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Delivery of Herbal Cardiovascular Drugs in the Scenario of Nanotechnology: An Insight
Published in Mahfoozur Rahman, Sarwar Beg, Mazin A. Zamzami, Hani Choudhry, Aftab Ahmad, Khalid S. Alharbi, Biomarkers as Targeted Herbal Drug Discovery, 2022
Kumar Anand, Subhabrata Ray, Md. Adil Shaharyar, Mahfoozur Rahman, Rudranil Bhowmik, Sanmoy Karmakar, Monalisha Sen Gupta
Breviscapine is one of the most significant drugs used for the treatment of cardiovascular and cerebrovascular disorders. It is a crude extract of many flavonoids of Erigeron breviscapus (Vant.). Hand.-Mazz., containing at least 85% of scutellarin, which is a famous traditional herbal drug used in China as a cerebrovascular medicine to improve cerebral blood supply. According to various in vivo and in vitro proofs of concept studies, it has been observed that breviscapine exerts a wide range of cardiovascular pharmacological effects, such as vasodilation, anticoagulat, antithrombotic, endothelial protector. Apart from that, it helps to reduce smooth muscle cell migration and proliferation and helps in anticardiac remodeling, antiarrhythmia, and blood lipid reduction. Further many clinical studies have reported that breviscapine could be used in conjunction with Western medicine for CVDs including coronary heart disease, myocardial infarction, atrial fibrillation, HTN, viral myocarditis, hyperlipidemia, pulmonary heart disease, and chronic heart failure.
Inhibiting Low-Density Lipoproteins Intimal Deposition and Preserving Nitric Oxide Function in the Vascular System
Published in Christophe Wiart, Medicinal Plants in Asia for Metabolic Syndrome, 2017
Caffeic acid, and 3,5-di-O-caffeoylquinic acid methyl ester isolated from the flowers of Erigeron annuus (L.) Pers. inhibited the formation of advanced glycation end products with IC50 values below 15 µM (aminoguanidine: IC50: 961 µM).266 Caffeic acid, and 3,5-di-O-caffeoylquinic acid methyl ester inhibited rat lens aldose reductase with IC50 values of 25.8, and 0.8 µM (epalrestat: IC50: 0.07 µM).266 Apigenin, luteolin, apigenin-7-O-β-d-glucuronide, apigenin-7-O-β-d-glucuronide methyl ester, kaempferol, quercetin, astragalin, and quercitrin from the flowers of this plant inhibited rat lens aldose reductase with IC50 values of ranging from 1 to 10 µM.267 Scutellarin which is common in the genus Erigeron L., inhibited the adherence of monocytes to ECV304 cells induced by high-glucose from 69% to 38%. It also reduced the expression of monocyte chemoattractant peptide-1 as well as nuclear translocation of nuclear factor-κB.268 In alloxan-induced diabetic Kunming mice this flavonoid at a dose of 50 mg/kg/day for 3 weeks had no effect on plasma glucose but lowered monocyte chemoattractant peptide-1.268
Emerging Highlights on Natural Prodrug Molecules with Multifarious Therapeutic Perspectives
Published in Debarshi Kar Mahapatra, Cristóbal Noé Aguilar, A. K. Haghi, Applied Pharmaceutical Practice and Nutraceuticals, 2021
Mojabir Hussen Ansari, Vaibhav Shende, Debarshi Kar Mahapatra
Baicalin is a prodrug flavonoid of baicalein, which has been acquired from the traditional Chinese medicinal plant Scutellaria Baicalensis Georgi. It shows many crucial activities such as antitumor, anti-inflammatory, antibacterial, immunostimulant, anti-allergic, and antiviral effects. Baicalein is more effective compared to baicalin because it is absorbed more slowly and to a lesser quantity than baicalein. However, it is very difficult to remove baicalein without delay because of its low content (0.2–0.5%) in the extract. A higher and reliable method of obtaining baicalein is by the enzyme hydrolysis from baicalin, which is present in better content material in the extract (6–10%).21,22 Cadmium-induced hepatic cytotoxicity, oxidative stress, and histomorphometric changes are additionally prevented by means of baicalin.23 Baicalin has also been investigated to have 5α-reductase inhibiting activity that is useful as a hair growth stimulant and is presently commercially available in several brands of shampoo.24 Based on the molecular studies, it is proved that the anti-inflammatory activity occurred due to its bioactive chemical flavones. Along with anti-inflammatory activities, the flavones isolated from Scutellarin have also shown cytostatic and cytotoxic properties against many human cancer cell lines.25 Baicalin also inhibited the growth of Chlamydia trachomatis, a prevalent sexually transmitted bacterial pathogen in humans that causes pelvic inflammatory disease, ectopic pregnancy, and infertility in women. Baicalin also protects the human fibroblasts toward ultraviolet B-triggered cyclobutane pyrimidine dimers formation.26,27
Scutellaria baicalensis extract and baicalein inhibit replication of SARS-CoV-2 and its 3C-like protease in vitro
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Hongbo Liu, Fei Ye, Qi Sun, Hao Liang, Chunmei Li, Siyang Li, Roujian Lu, Baoying Huang, Wenjie Tan, Luhua Lai
Based on the docking analysis, we searched for baicalein analogues from available flavonoid suppliers and selected eight flavonoids and two glycosides for experimental testing (Table 2). The docking scores are given in Table S1. Four flavonoid compounds were found to be potent SARS-CoV-2 3CLpro inhibitors. Among them, scutellarein is mainly distributed in genus Scutellaria and Erigerontis herba (Dengzhanxixin or Dengzhanhua in Chinese) in its glucuronide form, scutellarin. Scutellarin has long been used in cardiovascular disease treatment for its ability to improve cerebral blood supply37. As shown in Figure 4, scutellarein inhibits SARS-CoV-2 3CLpro with an IC50 value of 5.8 µM, while scutellarin showed mild inhibitory activity at 50 µM concentration. The other three flavonoid compounds, dihydromyricetin, quercetagetin, and myricetin derived from Ampelopsis japonica (Bailian in Chinese), Eriocaulon buergerianum (Gujingcao in Chinese), and Polygoni avicularis (Bianxu in Chinese), respectively, inhibit SARS-CoV-2 3CLpro with IC50 values of 1.20, 1.24, and 2.86 µM. Interestingly, scutellarein and myricetin were reported to inhibit the SARS-CoV, indicating their potential as multi-target anti-SARS-CoV-2 agents38.
Triglyceride-mimetic prodrugs of scutellarin enhance oral bioavailability by promoting intestinal lymphatic transport and avoiding first-pass metabolism
Published in Drug Delivery, 2021
Xinran Wang, Cai Zhang, Ning Han, Juyuan Luo, Shuofeng Zhang, Chunguo Wang, Zhanhong Jia, Shouying Du
Although the extensive pharmacological activity of scutellarin has attracted the attention of researchers, as a BCS class IV drug, its low solubility and low permeability lead to poor pharmacokinetic properties, which seriously hinders the further development of this compound. The oral bioavailability of scutellarin in rats and beagles was 10.6 and 0.4% (Huang et al., 2005), respectively. Plasma Cmax was < 5.0 ng/mL when 60 mg of scutellarin was taken orally in humans (Lu et al., 2010). To improve its pharmaceutical properties, structural modification and dosage form optimization were tried. In terms of structural modification, the researchers introduced hydrophilic fragments into the carboxyl group or 4′-phenolic hydroxyl group of scutellarin (Marina Shamis and Shabat, 2003; Ma et al., 2015) to improve the water solubility of the molecule (Figure 2). Unfortunately, although this solution could remarkably improve the water solubility of the molecule, it did not show significant improvement in oral absorption. On the other hand, the encapsulation of scutellarin in liposomes, nanoparticles, nanoemulsion, and other dosage forms can improve the gastrointestinal stability and permeability of drugs (Mu and Høy, 2004; Peng Dayan, 2011; Ma et al., 2015; Wang et al., 2017; Markovic et al., 2020), and its relative oral bioavailability (Frel) and area under the drug-time curve (AUC) can be increased by 2- to 3-fold. However, the deficiency of low drug loading has brought inconvenience to its clinical application. How to improve the oral bioavailability of scutellarin is still an urgent problem.
Inhibition of CYP3A4 and CYP3A5 expression by scutellarin is not mediated via the regulation of hsa-miR-27a, 27b, 148a, 298 and 451a levels
Published in Xenobiotica, 2020
Weiyao Ding, Change Cao, Yangyang Gao, Xuan Zhou, Yong Lai
Scutellarin, a flavonoid glycoside that is found in the dried whole traditional Chinese herb Erigeron breviscapous (Erigeron scutellarin (Vant.) Hand. Mazz.), is the main representative active component in breviscapine tablets, which are commonly used in clinical practice to treat cardio-cerebrovascular diseases (Gao et al., 2017). As required by the Chinese Pharmacopoeia, the scutellarin content in breviscapine tablets used in clinical practice should not be less than 90.0% for oral administration, or 98.0% for administration via injection (Pharmacopoeia, 2015). Because of the complexity of cardio-cerebrovascular diseases, combined drug treatment on a long-term basis is very common. As scutellarin is one of the most commonly used medicines to treat cardio-cerebrovascular diseases, interactions between scutellarin and other drugs are likely to occur frequently. Studies have demonstrated that scutellarin significantly inhibits cytochrome P450 3 A (CYP3A) activity in rats (Z et al., 2014). Therefore, we hypothesised that scutellarin might affect the metabolism of CYP3A substrates when used in combination with them, thereby inducing herb − drug interactions (HDI). Combined drug treatment could trigger serious adverse reactions, leading to treatment failure and even life-threatening side effects. Furthermore, the mechanisms by which scutellarin influences the CYP3A expression are still unclear, and elucidating these precise mechanisms is of great significance for the rational use of drugs in clinical practice.