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Carboxylesterase Inhibitors: Relevance for Pharmaceutical Applications
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Natural protostane triterpenoids, such as protopanaxadiol and protopanaxatriol, exhibit less potency and poor selectivity on CES1, but display strong inhibitory effects on CES2, suggesting that the long alkyl chain at the C-20 site is unbeneficial for CES1 inhibition (Zou et al., 2017). Recently, 22 protostane triterpenoids have been isolated from the rhizome of Alismaorientale (Mai et al., 2015b), five of which, including alismanol B, 25-O-ethylalisol A, alismanol D, alismanol F, and 11-deoxyalisol A, strongly inhibited CES2 with the IC50 values between 2.02 and 8.68 μM (Table 9.7) (Mai et al., 2015b). Alisol G (25-anhydroalisol A) is a major protostane triterpene obtained from dried rhizomes of Alismaorientalis. Following the biotransformation mediated by P. janthinellumAS 3.510, the metabolites of alisol G, including 25S-25,26-epoxy-alisol G, alisol G (23,24)-diol acetonide and 25,26-dihydroxy-alisol G (23,24)-diol acetonide were obtained, which showed significant CES2 inhibitory effects, with the IC50 values of 6.81, 3.38, and 6.33 μM, respectively (Mai et al., 2015a).
Effects of different drying methods on drying characteristics, microstructure, quality, and energy consumption of Panax Notoginseng roots (Araliaceae)
Published in Drying Technology, 2022
Dalong Jiang, Hongwei Xiao, Zhian Zheng
Panax Notoginseng (Burk.) F. H. Chen (Araliaceae), a traditional Chinese medicinal herb, mainly grows in southwestern China, Burma, and Nepal. In 2016, the total planting area of Panax Notoginseng in Yunnan province, China was 3,000 hm2.[1]Panax Notoginseng roots have been reported to have antihypertensive, antithrombotic, anti-atherosclerotic, and neuroprotective activities.[2,3] The dried roots of Panax Notoginseng have been classified as a healthy promoting dietary supplement.[4] Over 200 chemical constituents were isolated from Panax Notoginseng, including saponins (PNS), polysaccharides, dencichine, amino acids, flavonoids, phytosterols, cyclopeptides, saccharides, fatty acids, volatile oils, aliphatic acetylene hydrocarbons, and trace elements.[5,6] PNS are the main active compounds of Panax Notoginseng, and more than 100 PNS have been isolated and identified, including ginsenosides, notoginsenosides, and gypenosides. They belong to dammarane-type ginsenoside, which includes two classifications, namely the 20(S)-protopanaxadiol (PDS) and 20(S)-protopanaxatriol (PTS). PNS contain high levels of ginsenoside Rb1, Rd (PDS classification) and ginsenoside Rg1, Re, notoginsenoside R1 (PTS classification). The top five saponins, that is, ginsenoside Rb1, ginsenoside Rg1, notoginsenoside R1, ginsenoside Rd, and ginsenoside Re, are most often used in pharmacy and medicine.[7] Additionally, ginsenoside R1 is an important component of Xueshuantong capsule.[8] The sum of R1, Rg1, Re, Rd, and Rb1 contents is equal to the PNS value. Recently, PNS were shown to have the function of lowering atherosclerosis and thrombosis, preventing myocardial ischemia-reperfusion injury, enhancing cerebral microcirculation and protecting nerve cells.[9]
Effect of pulsed vacuum drying on drying kinetics and quality of roots of Panax notoginseng (Burk.) F. H. Chen (Araliaceae)
Published in Drying Technology, 2021
Dalong Jiang, Hongwei Xiao, Magdalena Zielinska, Guangfei Zhu, Tianyu Bai, Zhian Zheng
Panax notoginseng (Burk.) F. H. Chen (Araliaceae), a traditional Chinese medicinal herb, mainly grows in southwestern China, Burma, and Nepal. In 2016, the total planting area of Panax notoginseng in Yunnan province, China, was 3,000 hm.[1,2]Panax notoginseng roots have been reported to have antihypertensive, antithrombotic, anti-atherosclerotic, and neuroprotective activities.[2,3] The dried roots of Panax notoginseng have been classified as a healthy promoting dietary supplement.[4] Over 200 chemical constituents were isolated from Panax notoginseng, including saponins (PNS), polysaccharides, dencichine, amino acids, flavonoids, phytosterols, cyclopeptides, saccharides, fatty acids, volatile oils, aliphatic acetylene hydrocarbons, and trace elements.[5,6] PNS are the main active compounds of Panax notoginseng, and more than 100 PNS have been isolated and identified, including ginsenosides, notoginsenosides, and gypenosides. They belong to dammarane-type ginsenoside, which includes two classifications, namely the 20(S)-protopanaxadiol (PDS) and 20(S)-protopanaxatriol (PTS). PNS contains high levels of ginsenoside Rb1, Rd (PDS classification) and ginsenoside Rg1, Re, notoginsenoside R1 (PTS classification). The top five saponins, i.e., ginsenoside Rb1, ginsenoside Rg1, notoginsenoside R1, ginsenoside Rd, and ginsenoside Re, are most often used in pharmacy and medicine.[7] Additionally, ginsenoside R1 is an important component of Xueshuantong capsule.[8] The sum of R1, Rg1, Re, Rd, and Rb1 contents is equal to the PNS value. Recently, PNS was shown to have the function of lowering atherosclerosis and thrombosis, preventing myocardial ischemia–reperfusion injury, enhancing cerebral microcirculation and protecting nerve cells.[9]
Inhibitory effects of protopanaxatriol type ginsenoside fraction (Rgx365) on particulate matter-induced pulmonary injury
Published in Journal of Toxicology and Environmental Health, Part A, 2019
Wonhwa Lee, Sae-Kwang Ku, Ji-Eun Kim, Soo-Hyun Cho, Gyu-Yong Song, Jong-Sup Bae
Black ginseng (BG), steamed 9 times, as well as dried ginseng, has received attention from scientists because of the various pharmacological properties including anti-diabetic, wound healing, immune-stimulatory, and anti-antioxidant actions (Kang et al. 2017; Park et al. 2018; Saba et al. 2018). Ginsenosides, the major bioactive constituents of ginseng, are classified based upon their steroidal structure and number of hydroxyl groups/sugar moieties attached. These include protopanaxadiol (PPD) and protopanaxatriol (PPT) type. The major PPD-type ginsenosides of unsteamed ginseng are ginsenoside Rb1, Rc, Rd, and the major PPT-type ginsenosides of unsteamed ginseng are ginsenoside Re, Rf, Rg1. Because these major PPD and PPT type ginsenosides of ginseng contain high molecular weights and several types of sugars, their polarity is very high. Generally, the log octanol/water partition coefficient (log P) of a molecule reflects its ability to pass through the lipid bilayer (Walter and Gutknecht 1986). Because log P of ginsenoside Rg1 (Molecular weight; 801) with low polarity is 1.12 and log P of ginsenoside Re (Molecular weight; 947.15) with high polarity is −0.03, ginsenoside Rg1 is able to penetrate cells but ginsenoside Re cannot (Su et al. 2015). Interestingly, during the manufacturing process of BG, the structure of ginsenoside was converted into low molecular weights and low polarity rare ginsenosides occurred hydrolysis, isomerization, and dehydration at C-20, and hydrolysis also took place at C-3 or C-6 in the aglycon skeleton (Sun et al. 2009a). The main low polarity PPT-type ginsenosides of BG were rare ginsenoside Rg2, Rg4, Rg6, Rh1, and Rh4. Recently, it was reported that these rare ginsenosides Rg2, Rg4, Rg6, Rh1, and Rh4 exhibited potent anti-tumor, anti-inflammatory, and immunomodulatory effects (Duan et al. 2018; Tam et al. 2018; Yang, Ye, and Sun 2007). However, since the content of each rare ginsenoside (Rg2, Rg4, Rg6, Rh1, and Rh4) in BG was not only low but also very expensive, it was necessary to develop a new efficient manufacturing method of single rare ginsenoside and fraction of rare ginsenosides such as Rgx365 (Figure 1). Therefore, it was of interest to convert single ginsenoside Re, which was largely isolated from the ginseng leaf instead of root, into PPT type rare ginsenosides Rg2, Rg4, Rg6, Rh1, and Rh4, respectively. The Rgx365 was a PPT-type rare ginsenoside fraction containing five types of the above rare ginsenosides (Rg2, Rg4, Rg6, Rh1, and Rh4). Based upon the knowledge of the abovementioned effects of Rgx365, results from previous studies (Chen and Jia, 2013; Cho et al. 2016; Ren et al. 2017), it was postulated that Rgx365 might exhibit beneficial effects against PM-induced pulmonary injury. In this study, a mouse model was used to determine the influence of Rgx365 on pulmonary histology, inflammation, and oxidative stress following PM2.5 exposure. An in vitro model was also employed to study whether Rgx365 might inhibit PM2.5-induced vascular barrier disruptive responses.