, Volume 11 Issue 6 Previous Issue  
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    REVIEWS
    Advances in Research on Chemical Constituents and Their Biological Activities of the Genus Actinidia   Collect
    Jin-Tao Ma, Da-Wei Li, Ji-Kai Liu, Juan He
    Natural Products and Bioprospecting. 2021, 11 (6): 573-609.   DOI: 10.1007/s13659-021-00319-8
    Abstract ( 5913 )   HTML ()     PDF (4644KB) ( 9410 )  
    Kiwi, a fruit from plants of the genus Actinidia, is one of the famous fruits with thousand years of edible history. In the past twenty years, a great deal of research has been done on the chemical constituents of the Actinidia species. A large number of secondary metabolites including triterpenoids, flavonoids, phenols, etc. have been identified from differents parts of Actinidia plants, which exhibited significant in vitro and in vivo pharmacological activities including anticancer, anti-inflammatory, neuroprotective, anti-oxidative, anti-bacterial, and anti-diabetic activities. In order to fully understand the chemical components and biological activities of Actinidia plants, and to improve their further research, development and utilization, this review summarizes the compounds extracted from different parts of Actinidia plants since 1959 to 2020, classifies the types of constituents, reports on the pharmacological activities of relative compounds and medicinal potentials.
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    Natural Products as Potential Lead Compounds for Drug Discovery Against SARS-CoV-2   Collect
    Oyere Tanyi Ebob, Smith B. Babiaka, Fidele Ntie-Kang
    Natural Products and Bioprospecting. 2021, 11 (6): 611-628.   DOI: 10.1007/s13659-021-00317-w
    Abstract ( 5937 )   HTML ()     PDF (4656KB) ( 9105 )  
    For the past 2 years, the coronavirus responsible for the COVID-19 infection has become a world pandemic, ruining the lives and economies of several nations in the world. This has scaled up research on the virus and the resulting infection with the goal of developing new vaccines and therapies. Natural products are known to be a rich source of lead compounds for drug discovery, including against infectious diseases caused by microbes (viruses, bacteria and fungi). In this review article, we conducted a literature survey aimed at identifying natural products with inhibitory concentrations against the coronaviruses or their target proteins, which lie below 10 μM. This led to the identification of 42 compounds belonging to the alkaloid, flavonoid, terpenoid, phenolic, xanthone and saponin classes. The cut off concentration of 10 μM was to limit the study to the most potent chemical entities, which could be developed into therapies against the viral infection to make a contribution towards limiting the spread of the disease.
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    Anticancer Properties and Mechanism of Action of Oblongifolin C, Guttiferone K and Related Polyprenylated Acylphloroglucinols   Collect
    Christian Bailly, Gérard Vergoten
    Natural Products and Bioprospecting. 2021, 11 (6): 629-641.   DOI: 10.1007/s13659-021-00320-1
    Abstract ( 6522 )   HTML ()     PDF (7410KB) ( 8668 )  
    Polyprenylated acylphloroglucinols represent an important class of natural products found in many plants. Among them, the two related products oblongifolin C (Ob-C) and guttiferone K (Gt-K) isolated from Garcinia species (notably from edible fruits), have attracted attention due to their marked anticancer properties. The two compounds only differ by the nature of the C-6 side chain, prenyl (Gt-K) or geranyl (Ob-C) on the phloroglucinol core. Their origin, method of extraction and biological properties are presented here, with a focus on the targets and pathways implicated in their anticancer activities. Both compounds markedly reduce cancer cell proliferation in vitro, as well as tumor growth and metastasis in vivo. They are both potent inducer of tumor cell apoptosis, and regulation of autophagy flux is a hallmark of their mode of action. The distinct mechanism leading to autophagosome accumulation in cells and the implicated molecular targets are discussed. The specific role of the chaperone protein HSPA8, known to interact with Ob-C, is addressed. Molecular models of Gt-K and Ob-C bound to HSPA8 provide a structural basis to their common HSPA8-binding recognition capacity. The review shed light on the mechanism of action of these compounds, to encourage their studies and potential development.
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    ORIGINAL ARTICLES
    Six New 3,5-Dimethylcoumarins from Chelonopsis praecox, Chelonopsis odontochila and Chelonopsis pseudobracteata   Collect
    Chang-An Geng, Zhen-Tao Deng, Qian Huang, Chun-Lei Xiang, Ji-Jun Chen
    Natural Products and Bioprospecting. 2021, 11 (6): 643-649.   DOI: 10.1007/s13659-021-00318-9
    Abstract ( 5626 )   HTML ()     PDF (4734KB) ( 8699 )  
    Ten 3,5-dimethylcoumarins (1-6 and 8-11) involving six new ones (1-6), together with a known 3-methylcoumarin (7), were isolated from the aerial parts of three Chelonopsis plants, C. praecox, C. odontochila, and C. pseudobracteata. The structures of the new compounds were determined by extensive HRESIMS, 1D and 2D NMR spectroscopic analyses. According to the substitution at C-5, these coumarins were classified into 5-methyl, 5-hydroxymethyl, 5-formyl, and 5-nor types. All the isolates were assayed for their inhibition on α-glucosidase, protein tyrosine phosphatase 1B, and T-cell protein tyrosine phosphatase in vitro.
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    Furostanol Saponins from Asparagus cochinchinensis and Their Cytotoxicity   Collect
    Ruo-Song Zhang, Yang-Yang Liu, Pei-Feng Zhu, Qiong Jin, Zhi Dai, Xiao-Dong Luo
    Natural Products and Bioprospecting. 2021, 11 (6): 651-658.   DOI: 10.1007/s13659-021-00321-0
    Abstract ( 5716 )   HTML ()     PDF (5639KB) ( 8377 )  
    Phytochemical investigation on the roots of Asparagus cochinchinensis led to the isolation of one new furostanol saponin, named 26-O-β-D-glucopyranosyl-22α-hydroxyl-(25R)-Δ5(6)-furost-3β,26-diol-3-O-α-L-rhamnopyranosyl-(1→ 2)-[β-Dglucopyranosyl-(1→ 4)-α-L-rhamnopyranosyl-(1→ 4)]-β-D-glucopyranoside (1), along with three known congeners (2-4). The structure of new saponin was elucidated via comprehensive inspection of its HRMS and NMR spectral data as well as chemical technology, whereas those of known ones were identified by comparison of their NMR and MS spectral data with those reported in literatures. All isolated saponins were evaluated for their cytotoxic effects on two human liver (MHCC97H) and lung adenocarcinoma (H1299) cancer cells in vitro. Among them, both 1 and 2 showed significant cytotoxicity against above mentioned cell lines. Further studies revealed that these two saponins could significantly inhibit their proliferation of MHCC97H and H1299 cells.
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    Scutellarin Reduces Cerebral Ischemia Reperfusion Injury Involving in Vascular Endothelium Protection and PKG Signal   Collect
    Ya-Juan Chen, Chen Chen, Meng-Yuan Li, Qing-Qing Li, Xiu-Juan Zhang, Rong Huang, Xing-Wei Zhu, Chun-Yun Bai, Liu-Yi Zhang, Pei-Hua Peng, Wei-Min Yang
    Natural Products and Bioprospecting. 2021, 11 (6): 659-670.   DOI: 10.1007/s13659-021-00322-z
    Abstract ( 5160 )   HTML ()     PDF (6783KB) ( 7198 )  
    Flavonoid glycoside scutellarin (SCU) has been widely applied in the treatment of cerebral ischemic diseases in China. In this article, we conducted research on the working mechanisms of SCU in hypoxia reoxygenation (HR) injury of isolated cerebral basilar artery (BA) and erebral ischemia reperfusion (CIR) injury in rat models. In isolated rat BA rings, HR causes endothelial dysfunction (ED) and acetylcholine (ACh) induces endothelium-dependent vasodilation. The myography result showed that SCU (100 μM) was able to significantly improve the endothelium-dependent vasodilation induced by Ach. However, SCU did not affect the ACh-induced relaxation in normal BA. Further studies suggested that SCU (10-1000 μM) dose-dependently induced relaxation in isolated BA rings which were significantly blocked by the cGMP dependent protein kinase (PKG) inhibitor Rp-8-Br-cGMPs (PKGI-rp, 4 μM). Pre-incubation with SCU (500 μM) reversed the impairment of endothelium-dependent vasodilation induced by HR, but the reversing effect was blocked if PKGI-rp (4 μM) was added. The brain slice staining test in rats' model of middle cerebral artery occlusion (MCAO) induced CIR proved that the administration of SCU (45, 90 mg/kg, iv) significantly reduced the area of cerebral infarction. The Western blot assay result showed that SCU (45 mg/kg, iv) increased brain PKG activity and PKG protein level after CIR surgery. In conclusion, our findings suggested that SCU possesses the ability of protecting brain cells against CIR injury through vascular endothelium protection and PKG signal.
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    Isoprenylated Flavonoids as Cav3.1 Low Voltage-Gated Ca2+ Channel Inhibitors from Salvia digitaloides   Collect
    Jian-Jun Zhao, Song-Yu Li, Fan Xia, Ya-Li Hu, Yin Nian, Gang Xu
    Natural Products and Bioprospecting. 2021, 11 (6): 671-678.   DOI: 10.1007/s13659-021-00307-y
    Abstract ( 5588 )   HTML ()     PDF (5127KB) ( 6842 )  
    Saldigones A-C (1, 3, 4), three new isoprenylated flavonoids with diverse flavanone, pterocarpan, and isoflavanone architectures, were characterized from the roots of Salvia digitaloides, together with a known isoprenylated flavanone (2). Notably, it's the first report of isoprenylated flavonoids from Salvia species. The structures of these isolates were elucidated by extensive spectroscopic analysis. All of the compounds were evaluated for their activities on Cav3.1 low voltage-gated Ca2+ channel (LVGCC), of which 2 strongly and dose-dependently inhibited Cav3.1 peak current.
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    CORRECTION
    Correction to: Isoprenylated Flavonoids as Cav3.1 Low Voltage-Gated Ca2+ Channel Inhibitors from Salvia digitaloides   Collect
    Jian-Jun Zhao, Song-Yu Li, Fan Xia, Ya-Li Hu, Yin Nian, Gang Xu
    Natural Products and Bioprospecting. 2021, 11 (6): 679-679.   DOI: 10.1007/s13659-021-00308-x
    Abstract ( 4042 )   HTML ()     PDF (3114KB) ( 4796 )  
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2021, Volume 11 Issue 6