TOXICON
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2024
·
IF 2.6
Xuelin Chen,Kun Zhang,Hanlei Wang,Xia Zhao,Yumei Zhang
Kochiae Fructus (KF) is a traditional Chinese medicine, which has been used to delay aging and treat inflammation, such as rubella, eczema, cutaneous pruritus, etc . In order to fully understand the traditional medicinal value of KF, we evaluated the antioxidant properties and oral safety of its ethanolic extract. Considering flavonoids and phenolics in medicinal plants generally have strong antioxidant activity, we firstly detected the total flavonoids and phenolics contents of KFEE and its fractions. Secondly, we evaluated the antioxidant activities of KFEE and its fractions. Finally, we evaluated the oral safety of KFEE by the acute and 28-day subacute toxicities. The n-butanol fraction (ENBF) possessed the highest phenolics and flavonoids with values of 77.30 ± 3.17 mg gallic acid equivalents/g and 228.81 ± 7.56 mg rutin equivalents/g, respectively. The results of antioxidant tests showed that ENBF possessed potent antioxidant ability. Among them, the high antioxidation capacity observed in ENBF could be attributed to its rich content of flavonoids and phenolics. The results of toxicological studies showed that the LD 50 value of KFEE was 6000 mg/kg BW, and the no observed adverse effect level (NOAEL) of KFEE was 600 mg/kg BW. According to the standards of the American Academy of Sciences for the classification of toxic substances, KFEE can be classified as practically non-toxic substance, which provided valuable evidence for the oral safety of KF as a natural aging delay medicine.
研究领域:
中药学
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药理学
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毒理学
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天然产物
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产品关联
DOI
PubMed
高影响因子
BMC Complementary and Alternative Medicine
·
2017
·Vol. 17
·期 1
·1-10
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IF 2.288
Chen Long,Liu Tianjun,Wang Qiangsong,Liu Juan
Background Resveratrol and curcumin, as natural flavones products, have good therapeutic effect in acute and chronic inflammation; on the other hand, tetramethylpyrazine (TMP) has angiogenesis and vessel protection effect as well as anti-inflammatory function. In this paper, the anti-inflammatory effect of the tetramethylpyrazine, resveratrol and curcumin (TRC) combination in acute and chronic inflammation was reported in vivo.Methods The dose of the combined three natural products was optimized based on the acute paw swelling mouse model with a Uniform Design methodology. The therapeutic effect of TRC combination on chronic inflammation was investigated by using the collagen-induced arthritis (CIA) rat model based upon the following indexes: the volume of paw swelling, arthritis score, serum mediators and histological examination as well as immunohistochemical staining. The levels of alanine aminotransferase (ALT) and aspartate transaminase (AST) in serum were measured and the pathological sections of liver and kidney were analysed. LD50 was measured based on the acute oral toxicity (AOT) standard method.Results The best formulation was the three components combined at the same mass proportion revealed by the Uniform Design methodology. This combination could significantly reduce the paw swelling in acute paw swelling mouse model, could reduce paw swelling and alleviate the damage in joint structural of ankle, cartilages and fibrous tissue in CIA rat model. The dose relationship was clear in both cases. Immunohistochemical staining of ankle tissue revealed that TRC combination was able to inhibit the expression of NF-κB p65 and TNF-α which were closely related to the inflammatory process. Analysis of serum mediators revealed TRC combination could inhibit the production of TNF-α, IL-1β, and IL-6 in the serum. Toxic study revealed this formulation was low toxic, LD50 was larger than 5 g/kg, both the level of ALT and AST and histopathology in the liver and kidney exhibited no distinctions between the TRC combination and the blank group, no mortality occurred at the administered doses of 5 g/kg.Conclusion sThe results showed this formulation could provide a novel potent treatment for acute and chronic inflammation (RA) without side effect like gastric injury occurring in NSAIDs.
研究领域:
药理学
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免疫学
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毒理学
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风湿病学
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产品关联
DOI
PubMed
高影响因子
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
·
2023
·
IF 6.7
Yang Wang,Ruiqi Su,Jianwen Chen,Xuan Liu,Jingning Luo,Yaoqiang Lao,Ping Huang,Jinguo Shi,Caibao Jiang,Liping Liao,Jingxia Zhang
Acute ischemic stroke (AIS) is a serious cardiovascular and cerebrovascular disease; Oxidative stress and neuroinflammation are important factors which destroy blood-brain barrier (BBB) in AIS. In the study, a series of 1,3,5-triphenyl-1,2,4-triazole derivatives were designed and synthesized; the optimal compound 9 was obtained by screening their anti-oxidant and anti-inflammatory effects; the neuroprotection effect of compound 9 was evaluated with a rat middle cerebral artery occlusion (MCAO) model. Subsequently, the mechanism of neuroprotection were explored via Western blot. The results prompt compound 9 maybe exert anti-AIS neuroprotection by inhibiting oxidative stress and neuroinflammation inhibition by inhibiting Keap1, COX-2 and iNOS. At the same time, it can protect BBB by reducing glycocalyx degradation and matrix metallopeptidase-9 levels. Its LD 50 > 1000 mg/kg on mice and hERG channel inhibition IC 50 > 30 μM, which lower acute toxicity and hERG channel inhibition would make compound 9 a promising stroke treatment candidate.
研究领域:
药理学
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神经科学
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心血管疾病
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药物发现
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DOI
PubMed
高影响因子
Journal of Functional Foods
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2021
·
IF 4.451
Zhenfeng Huang,You Luo,Xuesen Xia,Anping Wu,Zhenqiang Wu
Fermentation results in the release and biotransformation of phenolic compounds in guava leaves. This study aimed to evaluate the bioaccessibility, safety and antidiabetic effect of phenolic-rich extract from fermented guava leaves (PE-fgl) using Monascus anka and Bacillus sp. BS2. The total phenolics and flavonoids were 51.18% and 16.60% bioaccessible after gastrointestinal digestion, respectively. High bioaccessibility was observed, particularly for ellagic acid, isoquercitrin, quercetin-3-O-β-D-xylopyranoside, quercetin-3-O-α-L-arabinofuranoside and avicularin, resulted in high recovery of α-glucosidase inhibition activity and antioxidant capacity. Moreover, PE-fgl was practically nontoxic with a median lethal dose (LD 50 ) greater than 5000 mg/kg and was without evidence of toxicity following subchronic administration up to the dose limit of 2000 mg/kg. Furthermore, PE-fgl significantly improved serum glucose and lipid levels as well as antioxidant capacity in diabetic mice. Liver, kidney and pancreas damage was also significantly alleviated. These results suggested that PE-fgl could be a nontoxic candidate for diabetes treatment.
研究领域:
药理学
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营养学
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糖尿病研究
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食品科学
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毒理学
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）