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Nanocarriers Systems and Their Application for the Delivery of Different Phytoconstituents
Published in Madhu Gupta, Durgesh Nandini Chauhan, Vikas Sharma, Nagendra Singh Chauhan, Novel Drug Delivery Systems for Phytoconstituents, 2020
Ebru Altuntaş, Gülgün Yener, Burcu Özkan
It has been shown that an active component named Oxymatrine (OMT), extracted from Sophora flavescens, possesses antiproliferation and antioxidative characteristics (Guzman et al., 2013, Jayaprakasam et al., 2013, Jin et al., 2010). OMT is applied for treating viral hepatitis (Liu et al., 2016), ischemia reperfusion injury, and bronchial asthma in China (Yuan et al., 2011). OMT–phospholipid complex (OMT–PLC) was developed with the aim of improving the bioavailability of OMT by Yue et al. (2010). Optimum conditions for the process were 3 hours of reaction time, 60°C of reaction temperature, and 3:1 of the OMT-PLC ratio. An improvement of the mean Cmax value of 0.164 μg/mL was obtained on the oral use of a drug solution at a dose of 0.437 μg/mL, and on the oral use of the phospholipid complex at a dose of 100 mg/kg of OMT administered to rats. Detection of Tmax as 2.17 and 1.71 hours, respectively, in drug solution and complex applications, suggests that the plasma drug concentration has a sustained pattern. The AUC of OMT-PLC (9.43 μg−1 h) elevated considerably to that of free OMT (2.87 μg−1 h) in rats administered via oral route. The overall bioavailability of OMT complex has been shown to be 3.29 times greater compared to OMT.
The Effect of Induced Diabetes Mellitus on the Cerebellar Cortex of Adult Male Rat and the Possible Protective Role of Oxymatrine: A Histological, Immunohistochemical and Biochemical Study
Published in Ultrastructural Pathology, 2021
Amany Mohamed Shalaby, Adel Mohamed Aboregela, Mohamed Ali Alabiad, Mona Tayssir Sadek
Traditional Chinese remedies are commonly employed in both prophylaxis and management of refractory health problems due to their available resources, therapeutic outcomes on various targets, less adverse effects and reduced cost care.13 Oxymatrine is the major quinolizidine alkaloid extracted from the root of a traditional Chinese herb; Sophora flvescens.14 Oxymatrine has extensive pharmacological activities, including anti-viral,15 anti-oxidant,16 anti-tumor17 and anti-inflammatory effects.18 Also, it has been shown to suppress the neuroinflammatory reactions and to delay the development of neurodegenerative diseases.19 Additionally, oxymatrine was reported to exert neuroprotective effects on cerebral ischemia/reperfusion injury in animal models.20 Previous studies showed that administration of oxymatrine significantly reduced the level of blood glucose in mice fed with high fructose diet21 and improved the insulin sensitivity in diabetic rats, thus, it was predicted that oxymatrine may have a beneficial impact on diabetes mellitus.22 Hence, this work was performed to investigate the potential role of oxymatrine against cerebellar cortex injury caused by DM in rats using different histological methods.
Natural products for the management of the hepatitis C virus: a biochemical review
Published in Archives of Physiology and Biochemistry, 2020
Walid Hamdy El-Tantawy, Abeer Temraz
Oxymatrine is major alkaloids in Sophora root. It is reported to have antiviral activity against HCV in cell cultures and in animal and human studies (Liu et al.2003). Clinical trials have looked at the effect of oxymatrine in chronic HCV patients. In the first one, 40 patients were randomised to receive either an intravenous injection of 600 mg/day oxymatrine, after 3 months of treatment, 47% of the treated cases cleared HCV. No serious adverse events were reported. The treated group had a significantly higher ALT normalisation rate relative to the control group in the first 2 months, but this significant difference was not maintained at the end of the third month of treatment. In the second trial, the effect of oxymatrine on liver fibrosis in both HBV and HCV chronically infected patients was assessed. The treated patients took one capsule containing 300 mg oxymatrine orally three times a day, in addition to a complex of vitamins B and C. One hundred and thirty two (132) patients out of 144 showed a significant improvement in liver fibrosis as measured by a series of indicators, including serum hyaluronic acid and type-III procollagen peptide. The authors also reported a significant improvement in ALT. These results are promising and indicate that treatment with oxymatrine capsules warrants further evaluation in HCV cases (Mao et al.2004).
The inhibitory effects of five alkaloids on the substrate transport mediated through human organic anion and cation transporters
Published in Xenobiotica, 2018
Tahiatul Shams, Xiaoxi Lu, Ling Zhu, Fanfan Zhou
The previous studies reported that oxymatrine inhibited the function of human OCT1 with the IC50 value of 513 ± 135 μM; oxymatrine and matrine led to 42% and 88% inhibition of OCT3-mediated substrate uptake at 3 and 6 mM, respectively (Pan et al., 2014). However, in the current study, matrine and oxymatrine have minimal impact on the transport activity of OCTs at 10 μM (Figures 2–4). This is because the concentrations of oxymatrine and matrine used in our study (10 μM) are much lower than those used in the previous studies. As expected, it is hard to achieve plasma concentrations of these compounds as high as 3 and 6 mM. After oral administration of oxymatrine, the Cmax of oxymatrine and matrine in human plasma was only reported to be 1.38 ± 0.55 μM and 8.28 ± 1.68 μM, respectively (Fan et al., 2013). Therefore, our study is more clinically relevant that oxymatrine and matrine are not likely to impact on the substrate transport mediated by OCTs.