• Title/Summary/Keyword: In-vivo bioavailability

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Biotransformation of Pregnane Glycosides from Cynanchum wilfordii Roots by β-Glucosidase (당 분해효소를 이용한 백하수오 뿌리로부터 분리한 Pregnane Glycosides의 생전환)

  • Yoon, Mi-Young;Cuong, Mai Nguyen;Choi, Gyung-Ja;Choi, Yong-Ho;Jang, Kyoung-Soo;Cha, Byeong-Jin;Kim, Jin-Cheol
    • Research in Plant Disease
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    • v.18 no.3
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    • pp.186-193
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    • 2012
  • Biotransformation is an eco-friendly and efficient method for enhancing the bioavailability of biopesticide. To increase the antifungal activity of the crude extract of Cynanchum wilfordii roots against barely powdery mildew, we performed biotransformation of wilfoside C1G using ${\beta}$-glucosidase (cellobiase from Aspergillus niger). The mixture (G sample) of partially purified wilfoside C1G and cynauricuoside A (K1G) was treated with ${\beta}$-glucosidase to remove a glucopyranosyl moiety. The enzyme completely converted C1G to C1N and K1G to K1N. Optimal conditions for enzymatic biotransformation of G sample were determined to be 10% ethanol, 1,555 ${\mu}U$ ${\beta}$-glucosidase/ml, pH 5, and $45^{\circ}C$. In in vivo experiment, the G sample transformed by ${\beta}$-glucosidase showed stronger antifungal activity against barley powdery mildew than the non-treated G sample. These results suggest that ${\beta}$-glucosidase biotransformation can be applied to increase the antifungal activity of the crude extract of C. wilfordii roots against powdery mildews.

Ginsenoside compound K protects against cerebral ischemia/ reperfusion injury via Mul1/Mfn2-mediated mitochondrial dynamics and bioenergy

  • Qingxia Huang;Jing Li;Jinjin Chen;Zepeng Zhang;Peng Xu;Hongyu Qi;Zhaoqiang Chen;Jiaqi Liu;Jing Lu;Mengqi Shi;Yibin Zhang;Ying Ma;Daqing Zhao;Xiangyan Li
    • Journal of Ginseng Research
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    • v.47 no.3
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    • pp.408-419
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    • 2023
  • Background: Ginsenoside compound K (CK), the main active metabolite in Panax ginseng, has shown good safety and bioavailability in clinical trials and exerts neuroprotective effects in cerebral ischemic stroke. However, its potential role in the prevention of cerebral ischemia/reperfusion (I/R) injury remains unclear. Our study aimed to investigate the molecular mechanism of ginsenoside CK against cerebral I/R injury. Methods: We used a combination of in vitro and in vivo models, including oxygen and glucose deprivation/reperfusion induced PC12 cell model and middle cerebral artery occlusion/reperfusion induced rat model, to mimic I/R injury. Intracellular oxygen consumption and extracellular acidification rate were analyzed by Seahorse multifunctional energy metabolism system; ATP production was detected by luciferase method. The number and size of mitochondria were analyzed by transmission electron microscopy and MitoTracker probe combined with confocal laser microscopy. The potential mechanisms of ginsenoside CK on mitochondrial dynamics and bioenergy were evaluated by RNA interference, pharmacological antagonism combined with co-immunoprecipitation analysis and phenotypic analysis. Results: Ginsenoside CK pretreatment could attenuate mitochondrial translocation of DRP1, mitophagy, mitochondrial apoptosis, and neuronal bioenergy imbalance against cerebral I/R injury in both in vitro and in vivo models. Our data also confirmed that ginsenoside CK administration could reduce the binding affinity of Mul1 and Mfn2 to inhibit the ubiquitination and degradation of Mfn2, thereby elevating the protein level of Mfn2 in cerebral I/R injury. Conclusion: These data provide evidence that ginsenoside CK may be a promising therapeutic agent against cerebral I/R injury via Mul1/Mfn2 mediated mitochondrial dynamics and bioenergy.

Safety of Nano-sized Bee Pollen in both In-vitro and In-vivo Models (생체 외 및 생체 내 실험조건에서 나노화 벌 화분의 안전성 규명)

  • Pyeon, Hae-In;So, Soojeong;Bak, Jia;Lee, Seunghyun;Lee, Seungmin;Suh, Hwa-Jin;Lim, Je-Oh;Kim, Jung-Woo;Kim, Sun Youn;Lee, Se Ra;Lee, Yong Hyun;Chung, Il Kyung;Choi, Yun-Sik
    • Journal of Life Science
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    • v.28 no.5
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    • pp.605-614
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    • 2018
  • Bee pollen has an outer wall which is resistant to both acidic and basic solutions and even the digestive enzymes in the gastrointestinal tract. Therefore, the oral bioavailability of bee pollen is only 10-15%. A previous study reported on wet-grinding technology which increased the extraction of active ingredients from bee pollen by 11 times. This study was designed to investigate the safety of wet-ground bee pollen. First, a single dose of wet-ground bee pollen was tested in both rats and beagle dogs at dosages of 5, 10, and 20 g/kg and 1.5, 3, and 6 g/kg, respectively. In rats, compound-colored stools were found in those administered 10 g/kg or more of wet-ground bee pollen. In beagle dogs, 6 g/kg of wet-ground bee pollen induced diarrhea in one male for four hours. However, no obvious clinical signs were found through the end of the experiment in rats and beagle dogs. In addition, no histological abnormality was found in all animals. The data indicates that a single dose of up to 20 g/kg of wet-ground bee pollen is safe. Next, the genetic toxicity of nano-sized bee pollen was tested. This study employed a bacterial reverse mutation test, a micronucleus assay, and a chromosomal aberration assay. In the micronucleus assay, there was no genetic toxicity up to the dosage of 2 g/kg. There was also no genetic toxicity in the bacterial reverse mutation test and chromosomal aberration assay. This data provides important information in developing nano-sized bee pollen into more advanced functional foods and herbal medicines.