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Effects of Traditional Chinese Medicinal Plants on Antiinsulin Resistance Bioactivity of DXMS-Induced Insulin Resistant HepG2 Cells
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Jun-Zeng Ma, Li-Xin Yang, Xiao-Ling Shen, Ji-Huan Qin, Li-Lan Deng, Selena Ahmed, Hong-Xi Xu, Da-Yuan Xue, Jiang-Xia Ye, Gang Xu
Natural Products and Bioprospecting. 2014, 4 (4): 197-206.
DOI: 10.1007/s13659-014-0028-0
Medicinal plants have a long history of use in China to treat diabetic symptoms. Ancient Chinese medical manuscripts and ethnobotanical surveys document plant remedies that continue to be actively used in China for the treatment of diabetic symptoms. Based on a systematic ancient Chinese medical manuscripts review in combination with ethnobotanical survey, 16 medicinal plants for the traditional treatment of diabetic symptoms were identified for the evaluation of anti-insulin resistance bioactivity. The biological activity of 16 medicinal plants was tested on dexamethasone(DXMS)-induced insulin resistant HepG2 cells. The result shows that 11 of the 16 medicinal plants enhanced glucose uptake of DXMS-induced insulin resistant HepG2 cells, thereby demonstrating their ability to increase insulin sensitivity, other five medicinal plants including Astragalus membranaceus were found ineffective. The study shows that ancient Chinese medical manuscripts and ethnobotanical surveys on plants for the prevention and treatment of diabetic symptoms provide a promising knowledge base for drug discovery to mitigate the global diabetes epidemic.
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Three New Humulane Sesquiterpenes from Cultures of the Fungus Antrodiella albocinnamomea
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Zi-Ming Chen, Qiong-Ying Fan, Xia Yin, Xiao-Yan Yang, Zheng-Hui Li, Tao Feng, Ji-Kai Liu
Natural Products and Bioprospecting. 2014, 4 (4): 207-211.
DOI: 10.1007/s13659-014-0032-4
Three new humulane-type sesquiterpenes, antrodols A-C(1-3), were isolated from cultures of the fungus Antrodiella albocinnamomea. Their structures were elucidated on the basis of extensive spectroscopic analysis. Antrodols A-C(1-3) are first examples of humulane-type sesquiterpenes isolated from cultures of higher fungi, and antrodol A(1) was the first report of humulane-type sesquiterpene with a methyl rearranged at C-3. All compounds were evaluated in the enzyme inhibition assay against two protein-tyrosine phosphatases(PTPs):MEG2 and PTP1Bc.
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Lycopodine-Type Alkaloids from Lycopodium japonicum
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Juan He, Xing-De Wu, Fei Liu, Yu-Cheng Liu, Li-Yan Peng, Yu Zhao, Xiao Cheng, Huai-Rong Luo, Qin-Shi Zhao
Natural Products and Bioprospecting. 2014, 4 (4): 213-219.
DOI: 10.1007/s13659-014-0027-1
Three new lycopodine-type alkaloids, 4α-hydroxyanhydrolycodoline(1), 4α, 6α-dihydroxyanhydrolycodoline(2), and 6-epi-8β-acetoxylycoclavine(3), and an artifact, lycoposerramine G nitrate(4), along with seventeen related known compounds, were isolated from the club moss Lycopodium japonicum Thunb. ex Murray(Lycopodiaceae). Their structures were elucidated by extensive spectroscopic methods as well as X-ray analysis. Compounds 1-4 were evaluated for their acetylcholine esterase inhibitory activity.
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Carinatines A and B, Lycopodium Alkaloids from Phlegmariurus carinatus
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Fei Liu, Yu-Cheng Liu, Wei-Wei Jiang, Juan He, Xing-De Wu, Li-Yan Peng, Jia Su, Xiao Cheng, Qin-Shi Zhao
Natural Products and Bioprospecting. 2014, 4 (4): 221-225.
DOI: 10.1007/s13659-014-0030-6
Carinatine A(1), a C16N2-type Lycopodium alkaloid possessing a 5/6/6/6 ring system formed by a new C-4/C-12 bond, and carinatine B(2), the first derivative of lycojaponicumin C, along 16 known compounds, were isolated from the whole plant of Phlegmariurus carinatus. Their structures were elucidated based on the spectroscopic data. The two new isolates were no inhibitory activity for the acetylcholinesterase(AChE).
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Highly Oxygenated Limonoids and Lignans from Phyllanthus flexuosus
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Jian-Qiang Zhao, Yan-Ming Wang, Hong-Tao Zhu, Dong Wang, Sheng-Hong Li, Rong-Rong Cheng, Chong-Ren Yang, Yi-Fei Wang, Min Xu, Ying-Jun Zhang
Natural Products and Bioprospecting. 2014, 4 (4): 233-242.
DOI: 10.1007/s13659-014-0026-2
Two new highly oxygenated limonoids, flexuosoids A(1) and B(2), and three new arylnaphthalene lignan glycosides, phyllanthusmins D-F(3-5), were isolated from the roots of Phyllanthus flexuosus, in addition to three known lignans, phyllanthusmin C, arabelline, and(+)-diasyringaresinol. Their structures were elucidated on the basis of detailed spectroscopic analysis and chemical methods. Compounds 1 and 2, two new decaoxygenated limonoids with a C-19/29 lactol bridge and heptaoxygenated substituents at C-1, C-2, C-3, C-7, C-11, C-17, and C-30, represent the second example of limonoids in the Euphorbiaceae family. Most of the isolates were tested for their antifeedant, anti-herpes simplex virus 1, and cytotoxic activities. The new limonoids 1 and 2 showed promising antifeedant activity against the beet army worm(Spodoptera exigua) with EC50 values of 25.1 and 17.3 μg/cm2, respectively. In addition, both of them displayed moderate cytotoxicity against the ECA109 human esophagus cancer cell line, along with the known lignan glycoside, phyllanthusmin C, with the IC50 values of 11.5(1), 8.5(2), and 7.8(phyllanthusmin C) μM, respectively.
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Anti-onchocerca Metabolites from Cyperus articulatus: Isolation, In Vitro Activity and In Silico ‘Drug-Likeness’
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Jonathan Alunge Metuge, Smith B. Babiaka, James A. Mbah, Fidele Ntie-Kang, Godfred A. Ayimele, Fidelis Cho-Ngwa
Natural Products and Bioprospecting. 2014, 4 (4): 243-249.
DOI: 10.1007/s13659-014-0023-5
The aims of this investigation were to isolate active ingredients from the roots/rhizomes of Cyperus articulatus used as herbal medicine in Cameroon for the treatment of human onchocerciasis and to assess the efficacy of the metabolites on the Onchocerca worm. The antifilarial activity was evaluated in vitro on microfilariae(Mfs) and adult worms of the bovine derived Onchocerca ochengi, a close relative of Onchocerca volvulus. Cytotoxicity was assessed in vitro on monkey kidney epithelial cells. The structures of the active compounds were determined using spectroscopic methods and their drug-likeness evaluated using Lipinski parameters. Two secondary metabolites, AMJ1[containing mustakone(1) as the major component] and linoleic acid or(9Z, 12Z)-octadeca-9, 12-dienoic acid(2) were isolated. Both compounds were found to kill both the microfilariae and adult worms of O. ochengi in a dose dependent manner. The IC50s for AMJ1 were 15.7 μg/mL for Mfs, 17.4 μg/mL for adult males and 21.9 μg/mL for adult female worms while for linoleic acid the values were, 15.7 μg/mL for Mfs, 31.0 μg/mL for adult males and 44.2 μg/mL for adult females. The present report provides the first ever evidence of the anti-Onchocerca efficacy of AMJ1 and linoleic acid. Thus, these secondary metabolites may provide a lead for design and development of new antifilarial agents.
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Molecular Docking of Bacosides with Tryptophan Hydroxylase: A Model to Understand the Bacosides Mechanism
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David Mary Rajathei, Jayakumar Preethi, Hemant K. Singh, Koilmani Emmanuvel Rajan
Natural Products and Bioprospecting. 2014, 4 (4): 251-255.
DOI: 10.1007/s13659-014-0031-5
Tryptophan hydroxylase(TPH) catalyses L-tryptophan into 5-hydroxy-L-tryptophan, which is the first and ratelimiting step of serotonin(5-HT) biosynthesis. Earlier, we found that TPH2 up-regulated in the hippocampus of postnatal rats after the oral treatment of Bacopa monniera leaf extract containing the active compound bacosides. However, the knowledge about the interactions between bacosides with TPH is limited. In this study, we take advantage of in silico approach to understand the interaction of bacoside-TPH complex using three different docking algorithms such as HexDock, PatchDock and AutoDock. All these three algorithms showed that bacoside A and A3 well fit into the cavity consists of active sites. Further, our analysis revealed that major active compounds bacoside A3 and A interact with different residues of TPH through hydrogen bond. Interestingly, Tyr235, Thr265 and Glu317 are the key residues among them, but none of them are either at tryptophan or BH4 binding region. However, its note worthy to mention that Tyr 235 is a catalytic sensitive residue, Thr265 is present in the flexible loop region and Glu317 is known to interacts with Fe. Interactions with these residues may critically regulate TPH function and thus serotonin synthesis. Our study suggested that the interaction of bacosides(A3/A) with TPH might up-regulate its activity to elevate the biosynthesis of 5-HT, thereby enhances learning and memory formation.
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