effective in the prevention of various human diseases. In particular, the potato contains a large amount of polar compounds, including the saponin in the polar compounds, and the physiological activity of the saponins, such as immunity enhancement, antioxidant and anti-inflammatory is known. In this study, the antioxidative activity of polar compounds from five potatoes was examined by cell based anti-oxidation assay. The smallest amount of ROS(Reactive oxygen species) was generated when the compound was derived from 'Haryung' and 'hongyoung' and strong SOD(Superoxide dismutase) activity was observed in 'Sumi' and 'Jayoung'. The results of this study reveal the antioxidative effect of polar compounds extracted from various kind of potatoes, which will enable the acquisition of new bioactive candidates and the establishment of new profit generation models for farmers

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Anti-Inflammatory Activities of (+)-Afzelechin against Lipopolysaccharide-Induced Inflammation

  • In-Chul Lee;Jong-Sup Bae
    • Biomolecules & Therapeutics
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    • v.32 no.4
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    • pp.467-473
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    • 2024
  • In this study, we investigated the potential protective effects of (+)-afzelechin (AZC), a natural compound that is derived from Bergenia ligulata, on lipopolysaccharide (LPS)-induced inflammatory responses. AZC is known to have antioxidant, anticancer, antimicrobial, and cardiovascular protective properties. However, knowledge regarding the therapeutic potential of AZC against LPS-induced inflammatory responses is limited. Thus, we investigated the protective attributes of AZC against inflammatory damage caused by LPS exposure. We examined the effects of AZC on heme oxygenase (HO)-1, cyclooxygenase (COX)-2, and inducible nitric oxide synthase (iNOS) in LPS-activated human umbilical vein endothelial cells (HUVECs). In addition, the effects of AZC on the expression of iNOS, tumor necrosis factor (TNF)-α, and interleukin (IL)-1β were analyzed in the lung tissues of LPS-injected mice. Data revealed that AZC promoted the production of HO-1, inhibited the interaction between luciferase and nuclear factor (NF)-κB, and reduced the levels of COX-2/PGE2 and iNOS/NO, thereby leading to a decrease in the signal transducer and activator of transcription (STAT)-1 phosphorylation. Moreover, AZC facilitated the nuclear translocation of Nrf2, increased the binding activity between Nrf2 and the antioxidant response elements (AREs), and lowered the expression of IL-1β in the LPS-treated HUVECs. In the animal model, AZC significantly reduced the expression of iNOS in the lung tissue structure and the TNF-α level in the bronchoalveolar lavage fluid. These findings demonstrate that AZC possesses anti-inflammatory properties that regulate iNOS through the inhibition of both NF-κB expression and p-STAT-1. Consequently, AZC has potential as a future candidate for the development of new clinical substances for the treatment of pathological inflammation.

Bioactivity-Guided Fraction from Viscera of Abalone, Haliotis discus hannai Suppresses Cellular Basophils Activation and Anaphylaxis in Mice

  • Kap Seong Choi;Tai-Sun Shin;Ginnae Ahn;Shin Hye Kim;Jiyeon Chun;Mina Lee;Dae Heon Kim;Han-Gil Choi;Kyung-Dong Lee;Sun-Yup Shim
    • Journal of Microbiology and Biotechnology
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    • v.34 no.2
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    • pp.379-386
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    • 2024
  • Basophils and mast cells are specialized effector cells in allergic reactions. Haliotis discus hannai (abalone), is valuable seafood. Abalone male viscera, which has a brownish color and has not been previously reported to show anti-allergic activities, was extracted with acetone. Six different acetone/hexane fractions (0, 10, 20, 30, 40, and 100%) were obtained using a silica column via β-hexosaminidase release inhibitory activity-guided selection in phorbol myristate acetate and a calcium ionophore, A23187 (PMACI)-induced human basophils, KU812F cells. The 40% acetone/hexane fraction (A40) exhibited the strongest inhibition of PMACI-induced-β-hexosaminidase release. This fraction dose-dependently inhibited reactive oxygen species (ROS) production and calcium mobilization without cytotoxicity. Western blot analysis revealed that A40 down-regulated PMACI-induced MAPK (ERK 1/2, p-38, and JNK) phosphorylation, and the NF-κB translocation from the cytosol to membrane. Moreover, A40 inhibited PMACI-induced interleukin (IL)-1β, IL-6, and IL-8 production. Anti-allergic activities of A40 were confirmed based on inhibitory effects on IL-4 and tumor necrosis factor alpha (TNF-α) production in compound (com) 48/80-induced rat basophilic leukemia (RBL)-2H3 cells. A40 inhibited β-hexosaminidase release and cytokine production such as IL-4 and TNF-α produced by com 48/80-stimulated RBL-2H3 cells. Furthermore, it's fraction attenuated the IgE/DNP-induced passive cutaneous anaphylaxis (PCA) reaction in the ears of BALB/c mice. Our results suggest that abalone contains the active fraction, A40 is a potent therapeutic and functional material to treat allergic diseases.

Arctigenin from Burdock Root Exhibits Potent Antibacterial and Anti-Virulence Properties against Pseudomonas aeruginosa

  • Abdulrahman E. Koshak;Mahmoud A. Elfaky;Hossam M. Abdallah;Dina A. I. Albadawi;Gamal A. Mohamed;Sabrin R. M. Ibrahim;Abdulrahim A. Alzain;El-Sayed Khafagy;Azza A. H. Rajab;Wael A. H. Hegazy
    • Journal of Microbiology and Biotechnology
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    • v.34 no.8
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    • pp.1642-1652
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    • 2024
  • Arctium lappa (Burdock) root is used in various culinary applications especially in Asian Cuisine. Arctigenin (ARC) is a polyphenolic compound abundant in the roots of the burdock plant from which it derives its name. The emergence of bacterial resistance is a growing global worry, specifically due to the declining availability of new antibiotics. Screening for the antibacterial candidates among the safe natural products is a promising approach. The present study was aimed to assess the antibacterial activity of ARC against Pseudomonas aeruginosa exploring its effect on the bacterial cell membrane. Furthermore, the anti-virulence activities and anti-quorum sensing (QS) activities of ARC were in vitro, in vivo and in silico assessed against P. aeruginosa. The current results showed the ARC antibacterial activity was owed to its disruption effect of the cell membrane. ARC at sub-MIC significantly decreased the formation of biofilm, motility, production of extracellular enzymes and in vivo protected mice against P. aeruginosa. These anti-virulence activities of ARC are owed to its interference with bacterial QS and its expression. Furthermore, ARC showed mild effect on mammalian erythrocytes, low probability to induce resistance and synergistically combined with antibiotics. In summary, the promising anti-virulence properties of ARC indicate its potential as an effective supplement to conventional antibiotics for treating severe P. aeruginosa infections.