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Chemopreventive Agents
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Matrine (Figure 12.23) is a tetracyclo-quinolizidine, and the predominant alkaloid in Sophora plants. It has a structure based on four saturated six-membered rings with two ring-junction nitrogen atoms, making it rich in stereochemistry. Matrine is reported to have both in vitro and in vivo antitumor activity, and is the main bioactive compound in Kushen at a concentration of 1 g/10 kg. It is also a constituent of the herb Sophora flavescens used in Chinese medicine. Structure of the alkaloid matrine.
Herbs in Cancer Therapy
Published in Anil K. Sharma, Raj K. Keservani, Surya Prakash Gautam, Herbal Product Development, 2020
Annum Malik, Shahzadi Sidra Saleem, Kifayat Ullah Shah, Learn-Han Lee, Bey Hing Goh, Tahir Mehmood Khan
G. lucidum is medicinal fungus having effects on immune system. It stimulates the immune system by activating the macrophages, t-cells and NK cells (natural killer cells). It also causes an increase in TNF, interleukins and interferon’s by stimulating their production (Smith-Hall et al. 2012). Leukocytes increase and improved immune system was shown by the use of Sophora flavescens (Yang et al. 2006). Heat and toxin clearing plant group includes S. baicalensis. This plant also has anti-tumor and immune system stimulatory effects which includes inhibition of platelet aggregation and induction of apoptosis.
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.
Acute and 13 weeks subchronic toxicological evaluation of the flavonoid-rich extract of Sophora flavescens
Published in Drug and Chemical Toxicology, 2023
Chaoqun Wu, Yun Huang, Huiqi Huang, Yuanren Ma, Qinxiong Lin, Xinzhou Yang, Kejian Pang
The roots of Sophora flavescens were collected from Lingyuan City, Liaoning province, PR China in September 2012, and identified by Dr. Dingrong Wan of School of Pharmaceutical Sciences, South-Central University for Nationalities, Wuhan, PR China. A voucher specimen (no. SF20120520) was deposited in the School of Pharmaceutical Sciences, South-Central University for Nationalities. Air-dried roots of S. flavescens (30 kg) were ground and then extracted sequentially by maceration at room temperature with n-hexane (3 × 50 L, 3 d each), followed by ethyl acetate (3 × 50 L, 3 d each) and methanol (3 × 50 L, 3 d each). The solvents were evaporated at reduced pressure to yield 183.8 g, 863.5 g, and 1426.9 g of n-hexane, ethyl acetate, and methanol fractions, respectively. The ethyl acetate fraction of S. flavescens was chemically characterized based on off-line semi-preparative HPLC and NMR, similar to our previous study (Yang et al.2015).
Liver metabolomic characterization of Sophora flavescens alcohol extract-induced hepatotoxicity in rats through UPLC/LTQ-Orbitrap mass spectrometry
Published in Xenobiotica, 2020
Peng Jiang, Yancai Sun, Nengneng Cheng
Sophora flavescens (Fabaceae) has been used as a traditional Chinese medicine (TCM) and functional food ingredient for thousands of years in Asian countries because of its potential health benefits. It is widely used to treat cancers, antimicrobial activities (Liu et al., 2018), anti-inflammatory activities (Ma et al., 2018), chronic osteomyelitis (Wang et al., 2018), viral hepatitis (Zhang et al., 2018), viral myocarditis and gastrointestinal hemorrhage (Yang et al., 2012). Many herbal products, including Kushen tablets, Xiaoyin tablets, Shiduqing capsules and Zhixue capsules, contain S. flavescens. However, S. flavescens was found to be the toxic ingredient of Zhixue capsules, which were removed from markets on account of severe hepatotoxic events (Tai et al., 2010). Unfortunately, the mechanisms of S. flavescens-induced hepatotoxicity remain unclear. In general, the preparation of S. flavescens used in clinics is an aqueous extract whose major components are matrine and oxymatrine, which are alkaloids that have hepatoprotective effects (Gao et al., 2018; Shi et al., 2013). However, S. flavescens alcohol extract (SFAE) mainly contains prenylflavanones, such as sophoraflavanone G and kurarinone, which are hepatotoxic constituents (Yu et al., 2013). Many herbal preparations contain SFAE, and the risks of its clinical use should be explored.
Inhibition of CYP2C9 by natural products: insight into the potential risk of herb-drug interactions
Published in Drug Metabolism Reviews, 2020
Kai Wang, Qing Gao, Tingting Zhang, Jinqiu Rao, Liqin Ding, Feng Qiu
Except for noscapine, most alkaloids act as reversible inhibitors of CYP2C9 and the inhibitory effect is usually moderate (Table 5). Another common isoquinoline alkaloid, berberine, decreased CYP2C9 activity in healthy male subjects in a clinical study (Guo et al. 2012). An in vitro study confirmed berberine as a moderate inhibitor of CYP2C9 with an IC50 value of 190 μM (Li et al. 2016), which was consistent with the results of another report that showed that berberine slightly increased the plasma concentration of losartan in rats (Chatterjee and Franklin 2003). Epiberberine noncompetitively inhibited CYP2C9, and the IC50 was 8.18 μM (Chen et al. 2017; Chen et al. 2018), which was much lower than that of berberine. However, an alternative study comparing two herbal prescriptions widely used in China showed that the Cmax of epiberberine was only approximately 0.041 μM (13.65 ng/ml) or 0.014 μM (4.82 ng/ml) in rat plasma after oral administration of the Zuojin formula or the Fan-Zuojin formula, respectively (Qian et al. 2017). Another alkaloid, sophocarpine, which is found in the root of Sophora Flavescens Ait., also exhibited a more potent inhibitory effect on CYP2C9 (IC50 = 15.96 μM) in a competitive manner. It was reported that the maximum concentration of sophocarpine measured in rabbit plasma was approximately 0.61 μM after the administration of Kuhuang by injection (Wu et al. 2005).