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Natural Products and Bioprospecting

Hui Liu, Xingyong Liu, Li Zhang
The study on antitumor activities of artemisinin and its derivatives has been closely focused on in recent years. Herein, 2D and 3D QSAR analysis was performed on the basis of a series of artemisinin derivatives with known bioactivities against the non-small-cell lung adenocarcinoma A549 cells. Four QSAR models were successfully established by CoMSIA, CoMFA, topomer CoMFA and HQSAR approaches with respective characteristic values q(2) = 0.567, R(2) = 0.968, ONC = 5; q(2) = 0.547, R(2) = 0.980, ONC = 7; q(2) = 0...
November 1, 2017: Natural Products and Bioprospecting
Ahmed Mahal, Ping Wu, Zi-Hua Jiang, Xiaoyi Wei
Tetrahydrocurcumin (THC) is a major metabolite of curcumin and plays an important role in curcumin-induced biological effects. THC is a promising preventive and chemotherapeutic agent for cancer. A series of new pyrazole derivatives of THC have been synthesized as potent anticancer agents. Direct condensation of THC with various substituted hydrazines leads to new pyrazole derivatives of THC (1-18). The prepared compounds have been evaluated via in vitro MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay for their cell proliferation-inhibitory activity against human lung adenocarcinoma (A549), human cervical carcinoma (HeLa) and human breast carcinoma (MCF-7) cells...
November 1, 2017: Natural Products and Bioprospecting
Xin Wei, Li-Ping Jiang, Ying Guo, Afsar Khan, Ya-Ping Liu, Hao-Fei Yu, Bei Wang, Cai-Feng Ding, Pei-Feng Zhu, Ying-Ying Chen, Yun-Li Zhao, Yong-Bing Chen, Yi-Fen Wang, Xiao-Dong Luo
Uncaria rhynchophylla is commonly recognized as a traditional treatment for dizziness, cerebrovascular diseases, and nervous disorders in China. Previously, the neuro-protective activities of the alkaloids from U. rhynchophylla were intensively reported. In current work, three new indole alkaloids (1-3), identified as geissoschizic acid (1), geissoschizic acid N 4-oxide (2), and 3β-sitsirikine N 4-oxide (3), as well as 26 known analogues were isolated from U. rhynchophylla. However, in the neural stem cells (NSCs) proliferation assay for all isolated compounds, geissoschizic acid (1), geissoschizic acid N 4-oxide (2), isocorynoxeine (6), isorhynchophylline (7), (4S)-akuammigine N-oxide (8), and (4S)-rhynchophylline N-oxide (10) showed unexpected inhibitory activities at 10 μM...
October 2017: Natural Products and Bioprospecting
Yu-Chen Liu, Zhi-Jun Zhang, Jia Su, Li-Yan Peng, Lu-Tai Pan, Xing-De Wu, Qin-Shi Zhao
Three new lycodine-type Lycopodium alkaloids, namely 1-methyllycodine (1), 8α-hydroxy-15,16-dehydro-des-N-methyl-α-obscurine (2), N-methyl-16-hydroxyhuperzine B (3), and one new natural lycodine-type Lycopodium alkaloid, N-methylhuperzine A (4), along with 11 known analogues (5-15), were isolated from the whole plants of club moss Huperzia serrata. The structures of 1-4 were elucidated on the basis of NMR spectroscopic and mass spectrometry data. Among them, compound 1 was the first lycodine-type alkaloid possessing a methyl group at C-1...
October 2017: Natural Products and Bioprospecting
Ai-Jun Ding, Shan-Qing Zheng, Xiao-Bing Huang, Ti-Kun Xing, Gui-Sheng Wu, Hua-Ying Sun, Shu-Hua Qi, Huai-Rong Luo
Aging is a process characterized by accumulating degenerative damages, resulting in the death of an organism ultimately. The main goal of aging research is to develop therapies that delay age-related diseases in human. Since signaling pathways in aging of Caenorhabditis elegans (C. elegans), fruit flies and mice are evolutionarily conserved, compounds extending lifespan of them by intervening pathways of aging may be useful in treating age-related diseases in human. Natural products have special resource advantage and with few side effect...
October 2017: Natural Products and Bioprospecting
Li-Wen Tian, Zhen Zhang, Hai-Lan Long, Ying-Jun Zhang
The Smilax species, widely distributed in tropical region of the world and the warm areas of East Asia and North America, are extensively used as folk medicine to treat inflammatory disorders. Chemical investigation on Smilax species showed they are rich sources of steroidal saponins with diversified structure types, including spirostane, isospirostane, furostane, pregnane, and cholestane. This review mainly summarizes the steroidal saponins (1-104) reported from the genus Smilax between 1967 and 2016, and their biological activities...
August 2017: Natural Products and Bioprospecting
Rui-Min Yang, Xiu-Lei Zhang, Li Wang, Jian-Ping Huang, Jing Yang, Yi-Jun Yan, Jian-Ying Luo, Xiang-Ting Wang, Sheng-Xiong Huang
Tamoxifen resistance (TamR) is the underlying cause of treatment failure in many breast cancer patients receiving tamoxifen. In order to look for noncytotoxic natural products with the ability to reverse TamR, an extract from strain Streptomyces sp. KIB-H0495 was detected to be active. Subsequent large scale fermentation and isolation led to the isolation of four α-pyrone derivatives including two new compounds, violapyrones J (2) and K (3), and two known analogues, violapyrones B (1) and I (4). Further bioactivity assays indicated that only 1 and 3 exerted potent resensitization effects on MCF-7/TamR cells at a concentration of 1 μM...
August 2017: Natural Products and Bioprospecting
Xu-Jie Qin, Tong Shu, Qian Yu, Huan Yan, Wei Ni, Lin-Kun An, Pan-Pan Li, Yin-E Zhi, Afsar Khan, Hai-Yang Liu
Callisalignenes G-I (1-3), three new meroterpenoids of β-triketone and monoterpene, along with two known analogues (4 and 5), were isolated from Callistemon salignus. Their structures and absolute configurations were unambiguously established by a combination of NMR and MS analysis and electronic circular dichroism (ECD) evidence. Callisalignenes H (2) and I (3) have a rare sec-butyl moiety at C-7. Meroterpenoids 1-3 exhibited cytotoxicity against HCT116 cells with IC50 values of 8.51 ± 1.8, 9.12 ± 0...
August 2017: Natural Products and Bioprospecting
Xin Wei, Afsar Khan, Da Song, Zhi Dai, Ya-Ping Liu, Hao-Fei Yu, Bei Wang, Pei-Feng Zhu, Cai-Feng Ding, Xu-Dong Zhao, Yi-Fen Wang, Xiao-Dong Luo
Three new pyridine type alkaloids, (-)-vinmajpyridines A-C (1-3), along with two known alkaloids, have been isolated from the aerial parts of Vinca major cultivated in Pakistan. Their structures have been elucidated by means of NMR and HRESIMS spectroscopic data. The new alkaloids were evaluated for their cytotoxicity against glioma initiating cell lines (GITC-3(#) and GITC-18(#)), glioblastoma cell lines (U-87MG and T98G), and lung cancer cell line A-549, but none of them was active at 20 μg/mL concentration...
August 2017: Natural Products and Bioprospecting
Shai-Ping Hu, Wei-Wu Song, Si-Meng Zhao, Ning-Hua Tan
Two new cyclic nonapeptides, named clausenlanins A (1) and B (2), were isolated from the roots and rhizomes of Clausena lansium. Their structures were elucidated as cyclo-(Gly(1)-L-Leu(2)-L-Ile(3)-L-Leu(4)-L-Leu(5)-L-Leu(6)-L-Leu(7)-L-Leu(8)-L-Leu(9)) (1) and cyclo-(Gly(1)-L-Leu(2)-L-Val(3)-L-Leu(4)-L-Leu(5)-L-Leu(6)-L-Leu(7)-L-Leu(8)-L-Leu(9)) (2) respectively on the basis of extensive spectroscopic analysis, particularly 2D NMR spectra taken at the temperature of 338 or 303 K and MS.
August 2017: Natural Products and Bioprospecting
Euloge S Adjou, René G Dègnon, Edwige Dahouenon-Ahoussi, Mohamed M Soumanou, Dominique C K Sohounhloue
The aim of this study was to evaluate the efficacy of the essential oil extracted from fresh leaves of Pimenta racemosa in the improvement of fermented fish flour producing technology. Essential oil of Pimenta racemosa was extracted by hydrodistillation and its chemical composition was determined by GC and GC/MS. Different types of fermented fish flours from Lesser African Threadfin (Galeoides decadactylus) were produced by the modification of the traditional processing technology and the introduction of a step of essential oil adjunction during the process...
August 2017: Natural Products and Bioprospecting
Pei-Feng Zhu, Zhi Dai, Bei Wang, Xin Wei, Hao-Fei Yu, Zi-Ru Yan, Xu-Dong Zhao, Ya-Ping Liu, Xiao-Dong Luo
Four new phenolic amides, 4-O-methylgrossamide (1), (E)-2-(4,5-dihydroxy-2-{3-[(4-hydroxyphenethyl)amino]-3-oxopropyl}-phenyl)-3-(4-hydroxy-3-methoxyphenyl)-N-(4-hydroxyphenethyl)acryl-amide (2), (Z)-lyciumamide C (3), (Z)-thoreliamide B (4), together with thirteen known phenolic amides were identified from the stem of Lycium barbarum. The structures of the new compounds were determined by spectroscopic methods. All compounds were evaluated for their anti-cancer activities against human glioma stem cell lines...
June 6, 2017: Natural Products and Bioprospecting
Yinglan Pu, Hui Liu, Yeheng Zhou, Jiale Peng, Yaping Li, Penghua Li, Yingying Li, Xingyong Liu, Li Zhang
Coagulation Factor Xa (FXa) is the crucial enzyme at the convergent point of the intrinsic and extrinsic coagulation pathways. The inhibition of FXa is an effective approach against thrombotic diseases. In the present study, a specific strategy is reported to discover 10 novel FXa inhibitors based on ligand-based (pharmacophore) virtual screening and molecular docking analysis from a dataset of specs(containing 220000 molecules). The binding modes analysis provide insights into the contribution of particular structural moieties of the compounds towards their activity against FXa, and 10 novel structural compounds were discovered as potent candidate molecules...
June 2017: Natural Products and Bioprospecting
Li Peng, Yanting Lu, Yuhui Xu, Jing Hu, Fang Wang, Yumei Zhang, Wenyong Xiong
Obesity is crucially involved in many metabolic diseases, such as type 2 diabetes, cardiovascular disease and cancer. Regulating the number or size of adipocytes has been suggested to be a potential treatment for obesity. In this study, we investigated the effect of pyrocincholic acid 3β-O-β-D-quinovopyranosyl-28-O-β-D-glucopyranoside (PAQG), a 27-nor-oleanolic acid saponin extracted from Metadina trichotoma, on adipogenesis and lipid metabolism in 3T3-L1 adipocytes. The 3T3-L1 pre-adipocytes were incubated with vehicle or PAQG for 6 days in differentiation process...
June 2017: Natural Products and Bioprospecting
Michel Feussi Tala, Jianchun Qin, Joseph T Ndongo, Hartmut Laatsch
In the (1)H NMR-guided fractionation of extracts from the edible mushroom Lactarius deliciosus, two new azulene-type sesquiterpenoids, 7-isopropenyl-4-methyl-azulene-1-carboxylic acid (1) and 15-hydroxy-3,6-dihydrolactarazulene (2), together with seven known compounds were characterized. Their structures were determined on basis of spectroscopic evidence, as well as by comparing with literature data. Amongst the known metabolites, the (13)C NMR assignment of 15-hydroxy-6,7-dihydrolactarazulene (3) is reported here for the first time...
June 2017: Natural Products and Bioprospecting
Ting Wu, Zhiqiang Pan, Chengfeng Xia
A highly efficient and direct approach was developed to construct the structurally diverse spirooxindole skeleton, which is an important basic motif in natural products. Both the 3,3'-pyrrolidonyl spirooxindoles and spiroindolin-2-one δ-lactones were smoothly obtained by the intramolecular Dieckmann cyclization of oxindoles in excellent yield under mild conditions.
June 2017: Natural Products and Bioprospecting
Miao Liu, Zheng-Xi Hu, Yuan-Qing Luo, Min Zhou, Wei-Guang Wang, Xiao-Nian Li, Xue Du, Jian-Xin Pu, Han-Dong Sun
Schisanpropinoic acid (1), a new bergamotane sesquiterpenoid, and schisanpropinin (2), a new tetrahydrofuran lignan with a rare epoxyethane unit, were identified from the stems and leaves of Schisandra propinqua var. propinqua. Their structures were determined based on comprehensive spectroscopic and mass spectrometric analysis. The absolute configuration of 1 was determined by X-ray analysis. Compounds 1 and 2 were tested for their cytotoxic activity against five human tumor cell lines.
June 2017: Natural Products and Bioprospecting
Ya-Mei Li, Bing Xiang, Xiao-Zheng Li, Yong-Ming Yan, Yong-Xian Cheng
Two new diterpenoids, neoorthosiphonones B and C (1 and 2), and one known diterpenoid, were isolated from the aerial parts of Clerodendranthus spicatus. Their structures including absolute configurations were determined by comprehensive spectroscopic analyses and X-ray crystallographic methods. No compound was found to inhibit fibronectin production at the concentration of 20 μM.
June 2017: Natural Products and Bioprospecting
Kennedy D Nyongbela, Fidele Ntie-Kang, Thomas R Hoye, Simon M N Efange
The antiparasitic activity and preliminary in vitro and in silico drug metabolism and pharmacokinetic (DMPK) assessment of six isomeric sesquiterpenes (1-6), isolated from the Cameroonian spice Scleria striatinux De Wild (Cyperaceae) is reported. The study was prompted by the observation that two of the compounds (1 and 2) exhibited varying levels of antiparasitic activity on Plasmodium falciparum, Trypanosoma brucei rhodesiense, Trypanosoma cruzi and Leishmania donovani. The in silico method employed a total of 46 descriptors, calculated using Schrödinger QikProp software...
June 2017: Natural Products and Bioprospecting
Xiu-Juan Yin, Chang-An Geng, Xing-Long Chen, Chang-Li Sun, Tong-Hua Yang, Tian-Ze Li, Jun Zhou, Xue-Mei Zhang, Ji-Jun Chen
Sixteen tropinone derivatives were prepared, and their antitumor activities against five human cancer cells (HL-60, A-549, SMMC-7721, MCF-7 and SW480) were evaluated with MTS [3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxy methoxyphenyl)-2-(4-sulfopheny)-2H-tetrazolium] assay. Most of the derivatives exhibited better activities compared with tropinone at the concentration of 40 μM. Particularly, derivative 6 showed significant activities with IC50 values of 3.39, 13.59, 6.65, 13.09 and 12.38 μM respectively against HL-60, A-549, SMMC-7721, MCF-7 and SW480 cells, which suggested more potent activities than that of cis-dichlorodiamineplatinum (DDP)...
April 2017: Natural Products and Bioprospecting
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