Cleaner production of baicalein by novel high-temperature-little-acid hydrolysis of baicalin
Baicalein, usually obtained after the removal of 7-O-β-D-glucuronic acid from baicalin, has strong pharmacological activity. In this study, a novel strategy for efficient and eco-friendly preparation of baicalein was established by high-temperature-little-acid hydrolysis of baicalin. The effects of...
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2024-12-01
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| Series: | Green Chemistry Letters and Reviews |
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| Online Access: | https://www.tandfonline.com/doi/10.1080/17518253.2024.2319698 |
| _version_ | 1826948389816762368 |
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| author | Lingling Tang Jiali Shao Hanxue Zheng Jixuan Chen Guohua Xia Huan Yang Yaya Yang Yuping Shen |
| author_facet | Lingling Tang Jiali Shao Hanxue Zheng Jixuan Chen Guohua Xia Huan Yang Yaya Yang Yuping Shen |
| author_sort | Lingling Tang |
| collection | DOAJ |
| description | Baicalein, usually obtained after the removal of 7-O-β-D-glucuronic acid from baicalin, has strong pharmacological activity. In this study, a novel strategy for efficient and eco-friendly preparation of baicalein was established by high-temperature-little-acid hydrolysis of baicalin. The effects of inorganic acids, solvents, solid–liquid ratio, HCl concentration and hydrolysis duration on the yield of baicalein were investigated by one-factor-at-a-time experiment. Then, an orthogonal experiment design was conducted for the optimal hydrolysis conditions, namely, baicalin was boiled in n-BuOH solution containing 0.50% HCl (w/v) at 130°C for 2.0 h with solid–liquid ratio at 1:25 (g/mL). In the 60-fold scale-up experiment, the yield of baicalein was achieved at 83.5% ± 6.3%, and its purity was increased from 74.2% to 98.7% after purification. Compared with reported methods, acid consumption per unit product of the newly developed strategy was approximately 80 times lower than that of conventional acid hydrolysis, and time consumption was substantially reduced. Overall, the novel strategy showed great prospects for a cleaner large-scale production of baicalein, which provides a new alternative desirable for the preparation of natural products with high efficiency and low consumption in the pharmaceutical industry. |
| first_indexed | 2024-03-07T22:49:00Z |
| format | Article |
| id | doaj.art-e9e403c3abf545e9a737ca241bc933b3 |
| institution | Directory Open Access Journal |
| issn | 1751-8253 1751-7192 |
| language | English |
| last_indexed | 2025-02-17T21:48:37Z |
| publishDate | 2024-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Green Chemistry Letters and Reviews |
| spelling | doaj.art-e9e403c3abf545e9a737ca241bc933b32024-12-06T01:41:30ZengTaylor & Francis GroupGreen Chemistry Letters and Reviews1751-82531751-71922024-12-0117110.1080/17518253.2024.2319698Cleaner production of baicalein by novel high-temperature-little-acid hydrolysis of baicalinLingling Tang0Jiali Shao1Hanxue Zheng2Jixuan Chen3Guohua Xia4Huan Yang5Yaya Yang6Yuping Shen7School of Pharmacy, Jiangsu University, Zhenjiang, People’s Republic of ChinaSchool of Pharmacy, Jiangsu University, Zhenjiang, People’s Republic of ChinaSchool of Pharmacy, Jiangsu University, Zhenjiang, People’s Republic of ChinaSchool of Pharmacy, Jiangsu University, Zhenjiang, People’s Republic of ChinaSchool of Pharmacy, Jiangsu University, Zhenjiang, People’s Republic of ChinaSchool of Pharmacy, Jiangsu University, Zhenjiang, People’s Republic of ChinaSchool of Pharmacy, Jiangsu University, Zhenjiang, People’s Republic of ChinaSchool of Pharmacy, Jiangsu University, Zhenjiang, People’s Republic of ChinaBaicalein, usually obtained after the removal of 7-O-β-D-glucuronic acid from baicalin, has strong pharmacological activity. In this study, a novel strategy for efficient and eco-friendly preparation of baicalein was established by high-temperature-little-acid hydrolysis of baicalin. The effects of inorganic acids, solvents, solid–liquid ratio, HCl concentration and hydrolysis duration on the yield of baicalein were investigated by one-factor-at-a-time experiment. Then, an orthogonal experiment design was conducted for the optimal hydrolysis conditions, namely, baicalin was boiled in n-BuOH solution containing 0.50% HCl (w/v) at 130°C for 2.0 h with solid–liquid ratio at 1:25 (g/mL). In the 60-fold scale-up experiment, the yield of baicalein was achieved at 83.5% ± 6.3%, and its purity was increased from 74.2% to 98.7% after purification. Compared with reported methods, acid consumption per unit product of the newly developed strategy was approximately 80 times lower than that of conventional acid hydrolysis, and time consumption was substantially reduced. Overall, the novel strategy showed great prospects for a cleaner large-scale production of baicalein, which provides a new alternative desirable for the preparation of natural products with high efficiency and low consumption in the pharmaceutical industry.https://www.tandfonline.com/doi/10.1080/17518253.2024.2319698Baicaleinbaicalinacid hydrolysishigh-temperature-little-acid hydrolysis |
| spellingShingle | Lingling Tang Jiali Shao Hanxue Zheng Jixuan Chen Guohua Xia Huan Yang Yaya Yang Yuping Shen Cleaner production of baicalein by novel high-temperature-little-acid hydrolysis of baicalin Green Chemistry Letters and Reviews Baicalein baicalin acid hydrolysis high-temperature-little-acid hydrolysis |
| title | Cleaner production of baicalein by novel high-temperature-little-acid hydrolysis of baicalin |
| title_full | Cleaner production of baicalein by novel high-temperature-little-acid hydrolysis of baicalin |
| title_fullStr | Cleaner production of baicalein by novel high-temperature-little-acid hydrolysis of baicalin |
| title_full_unstemmed | Cleaner production of baicalein by novel high-temperature-little-acid hydrolysis of baicalin |
| title_short | Cleaner production of baicalein by novel high-temperature-little-acid hydrolysis of baicalin |
| title_sort | cleaner production of baicalein by novel high temperature little acid hydrolysis of baicalin |
| topic | Baicalein baicalin acid hydrolysis high-temperature-little-acid hydrolysis |
| url | https://www.tandfonline.com/doi/10.1080/17518253.2024.2319698 |
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