Selagintriflavonoids with BACE1 inhibitory activity from the fern Selaginella doederleinii

Zou, Zhen‐Xing; Xu, Ping; Zhang, Guogang; Cheng, Fei; Chen, Kai; Li, Jing; Zhu, Weixing; Cao, Dong‐Sheng; Xu, Kang‐Ping; Tan, Gui‐Shan

doi:10.1016/j.phytochem.2016.11.011

Cited by 26 publications

(20 citation statements)

References 41 publications

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“…Other triflavonoids derivatives, isolated from Selaginella doederleinii (Selaginellaceae) plant, have been investigated and showed promising BACE1 inhibitory activity. S. doederleinii is commonly used in Chinese herbal medicine as anti‐inflammatory, anticancer, and cardioprotective agent . Zou et al have successfully isolated several triflalvonoids, for example, selagin triflavonoids 25 , which possesses trimeric scaffolds isolated from S. doederleinii herb.…”

Section: Bace1 As a Potential Target For The Treatment Of Alzheimer'smentioning

confidence: 99%

“…An in vitro study using a fluorescence resonance energy transfer (FRET) technique displayed that compound 25 was the most potent BACE1 inhibitor with an IC 50 of 0.75 μM, while compound 26 was the weakest inhibitor (IC 50 = 46.99 μM). Moreover, SAR study suggested that a selagin triflavonoid with a naringenin unit (compound 25 ) rather than an apigenin unit (compound 26 ) is preferred, and have enhanced activity …”

Section: Bace1 As a Potential Target For The Treatment Of Alzheimer'smentioning

confidence: 99%

“…S. doederleinii is commonly used in Chinese herbal medicine as anti-inflammatory, anticancer, and cardioprotective agent. 81 . Moreover, SAR study suggested that a selagin triflavonoid with a naringenin unit (compound 25) rather than an apigenin unit (compound 26) is preferred, and have enhanced activity.…”

Section: Naturally-occurring Bace1 Inhibitorsmentioning

confidence: 99%

“…Moreover, SAR study suggested that a selagin triflavonoid with a naringenin unit (compound 25) rather than an apigenin unit (compound 26) is preferred, and have enhanced activity. 81 Another study was performed on Leea indica plant by Hosen et al, where 40 molecules were isolated from different parts of the plant. 82 L. indica is a huge shrub and its leaves were used in folk medicine as antispasmodic, anticancer, and antidiarrheal remedy.…”

Section: Naturally-occurring Bace1 Inhibitorsmentioning

confidence: 99%

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BACE1 inhibitors: Current status and future directions in treating Alzheimer's disease

Moussa-Pacha

Abdin

Omar

et al. 2019

Medicinal Research Reviews

185

169

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Alzheimer's disease (AD) is an irreversible, progressive neurodegenerative brain disorder with no current cure. One of the important therapeutic approaches of AD is the inhibition of β‐site APP cleaving enzyme‐1 (BACE1), which is involved in the rate‐limiting step of the cleavage process of the amyloid precursor protein (APP) leading to the generation of the neurotoxic amyloid β (Aβ) protein after the γ‐secretase completes its function. The produced insoluble Aβ aggregates lead to plaques deposition and neurodegeneration. BACE1 is, therefore, one of the attractive targets for the treatment of AD. This approach led to the development of potent BACE1 inhibitors, many of which were advanced to late stages in clinical trials. Nonetheless, the high failure rate of lead drug candidates targeting BACE1 brought to the forefront the need for finding new targets to uncover the mystery behind AD. In this review, we aim to discuss the most promising classes of BACE1 inhibitors with a description and analysis of their pharmacodynamic and pharmacokinetic parameters, with more focus on the lead drug candidates that reached late stages of clinical trials, such as MK8931, AZD‐3293, JNJ‐54861911, E2609, and CNP520. In addition, the manuscript discusses the safety concerns and insignificant physiological effects, which were highlighted for the most successful BACE1 inhibitors. Furthermore, the review demonstrates with increasing evidence that despite tremendous efforts and promising results conceived with BACE1 inhibitors, the latest studies suggest that their clinical use for treating Alzheimer's disease should be reconsidered. Finally, the review sheds light on alternative therapeutic options for targeting AD.

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Section: Bace1 As a Potential Target For The Treatment Of Alzheimer'smentioning

confidence: 99%

Section: Bace1 As a Potential Target For The Treatment Of Alzheimer'smentioning

confidence: 99%

Section: Naturally-occurring Bace1 Inhibitorsmentioning

confidence: 99%

Section: Naturally-occurring Bace1 Inhibitorsmentioning

confidence: 99%

See 2 more Smart Citations

BACE1 inhibitors: Current status and future directions in treating Alzheimer's disease

Moussa-Pacha

Abdin

Omar

et al. 2019

Medicinal Research Reviews

185

169

View full text Add to dashboard Cite

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“…It is widely used to treat sore throats, rheumatic arthralgia pain, nasopharyngeal carcinoma, chorionic carcinoma, lung cancer, cervical cancer and a variety of diseases such as traumatic bleeding [8][9][10][11][12][13]. However, its anti-tumor effect of the material basis has reported relatively less.…”

Section: Discussionmentioning

confidence: 99%

Identification of chemical constituents of Selaginella doederleinii Hieron

Brad¹,

Zhang²,

Xu³

et al. 2017

Proceedings of the 2017 6th International Conference on Energy and Environmental Protection (ICEEP 2017)

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Abstract.To determine the chemical constituents of Selaginella doederleinii Hieron. The compounds were isolated and purified from the Ethyl Acetate Fraction from Ethanol Extract of Selaginella doederleinii Hieron by multiple chromatographic techniques including macroporous resin, polyamide, silica gel, Sephadex LH-20 and pre-HPLC. The structures were identified on the basis of thierphysico-chemical properties and spectroscopic data analyses

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