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Marie Netopilova, Marketa Houdkova, Johana Rondevaldova, Vladimir Kmet, Ladislav Kokoska
Carvacrol and thymol, both plant-derived volatile compounds, have extensively been studied individually as well as in combination with other agents for their antimicrobial activity in liquid phase. However, in contrast to well-established assays for testing of antimicrobial combinatory effects in liquid media, there are no standardized methods for evaluation of interactions between volatile compounds in vapour phase. The objective of this study was to verify new broth volatilization chequerboard method by testing the combination of carvacrol and thymol and to determine in vitro inhibitory effect of these compounds in liquid and vapour phase against twelve Staphylococcus aureus strains...
July 5, 2018: Fitoterapia
Bao Yang, Hui Li, Qingfeng Ruan, Yi Tong, Zhongqiu Liu, Shenxin Xuan, Jing Jin, Zhongxiang Zhao
Triterpenoids, the major bioactive ingredients of Ilicis Rotundae Cortex, contributes a significant cardiovascular protection activity. Although many studies about the total saponin have been reported, the absorption triterpenoids and pharmacokinetic behaviors were unclear. Thus, the present study aims to comprehensive elucidate the absorption triterpenoids and their pharmacokinetics in rats after oral administration the crude extract using UPLC/Q-TOF-MS/MS. A total of forty-two triterpenoids were successfully characterized from the rat plasma, and thirty-two of them were validated by the reference substances, while the others were tentatively identified based on the mass spectral fragmental patterns...
July 5, 2018: Fitoterapia
Megil J McNeil, Roy B R Porter, Lois Rainford, Oliver Dunbar, Sheena Francis, Nicola Laurieri, Rupika Delgoda
Cleome rutidosperma DC, commonly known in Jamaica as 'consumption-weed' is a plant traditionally used in folklore for treating tuberculosis and other infectious and chronic ailments. We evaluate for the first time the chemical composition and biological activities of the essential oil components of the complete aerial parts of this plant. The essential oil obtained by steam distillation (0.02%) was analyzed by a combination of gas chromatography-flame ionization detector (GC-FID), gas chromatography-mass spectroscopy (GC-MS) and retention index (RI)...
July 5, 2018: Fitoterapia
Meigeng Hu, Yihang Li, Zhaocui Sun, Xiaowei Huo, Nailiang Zhu, Zhonghao Sun, Yangyang Liu, Haifeng Wu, Xudong Xu, Guoxu Ma, Guang Li
Nine new polyoxypregnane glycosides, obcordatas A-I (1-9), were isolated from Aspidopterys obcordata Hemsl vines. Their structures were elucidated by extensive spectroscopic methods. Separated compounds were evaluated for antitumor activities against the human cancer cell lines AGS, SW480, HuH-7 and MCF-7, and compounds 1-6 and 9 showed selective cytotoxicity against HuH-7 cells with IC50 values of 8.7, 10.2, 7.5, 12.1, 16.5, 14.3, and 17.4 μM, respectively. Flow cytometry experiments showed that the effects of compound 1 on the cell cycle were attributable to cell cycle arrest at G1/S phase...
July 4, 2018: Fitoterapia
Ya-Qian Ma, Meng-Han Liu, Kun Jiang, Lan Guo, Shi-Jin Qu, Yi-Qun Wan, Chang-Heng Tan
The fruits of Swietenia macrophylla (skyfruits) are commercially used as healthcare products to improve blood circulation. An investigation of active ingredients of skyfruits led to the isolation of four new limonoids, swietemacrolides A-D (1-4), together with ten known limonoids (5-14) and one proto-limonoid (15). Their structures were elucidated on the basis of MS and NMR data analysis. Swietemacrolide C (3) at the concentration of 10 μM showed significant protective effect on H2 O2 -induced apoptosis in human umbilical vascular endothelial cells (HUVECs), while swieteliacate D (5) displayed moderate anti-apoptotic activity...
July 4, 2018: Fitoterapia
Hongxin Liu, Haibo Tan, Kai Chen, Yuchan Chen, Saini Li, Haohua Li, Weimin Zhang
One new cerapicane cerrenin A (1), and two new isohirsutane sesquiterpenoids cerrenins B and C (2 and 3), were isolated from the broth extract of Cerrena sp. A593. Cerrenin A featured a rare cage-like bicyclo[3.2.1]octane skeleton, and cerrenin B represent the rearranged triquinane-type sesquiterpenoid. Their structures were extensively elucidated by NMR spectroscopic analysis with the absolute configuration determined by X-ray crystallography and ECD calculations. The anti-cancer activity for all the compounds were evaluated, and their plausible biosynthetic relationships involving fascinating carbon skeleton rearrangements were also suggested...
July 4, 2018: Fitoterapia
Fu-Ying Qin, Yong-Ming Yan, Zheng-Chao Tu, Yong-Xian Cheng
(+)- and (-)-Spirocochlealactones A-C (1-3), three pairs of new spiro meroterpenoidal dimeric enantiomers together with one known compound ganodilactone (4), were isolated from the fruiting bodies of Ganoderma cochlear. Their structures including absolute configurations were assigned by using spectroscopic methods and ECD calculations. All the isolated compounds were tested for their COX-2 inhibitory and cytotoxic activities toward human cancer lines (A549, K562, and Huh-7). The results show that all the compounds could inhibit COX-2 with IC50 values in the range of 1...
June 30, 2018: Fitoterapia
Lei Fang, Xiu-Qing Song, Tian-Tian He, Kong-Kai Zhu, Jin-Hai Yu, Jin-Tong Song, Jie Zhou, Hua Zhang
Two polyketides, stemonones A (1) and B (2) with new skeletons, were isolated from the roots of Stemona tuberosa. Their absolute structures were fully characterized by comprehensive spectroscopic analyses and comparison of experimental electronic circular dichroism (ECD) spectra with calculated ones. The plausible biosynthetic pathways for 1 and 2 were also proposed. Anti-inflammatory assay confirmed that the two compounds showed moderate inhibitory effects on β-glucuronidase release in rat polymorphonuclear leukocytes (PMNs) induced by platelet-activating factor...
June 28, 2018: Fitoterapia
Fangyou Chen, Chuangjun Li, Jie Ma, Lin Ni, Jiwu Huang, Li Li, Mingbao Lin, Qi Hou, Dongming Zhang
Three new diterpenoids (1-3) and three new esterifying lignans (4-6) were isolated from the leaves of Tripterygium wilfordii. The structures of these compounds were elucidated on the basis of spectroscopic techniques (UV, IR, NMR, HRESIMS, and ECD method). At 10 μmol/L, compounds 4-6 showed moderate inhibitory effects on nitric oxide production in LPS-induced macrophages with inhibitory rate >80%.
June 27, 2018: Fitoterapia
Mahmoud Aghaei, Mustafa Ghanadian, Seyed Ebrahim Sajjadi, Roshana Saghafian, Mohmmad Keyvanloo Shahrestanaki
Pimpinella haussknechtii is an annual native plant grows in west of Iran. Phytochemical study of the fruits of P. haussknechtii led to the isolation of a novel irregular sesquiterpene lactone with a new skeletone and oxidation pattern named: pimpinelol. The structure of the isolated compound was elucidated by extensive spectroscopic methods. Cytotoxic activity of Pimpinelol was evaluated using standard MTT assay against breast cancer cells. Induced endoplasmic reticulum stress and related gene expressions were evaluated with fluorescence microscopy analysis and real time PCR, respectively...
June 26, 2018: Fitoterapia
Gregorio Peron, Stefano Dall'Acqua, Stefania Sut
An UPLC-HR-MS metabolomics approach was used to study the effects of a 49-days oral supplementation with Polygonum cuspidatum extract in healthy rats. Multivariate analysis allowed to observe significant differences in the excretion of several markers between treated animals and control group. Among the others, the amounts of N-methyl-2-pyridone-5-carboxamide (2PY) and phenylacetylglycine (PAG) were reduced in the treated group compared to control. These compounds have been previously considered as markers of aging...
June 26, 2018: Fitoterapia
Yan Zhang, Lu Zhao, Shun-Wang Huang, Wei Wang, Shao-Jiang Song
Seven undescribed triterpene saponins, named kakisaponin I-VII (1-7), together with nine known ones (8-16) were isolated from the leaves of Diospyros kaki Thunb. by various chromatographic methods. Compounds 1-5 were novel 18, 19-secoursane triterpenoids, which were an uncommon type of triterpenoids. Their structures were elucidated by different spectroscopic methods, combining HRESIMS, 1D and 2D NMR. All isolated compounds were evaluated for their protective effects on H2 O2 -induced damage in human dopaminergic neuroblastoma cells (SH-SY5Y)...
June 26, 2018: Fitoterapia
Takashi Kikuchi, Kazutaka Kitaura, Ayaka Katsumoto, Jie Zhang, Takeshi Yamada, Reiko Tanaka
Three bisabolane-type sesquiterpenes (1-3) were isolated from the fruiting bodies of king trumpet mushrooms (Pleurotus eryngii), together with a known compound (4). All isolated compounds were evaluated for their inhibitory effects on nitric oxide (NO) production. Among these, 2 exhibited a moderate inhibitory effect on NO production with an IC50 of 90.9 μM.
June 26, 2018: Fitoterapia
Pan Luo, Zhi-Yong Yin, Zhe-Jun Sun, Hao Chen, Chan-Juan Li, Hui-Hao Zhou, Qiong Gu, Jun Xu
Three new cembrane-type diterpenoids, deheiculatins M-O (1-3), together with five known analogues (4-8), were isolated from the twigs of Macaranga pustulata King ex Hook. The structures of new compounds 1-3 were elucidated by extensive spectroscopic analyses, modified Mosher's method, and the experimental and calculated electronic circular dichroism (ECD) experiments. All the isolates were evaluated for their cytotoxicity on three human cancer cell lines (CNE1, CNE2, and HCT 116), and all of them showed weak cytotoxicity (IC50  > 20 μM)...
June 23, 2018: Fitoterapia
Shaimaa Fayez, Doris Feineis, Virima Mudogo, Ean-Jeong Seo, Thomas Efferth, Gerhard Bringmann
The Congolese liana Ancistrocladus likoko (Ancistrocladaceae) produces naphthylisoquinoline alkaloids that are, chemotaxonomically remarkable, all based on the same coupling type, with the biaryl axis located between C-5 and C-8'. About 20 alkaloids, belonging to the subclass of 5,8'-linked naphthylisoquinolines, have so far been discovered in this plant species. Here, we report on the isolation and structure elucidation of six further such 5,8'-coupled monomeric alkaloids, named ancistrolikokines I (9), C3 (10), F2 (11), J (12), J2 (13), and J3 (14)...
June 21, 2018: Fitoterapia
Wen Li, Jiaxin Pi, Ying Zhang, Xutong Ma, Bing Zhang, Shuya Wang, Dongli Qi, Nan Li, Pan Guo, Zhidong Liu
Baicalein (BE) is a flavonoid compound derived from the roots of Scutellaria baicalensis. It has widely been used as anti-oxidant, anti-virus, anti-bacteria, anti-inflammatory and anti-allergic therapies. Due to its poor water solubility (16.82 μg/ml), the therapeutic effectiveness and oral bioavailability of Baicalein are highly limited. The purpose of this study was to investigate the possibility of baicalein-theophylline (BE-TH) cocrystals to achieve the simultaneous enhancement in dissolution and oral bioavailability of BE...
June 21, 2018: Fitoterapia
Sheng-Yi Long, Yan Song, Qing-Jie Zhao, Dan Chen
A chemical investigation on the 80% EtOH extract of the aerial parts of Kopsia fruticosa led to five new indole alkaloids, kopsifolines G-K (1-5), and one known alkaloid, kopsifoline A (6). Structural elucidation of all the compounds were performed by spectral methods such as 1D and 2D (1 H-1 H COSY, HMQC, and HMBC) NMR spectroscopy, in addition to high resolution mass spectrometry. The isolated components were evaluated in vitro for cytotoxic activities against seven tumor cell lines, antimicrobial activities against two Gram-positive bacteria and five Gram-negative bacteria, and antifungal activities against five pathogens...
June 20, 2018: Fitoterapia
Jie-Li Lv, Lai-Bin Zhang, Li-Min Guo
Four new dimeric phthalides, angesinenolides C-F (1-4), along with three known ones, were isolated from the roots of Angelica sinensis. Their structures were determined by means of HRMS and NMR experiments. The structures of compounds 1 and 3 were confirmed using X-ray crystallographic data. All isolated compounds were tested for activities on the inhibition of COX-2 enzyme in vitro. Compounds 1-6 exhibited inhibitory activity against COX-2 with IC50 values ranging from 29.32 ± 0.07 to 137.91 ± 0...
June 20, 2018: Fitoterapia
Stefania Vergura, Ernesto Santoro, Marco Masi, Antonio Evidente, Patrizia Scafato, Stefano Superchi, Giuseppe Mazzeo, Giovanna Longhi, Sergio Abbate
Jonquailine, a new alkaloid recently isolated from Narcissus jonquilla quail, an Amaryllidacea species cultivated for its fragrance flowers in Europe and USA, shows very significant anti-proliferative activity against several malignant cancer cell types. Although it was reported that this activity is related to the functionalities and to its stereochemistry at C-8 of B ring, the absolute configuration at this stereocenter was not known. Density functional theory (DFT) calculations of chiroptical properties, namely electronic circular dichroism (ECD), vibrational circular dichroism (VCD), and optical rotatory dispersion (ORD) are employed here to complete assignment of absolute configuration of jonquailine, and then, by extension, to its analogues pretazettine and 8-O-methylpretazettine...
June 18, 2018: Fitoterapia
Yasuhiro Kamada, Hibiki Yakabu, Toshio Ichiba, Ayumi Tamanaha, Maria Shimoji, Megumi Kato, Chie Norimoto, Risa Yamasiro, Ikuko Miyagi, Akikazu Sakudo, Yasuharu Tanaka
Inhibition of poly(ADP-ribose) polymerase 1 (PARP1) is one of the most promising strategies for cancer chemotherapy, and a number of inhibitors possessing nicotinamide-like structures are being developed. To discover new types of PARP1 inhibitors, we screened a large number of substances of plant origin and isolated two inhibitory substances from the leaves of Syzygium samarangense (Blume) Merrill & L.M. Perry. The inhibitory substances were identified as vescalagin and its epimer castalagin by analyses using nuclear magnetic resonance and mass spectrometry...
June 18, 2018: Fitoterapia
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