• Natural Product Sciences
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• 제27권3호
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• pp.176-182
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• 2021

The phytochemical investigation of Broussonetia kazinoki roots led to the isolation of ten compounds, including six flavonoids (1-6), two lignans (7 and 8), and two coumarins (9 and 10) by comparing their ¹H and ¹³C NMR spectra with reference values. To the best of our knowledge, compounds 9 and 10 were isolated from this plant for the first time. Among the ten isolates, compounds 2, 4, and 6 exhibited inhibitory effects against lipopolysaccharide (LPS)-induced nitric oxide (NO) production in macrophage RAW264.7 cells with IC₅₀ values of 11.98, 10.16, and 24.06 μM, respectively. Furthermore, compounds 2, 4, and 6 reduced LPS-induced inducible nitric oxide synthase (iNOS) expression in a dose-dependent manner. Pre-incubation of cells with these compounds also significantly suppressed LPS-induced COX-2 protein expression. Compounds 2, 4, and 6 also showed cytotoxic activity against HL-60 cells with IC₅₀ values ranging between 46.43 and 94.06 μM.

• Natural Product Sciences
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• 제27권3호
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• pp.141-150
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• 2021

This short review on the chemistry, pharmacological properties and patents of obovatol and obovatal from Magnolia obovata is the first publication. Pharmacological properties are focused on anti-cancer, anti-inflammatory, anti-platelet and neuroprotective activities. Obovatol and obovatal were first isolated from the leaves of M. obovata. Also reported in the bark and fruits of M. obovata, obovatol and obovatal are neolignans i.e., biphenolic compounds bearing a C-O coupling. Other classes of compounds isolated and identified from M. obovata include sesquiterpene-neolignans, dineolignans, trineolignan, lignans, dilignans, phenylpropanoids, phenylethanoid glycosides, flavonoids, phenolic acids, alkaloids, sesquiterpenes, ketone and sterols. The anti-cancer properties of obovatol and obovatal involve apoptosis, inhibition of the growth, migration and invasion of cancer cell lines. However, obovatol displays cytotoxicity against cancer cells but not obovatal. Similarly, anti-inflammatory, anti-platelet, neuroprotective, anxiolytic and other pharmacological activities were only observed in obovatol. The disparity in pharmacological properties of obovatol and obovatal may be attributed to the -CHO group present in obovatal but absent in obovatol. From 2007 to 2013, eight patents were published on obovatol with one mentioning obovatal. They were all published at the U.S. Patent and Trademark Office by scientists of the Korea Research Institute of Bioscience and Biotechnology (KRIBB) as inventors and assignee, respectively. Some future research and prospects are suggested.

• Natural Product Sciences
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• 제28권3호
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• pp.153-160
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• 2022

Neuroinflammation is known to be associated with brain injury in Alzheimer's disease (AD), and the inhibition of microglial activation, a key player in inflammatory response, is considerd as important target for AD. In this study, the ethanol extract of aerial parts of Forsythia velutina Nakai, a Korean native species, significantly inhibited nitric oxide (NO) production in LPS-stimulated BV2 microglial cells. Thus, the active principles in F. velutina aerial parts were isolated based on activity-guided isolation method. As a result, six compounds were isolated and their structures were elucidated based on NMR data and the comparison with the relevant references as arctigenin (1), matairesinol (2), rengyolone (3), ursolic acid (4), secoisolariciresinol (5), and arctiin (6). Among them, four compounds including arctigenin (1), matairesinol (2), secoisolariciresinol (5), and arctiin (6) significantly inhibited NO production in a dose-dependent manner. In particular, matairesinol (2) and secoisolariciresinol (5) reduced 60% of NO production compared to LPS-treated group. This inhibitory effects of matairesinol (2) and secoisolariciresinol (5) were accompanied with the reduced expression levels of iNOS and COX-2. These results suggest that the extract of F. velutina and its active compounds could be beneficial for neuroinflammatory diseases including AD.

• 대한약침학회지
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• 제25권3호
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• pp.199-208
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• 2022

Objectives: In recent decades, the trend for treating diabetes mellitus (DM) has shifted toward alternative medicines that are obtained from plant sources. Existing literature suggests that phenolic compounds derived from plants possess promising health-promoting properties. This study aimed to discuss the role of plant-derived phenolic compounds in the effective treatment and management of diabetes. Methods: Information about plant secondary metabolites, phenolic compounds, and their role in the treatment and management of diabetes was collected from different databases, such as Pubmed, ScienceDirect, Scopus, and Google Scholar. Keywords like secondary metabolites, phenolic compounds, simple phenol, flavonoids, lignans, stilbenes, and diabetes were searched. Research and review articles with relevant information were included in the study. Results: Anti-diabetic studies of the four major classes of phenolic compounds were included in this review. The plant-derived phenolic compounds were reported to have potent anti-diabetic activities. However, each class of phenolic compounds was found to behave differently according to various mechanisms. Conclusion: The obtained results suggest that phenolic compounds derived from natural sources display promising anti-diabetic activities. Based on the available information, it can be concluded that phenolic compounds obtained from various natural sources play key roles in the treatment and management of diabetes.

• Mass Spectrometry Letters
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• 제13권4호
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• pp.152-157
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• 2022

Schisandra chinensis and its fruits have been used as a traditional herbal medicine to treat liver dysfunction, fatigue, and chronic coughs. Several in vitro and in vivo studies suggested that dibenzocyclooctadiene lignans present in Schisandra fruits strongly inhibit CYP3A4 activity. However, reports on the inhibitory potential of dietary Schisandra supplements against CYP3A activity are limited despite their increasing consumption as dietary supplements. In this study, we evaluated the CYP3A-inhibitory potential of four dietary Schisandra supplements in human liver microsomes. At a concentration of 0.05 mg/mL, Schisandra supplements from Nature's Way, Swanson, Planetary Herbals, and Only Natural inhibited CYP3A activity by 93.9, 70.8, 33.6, and 24.8%, respectively. Nature's Way, which exhibited the strongest inhibition against CYP3A, had the highest contents of gomisin B and gomisin C, which potently inhibit CYP3A activity. The in vivo pharmacokinetics of this product should be examined to determine whether the clinical relevance of inhibiting CYP3A activity by dietary Schisandra supplementation.

• 한국작물학회지
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• 제37권4호
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• pp.377-382
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• 1992

본 연구는 고항산화 양질 육종의 체계확립을 위해서 참깨에 있는 특수성분인 sesamin, sesamolin의 표준물질을 동정하고 그 분석기술을 개발하였는바 그 결과는 다음과 같다. 1. 한국산 참깨로부터 sesamin, sesamolin 성분을 분리하여 화학적 구조를 분광학적 방법(UV, $^1$H와 $^{13}$C-NMR, MS)으로 확인하여 sesamin, sesamolin의 표준물질을 동정하였다. 2. 참깨 lignan성분의 추출 및 분리에는 Unsaponifiable fration 보다 MeOH 냉온처리가 더 효과적이었다. 3. 검량선의 회귀직선의 방정식은 sesamin에서 y=53924.43＋1277.93x(r=0.9993)이었고 sesamolin의 경우는 y=11034.95＋1188.38x(r=0.9994)로 추정되었다. 4. 한국산 참깨의 lignan 성분함량은 단백깨의 경우 sesamin 0.42% sesamolin 0.3%로 나타났다.

• Biomolecules & Therapeutics
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• 제31권2호
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• pp.148-160
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• 2023

Depression is a neuropsychiatric disorder associated with persistent stress and disruption of neuronal function. Persistent stress causes neuronal atrophy, including loss of synapses and reduced size of the hippocampus and prefrontal cortex. These alterations are associated with neural dysfunction, including mood disturbances, cognitive impairment, and behavioral changes. Synaptic plasticity is the fundamental function of neural networks in response to various stimuli and acts by reorganizing neuronal structure, function, and connections from the molecular to the behavioral level. In this review, we describe the alterations in synaptic plasticity as underlying pathological mechanisms for depression in animal models and humans. We further elaborate on the significance of phytochemicals as bioactive agents that can positively modulate stress-induced, aberrant synaptic activity. Bioactive agents, including flavonoids, terpenes, saponins, and lignans, have been reported to upregulate brain-derived neurotrophic factor expression and release, suppress neuronal loss, and activate the relevant signaling pathways, including TrkB, ERK, Akt, and mTOR pathways, resulting in increased spine maturation and synaptic numbers in the neuronal cells and in the brains of stressed animals. In clinical trials, phytochemical usage is regarded as safe and well-tolerated for suppressing stress-related parameters in patients with depression. Thus, intake of phytochemicals with safe and active effects on synaptic plasticity may be a strategy for preventing neuronal damage and alleviating depression in a stressful life.

• Natural Product Sciences
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• 제13권3호
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• pp.199-206
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• 2007

Antioxidant activity of 70% aqueous ethanolic extract of leaves of Justicia gendarussa (EJ) was evaluated. EJ was prepared by cold maceration method. The antioxidant potency of EJ was investigated employing various established in vitro systems, such as DPPH radical scavenging, nitric oxide (NO) scavenging, ${\beta}-carotene$ linoleic acid module system (${\beta}$ CLAMS), hydroxyl (OH) radical scavenging, anti lipid peroxidation. $IC_{50}$ values were determined in each experiment. Also, ferric ion reduction capacity of extracts in presence and absence of chelating agent (EDTA) and total antioxidant capacity were determined. Preliminary phytochemical investigation was carried out to know the nature of constituents present in the leaves and correlate it with antioxidant activity. Further total phenolic content was determined in EJ. $IC_{50}$ values of EJ were 123.09 ${\pm}$ 3.01, 643.0 ${\pm}$ 61.10, 132.3 ${\pm}$ 6.03, 68.5 ${\pm}$ 11.5 and 68.13 ${\pm}$ 1.38 ${\mu}g/mL$ in DPPH radical scavenging, NO scavenging, ${\beta}$ CLAMS, OH radical scavenging and anti lipid peroxidation activity respectively. In total antioxidant capacity assay, ascorbic acid equivalent value was found to be 205.56 ${\pm}$ 4.69 ${\mu}g/mg$ of extract. Total phenolic content was found to be 43.76 ${\pm}$ 4.27 ${\mu}g$ equivalent of gallic acid per mg of extract. Phytochemical investigation reveals the presence of flavonoids. The results indicate that EJ possess antioxidant activity and flavonoids are responsible for this activity.

• Bulletin of the Korean Chemical Society
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• 제32권11호
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• pp.4049-4054
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• 2011

A new compound, kalopanaxin F (3), and 11 known compounds (1, 2, 4-12), were isolated from the stem bark of Kalopanax pictus. Their structures were elucidated on the basis of chemical and spectroscopic methods. Five of the compounds (2, 3, 5, 6, and 12) significantly inhibited $TNF{\alpha}$-induced NF-${\kappa}B$ transcriptional activity in HepG2 cells in a dose-dependent manner, with $IC_{50}$ values ranging from 6.2 to 9.1 ${\mu}M$. Furthermore, the transcriptional inhibitory function of these compounds was confirmed based on decreases in COX-2 and iNOS gene expression in HepG2 cells. Compounds 3-7, 9, and 12 significantly activated the transcriptional activity of PPARs dose-dependently, with $EC_{50}$ values ranging from 4.1-$12.7{\mu}M$. Compounds 4 and 5 exhibited $PPAR{\alpha}$, $PPAR{\gamma}$, and $PPAR{\beta}({\delta})$ transactivational activities in a dose-dependent manner, with $EC_{50}$ values of 16.0 and 17.0, 8.7 and 16.5, 26.2 and 26.3 ${\mu}M$, respectively.

• KSBB Journal
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• 제23권3호
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• pp.271-275
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• 2008

오미자를 이용한 고기능성 음료개발을 위하여 이번 연구에서는 추출조건별로 오미자의 기능성분 함량 및 anthocyanin 색소에 대한 최적 추출조건을 설정하였다. 분쇄하지 않은 오미자를 이용해서 추출한 경우, Bl값은 차이가 없었으나, schizandrin은 20% 수준에 그쳐 최종적으로 분쇄한 오미자를 시료로 설정하였다. 분쇄한 오미자는 $40^{\circ}C$, 75% ethanol로 추출했을 때 schizandrin 함량이 가장 높았으며, Bl 값은 온도와 ethanol 함량이 높아 질수록 감소하였다. 높은 기능성과 제품의 관능성을 고려할 때 schizandrin 함량과 Bl값을 최적으로 만족하는 조건은 분쇄 오미자를 $46^{\circ}C$에서 24% ethanol을 사용하여 3시간 추출했을 경우 높은 값을 얻을 수 있었다.