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https://www.readbyqxmd.com/read/28813096/cytotoxicity-and-bacterial-membrane-destabilization-induced-by-annona-squamosa-l-extracts
#1
Nícolas C C Pinto, Jucélia B Silva, Laura M Menegati, Maria Clara M R Guedes, Lucas B Marques, Thiago P DA Silva, Rossana C N DE Melo, Elaine M DE Souza-Fagundes, Marcos J Salvador, Elita Scio, Rodrigo L Fabri
This study aimed to further investigate the cytotoxicity against tumor cell lines and several bacterial strains of Annona squamosa and its mode of action. Methanol extracts of A. squamosa leaves (ASL) and seeds (ASS) were used. ASL showed significant antibacterial activity against S. aureus, K. pneumoniae and E. faecalis with MIC values of 78, 78 and 39 µg/mL respectively. Moreover, ASL exhibited significant biofilm disruption, rapid time dependent kinetics of bacterial killing, increased membrane permeability and significantly reduced the cell numbers and viability...
August 14, 2017: Anais da Academia Brasileira de Ciências
https://www.readbyqxmd.com/read/28813032/diterpenoid-alkaloids-from-consolida-regalis-s-f-gray-subsp-paniculata-host-soo-var-paniculata
#2
Filiz Mericl, Ali H Mericli, Haridutt K Desai, Ayhan Ulubelen, S William Pelletier
Seven diterpenoid alkaloids : delcosine(1), delsoline(2), gigactonine(3), lycoctonine(4), takaosamine(5), atisine(6) and hetisinone(7) have been isolated from the aerial parts of Consolida regalis subsp. paniculata var. paniculata. The presence of compounds 1,2,5,6 and 7 in this plant has not been previously reported.
August 16, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28812364/catalytic-asymmetric-desymmetrization-of-cyclopentendiones-via-diels-alder-reaction-of-3-hydroxy-2-pyrones-construction-of-multifunctional-bridged-tricyclic-lactones
#3
Li-Min Shi, Wu-Wei Dong, Hai-Yan Tao, Xiu-Qin Dong, Chun-Jiang Wang
An unprecedented asymmetric Diels-Alder reaction of 3-hydroxy-2-pyrones with prochiral cyclopentene-1,3-diones via desymmetrization was efficiently realized with high stereoselective control with the aid of fine-tunable cinchona alkaloid derived bifunctional amine-thiourea catalysts bearing multiple hydrogen-bonding donors. This protocol provides an expedient access to the multifunctional-bridged tricyclic lactones featuring four contiguous stereogenic centers and one remote quaternary stereogenic center with a broad substrate scope...
August 16, 2017: Organic Letters
https://www.readbyqxmd.com/read/28812277/milonine-an-alkaloid-of-cissampelos-sympodialis-eichl-menispermaceae-inhibits-histamine-release-of-activated-mast-cells
#4
Adriano Francisco Alves, Giciane Carvalho Vieira, Francisco Allysson A F Gadelha, Luiz Henrique Agra Cavalcante-Silva, Marco Aurélio Martins, José Maria Barbosa-Filho, Marcia Regina Piuvezam
Milonine is an alkaloid of Cissampelos sympodialis Eichl. (Menispermaceae), a plant used in the northeast of Brazil to treat allergies such as asthma, rhinitis, and other conditions. Previously, several alkaloids were isolated from its roots and leaves with pharmacological properties in asthma and acute inflammation models. Therefore, the aim of this study was to evaluate the milonine effect on mast cells degranulation in vivo and in vitro. Swiss mice (n = 8) were used in models of paw edema induced by carrageenan, compound 48/80, or histamine...
August 15, 2017: Inflammation
https://www.readbyqxmd.com/read/28812026/evidence-of-immunosuppressive-and-th2-immune-polarizing-effects-of-antidiabetic-momordica-charantia-fruit-juice
#5
Rufine Fachinan, Adnette Fagninou, Magloire Pandoua Nekoua, Abdou Madjid Amoussa, Marius Adjagba, Latifou Lagnika, Anatole Lalèyè, Kabirou Moutairou, Akadiri Yessoufou
The mechanism of action of the antidiabetic capacity of Momordica charantia is still under investigation. Here, we assessed phytochemical compositions, antioxidant activity, and effects of total and filtered fruit and leafy stem juices of Momordica charantia on human T cell proliferation and differentiation through quantification of Th1/Th2 cytokines. In the absence of stimulation, total fruit and leafy stem juices induced significant T cell proliferation. Under PHA stimulation, both juices potentiated plant-induced T cell proliferation...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28811827/pharmacodynamics-and-medicinal-chemistry-of-an-external-chinese-herbal-formula-for-mammary-precancerous-lesions
#6
Ruixue Chen, Guijuan Zhang, Yi Ma, Fengjie Bie, Hongxia Fan, Min Ma
Ruyan Neixiao Cream (RYNXC) is a traditional Chinese herbal formula for treating mammary precancerous disease. This study was carried out to investigate in vivo anticancer effect of RYNXC and multiple constituents. 32 virginal Sprague-Dawley rats were randomly divided into blank control group (BC), mammary precancer models group (MODEL), tamoxifen group (TAM), and Ruyan Neixiao Cream group (RYNXC). TAM was intervened by tamoxifen; RYNXC was intervened by Ruyan Neixiao Cream. The chromatographic separation was performed by high performance liquid chromatography (HPLC) coupled with mass spectrometry (MS)...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/28811034/a-simple-microdroplet-chip-consisting-of-silica-nanochannel-assisted-electrode-and-paper-cover-for-highly-sensitive-electrochemiluminescent-detection-of-drugs-in-human-serum
#7
Yi Xiao, Linru Xu, Ping Li, Xiao-Chong Tang, Lian-Wen Qi
This paper describes a simple and miniaturized microdroplet chip (μchip) that is constructed with a silica nanochannel (SNC)-assisted electrode array and a hydrophobic paper cover (SNC&P-μchip). Vertically aligned SNCs with uniform pore size of 2-3 nm in diameter and negatively charged surface can significantly accelerate the mass transport of the positively charged tris(2,2'-bipyridyl) ruthenium (II), resulting in a remarkably enhanced electrochemiluminescence (ECL) signal. The SNC-assisted electrode array was coupled to a low cost paper cover to achieve simultaneous detection of six samples in 1 min...
August 29, 2017: Analytica Chimica Acta
https://www.readbyqxmd.com/read/28809491/a-total-synthesis-of-the-marine-alkaloid-discoipyrrole-d
#8
Yiwen Zhang, Martin G Banwell
A total synthesis of the diastereoisomeric pair of compounds, 4, assigned to the marine alkaloid discoipyrrole D is reported. A series of palladium-catalysed cross-coupling and other reactions was employed to assemble the relevant 1,2,3,4-tetra-substituted pyrrole (16) that was engaged in MoOPH-mediated oxidative cyclization then conjugate addition and redox processes to complete the synthesis. This work serves to confirm the structure (4) originally assigned to discoipyrrole D.
August 15, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28809439/in-silico-profiling-of-the-biological-activities-of-amaryllidaceae-alkaloids
#9
Eman Shawky
OBJECTIVES: The large number of publications about Amaryllidaceae alkaloids reflects the abundance and variety in biological activity of these alkaloids. An in-silico approach was implemented in this work to rationalize the individual alkaloids to molecular biological activity. METHODS: A database was generated containing 313 Amaryllidaceae alkaloids which were then subjected to in-silico-validated structure-based virtual screening using extra precision (XP) approach of Glide docking program...
August 15, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28809120/structural-revision-of-the-hancock-alkaloid-galipeine
#10
Stephen G Davies, Ai M Fletcher, Ian T T Houlsby, Paul M Roberts, James E Thomson
The 1H and 13C NMR data of synthetic samples of (S)-N(1)-methyl-2-[2'-(3″-hydroxy-4″-methoxyphenyl)ethyl]-1,2,3,4-tetrahydroquinoline, the originally proposed structure of the Hancock alkaloid (-)-galipeine, do not match those of the natural product. Herein, the preparation of the regioisomer (S)-N(1)-methyl-2-[2'-(3″-methoxy-4″-hydroxyphenyl)ethyl]-1,2,3,4-tetrahydroquinoline is reported, the 1H and 13C NMR data of which are in excellent agreement with those of (-)-galipeine. Comparison of specific rotation data enables assignment of the absolute (S)-configuration of the alkaloid and together, these data engender the structural revision of (-)-galipeine to (S)-N(1)-methyl-2-[2'-(3″-methoxy-4″-hydroxyphenyl)ethyl]-1,2,3,4-tetrahydroquinoline...
August 15, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28808798/genetic-engineering-approach-using-early-vinca-alkaloid-biosynthesis-genes-led-to-increased-tryptamine-and-terpenoid-indole-alkaloids-biosynthesis-in-differentiating-cultures-of-catharanthus-roseus
#11
Abhishek Sharma, Priyanka Verma, Archana Mathur, Ajay Kumar Mathur
Catharanthus roseus today occupies the central position in ongoing metabolic engineering efforts in medicinal plants. The entire multi-step biogenetic pathway of its very expensive anticancerous alkaloids vinblastine and vincristine is fairly very well dissected at biochemical and gene levels except the pathway steps leading to biosynthesis of monomeric alkaloid catharanthine and tabersonine. In order to enhance the plant-based productivity of these pharma molecules for the drug industry, cell and tissue cultures of C...
August 14, 2017: Protoplasma
https://www.readbyqxmd.com/read/28808390/immunomodulatory-cytotoxicity-and-antioxidant-activities-of-roots-of-ziziphus-mauritiana
#12
Samina Afzal, Murium Batool, Bashir Ahmad Ch, Ashfaq Ahmad, Muhammad Uzair, Khurram Afzal
AIMS: The study is conducted to evaluate the immunomodulatory, cytotoxicity, and antioxidant potential of Ziziphus mauritiana (Rhamnaceae). Phytochemical analysis of Z. mauritiana revealed the presence of alkaloids, anthraquinone glycoside, cardiac glycoside, saponin, tannin, and flavonoids. METHODOLOGY: The cytotoxicity of the plant Z. mauritiana was evaluated by brine shrimp lethality test. Antioxidant parameters such as superoxide dismutase (SOD), total antioxidant capacity (T-AOC), and malondialdehyde (MDA) levels were calculated in the plasma of rats after chronic administration of 400 mg/kg of Z...
July 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/28808045/fighting-tubulin-targeting-anticancer-drug-toxicity-and-resistance
#13
REVIEW
Roberta Visconti, Domenico Grieco
Tubulin-targeting drugs, like taxanes and vinca alkaloids, are among the most effective anticancer therapeutics used in the clinic today. Specifically, anti-microtubule cancer drugs (AMCDs) have proven to be effective in the treatment of castration-resistant prostate cancer and triple-negative breast cancer. AMCDs, however, have limiting toxicities that include neutropenia and neurotoxicity, and, in addition, tumor cells can become resistant to the drugs after long-term use. Co-targeting mitotic progression/slippage with inhibition of the protein kinases WEE1 and MYT1 that regulate CDK1 kinase activity may improve AMCD efficacy, reducing the acquisition of resistance by the tumor and side effects from the drug and/or its vehicle...
September 2017: Endocrine-related Cancer
https://www.readbyqxmd.com/read/28807851/toxic-pyrrolizidine-alkaloids-provide-a-warning-sign-to-overuse-of-the-ethnomedicine-arnebia-benthamii
#14
Latif Ahmad, He Yi, Jia-Chen Hao, Andrew Semotiuk, Quan-Ru Liu, Paras Mazari
ETHNOPHARMACOLOGICAL RELEVANCE: From early times man has used medicinal plants for the treatment of various ailments and basic health care needs. The use of herbal medicines has increased day by day and with this, so do reports of adverse events, poisoning, and suspected toxicity. Similarly, the indigenous communities of Neelum Valley in Azad Kashmir commonly use Arnebia benthamii (Wall. ex G.Don) I.M.Johnst. for medicinal purposes to treat various human aliments. Besides their medicinal uses, it also contains hepatotoxic pyrrolizidine alkaloids (PAs)...
August 11, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28807230/global-identification-of-chemical-constituents-and-rat-metabolites-of-si-miao-wan-by-liquid-chromatography-electrospray-ionization-quadrupole-time-of-flight-mass-spectrometry
#15
Jin-Jin Lu, Xue-Wen Hu, Ping Li, Jun Chen
Si-Miao-Wan (SMW), a tradiational Chinese medicinal formula consisting of Atractylodis Rhizoma, Phellodendri Chinensis Cortex, Coicis Semen, and Achyranthis Bidentatae Radix, has been used for the treatment of gout and gouty arthritis for many years. In the present study, a liquid chromatography quadrupole-time-of-flight mass spectrometry (LC-Q-TOF/MS) method was established to identify the multiple constituents of SMW and its metabolites in rat biological samples after oral administration. A total of 48 compounds in SMW, including 21 alkaloids, 12 organic acids, 2 terpenes, 3 lactones, 2 phytosterols, and 8 other compounds, were tentatively characterized with the diagnostic-ion filtering strategy...
July 2017: Chinese Journal of Natural Medicines
https://www.readbyqxmd.com/read/28807228/antibacterial-steroidal-alkaloids-from-holarrhena-antidysenteriaca
#16
Li-Na Zhou, Xiao-Lei Ge, Ting-Ting Dong, Hui-Yuan Gao, Bo-Hang Sun
Two new steroidal alkaloids, isoconkuressine and N-formylconessimine, together with 6 known steroidal alkaloids including conkuressine, conessine, isoconessimine, conimine, conarrhimine, and funtudienine, were isolated from the seeds of Holarrhena antidysenteriaca Wall.ex A.DC. Their intrinsic antibacterial activities and synergistic effects with penicillin and vancomycin were analyzed in methicillin sensitive staphylococcus aureus (MSSA) and methicillin resistant staphylococcus aureus (MRSA). Two of the steroidal alkaloids including one new compound (N-formylconessimine) showed potential antibacterial activity and possessed synergistic effects with penicillin and vancomycin, respectively...
July 2017: Chinese Journal of Natural Medicines
https://www.readbyqxmd.com/read/28807162/chinese-herbal-medicine-for-the-treatment-of-drug-addiction
#17
Weili Zhu, Yinan Zhang, Yingjie Huang, Lin Lu
This chapter summarizes recent developments in preclinical and clinical research on Chinese herbal medicines and their neurochemical mechanism of action for the treatment of drug addiction. We searched Chinese and English scientific literature and selected several kinds of Chinese herbal medicines that have beneficial effects on drug addiction. Ginseng (Renshen) may be clinically useful for the prevention of opioid abuse and dependence. Rhizoma Corydalis (Yanhusuo) may be used to prevent relapse to chronic drug dependence...
2017: International Review of Neurobiology
https://www.readbyqxmd.com/read/28806947/conessine-as-a-novel-inhibitor-of-multidrug-efflux-pump-systems-in-pseudomonas-aeruginosa
#18
Thanyaluck Siriyong, Potjanee Srimanote, Sasitorn Chusri, Boon-Ek Yingyongnarongkul, Channarong Suaisom, Varomyalin Tipmanee, Supayang Piyawan Voravuthikunchai
BACKGROUND: Holarrhena antidysenterica has been employed as an ethnobotanical plant for the treatment of dysentery, diarrhoea, fever, and bacterial infections. Biological activities of the principle compound, conessine including anti-diarrhoea and anti-plasmodial effects were documented. Our previous study reported potency of Holarrhena antidysenterica extract and conessine as resistance modifying agents against extensively drug-resistant Acinetobacter baumannii. This study aimed to investigate (i) whether conessine, a steroidal alkaloid compound, could act as a resistance modifying agent against multidrug-resistant Pseudomonas aeruginosa, and (ii) whether MexAB-OprM efflux pump involved in the mechanism...
August 14, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28806604/chemodiversity-of-tryptamine-derived-alkaloids-in-six-costa-rican-palicourea-species-rubiaceae-palicoureeae
#19
Andreas Berger, Elias Tanuhadi, Lothar Brecker, Johann Schinnerl, Karin Valant-Vetschera
We report 14 harmala and tryptamine-iridoid alkaloids with various tri-, tetra- and pentacyclic cores from leaves and stem bark of six species of the large and complex neotropical genus Palicourea. Among them is the previously undescribed compound deoxostrictosamide which is related to strictosamide, a key intermediate in camptothecin biosynthesis. In addition, we describe the occurrence of 1,2,3,4-tetrahydronorharman-1-one for the first time within Rubiaceae and ophiorine A and B, two alkaloids with an unusual core bearing a betaine function and a zwitterion as new for the genus...
August 11, 2017: Phytochemistry
https://www.readbyqxmd.com/read/28805975/antofine-suppresses-endotoxin-induced-inflammation-and-metabolic-disorder-via-amp-activated-protein-kinase
#20
Shao-Ting Chou, Fang Jung, Shih-Hsing Yang, Hwei-Ling Chou, Guey-Mei Jow, Jau-Chen Lin
The inhibition of activated macrophages has been used to develop anti-inflammatory agents for therapeutic intervention to human diseases that cause excessive inflammatory responses. Antofine, a phenanthroindolizidine alkaloid, has a potent anti-inflammatory effect. However, the molecular mechanisms of its anti-inflammatory activity have not yet been fully detailed. In this study, we comprehensively explored the anti-inflammatory effects of antofine on endotoxin-induced inflammation in macrophages using cDNA microarray analysis, thereby elucidating the potential mechanism by which antofine suppresses inflammation...
August 2017: Pharmacology Research & Perspectives
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