bluuebunny/crossref_metadata_2025 huggingface dataset:
Bufadienolides from the Venom of Bufo Bufo gargarizans and Their Enzyme Inhibition Activities and Brine Shrimp Lethality
Authors: Xiao Jian , Zhao Xiang , Zhong Wan-Tong , Jiao Fu-Rong , Wang Xiao-Ling , Ma Lin , Duan Dong-Zhu , Yang De-Suo , Tang Shao-Qi
Published: March 2019

A new bufadienolide named dyscinobufotalin (1), along with twenty known bufadienolides (2–21) were isolated from the venom of Bufo bufo gargarizans. Their structures were elucidated by spectroscopic analysis. The absolute configuration of the new natural product 2 was determined by X-ray single crystal diffraction and the complete NMR data for 3 was delivered for the first time. Both compounds 4 and 8 showed comparable α-glucosidase inhibitory activity (IC50 values of 0.25 and 0.26 μM, respectively) to the positive control acarbose (IC50 value of 0.42 μM), and 5 displayed potent inhibitory activity on acetylcholinesterase with an IC50 value of 0.12 μM. Moreover, 5, 8 and 13 presented moderate toxicity against brine shrimp.
Mechanochemo-enzymatic Synthesis of Aromatic Aldehyde Oxime Esters
Authors: Arthur-Santiago Margarita A. , Oliart-Ros Rosa María , Sánchez-Otero María G. , Valerio-Alfaro Gerardo
Published: March 2019

The synthesis of aromatic aldehyde oxime esters (considered fragrances, antifungal and antimicrobial compounds) was achieved by two reactions which combine the advantage of green chemistry and biocatalysis. In the first step, the mechanochemical oxime synthesis by means of grindstone milling of six solid aromatic aldehydes and hydroxylamine hydrochloride in the presence of FlorisilR, as the best support, yielded the aromatic aldehyde oximes 1–6 with high purity and good yields. In the second step the lipase catalyzed acetylation reaction at 40°C for three days of those oximes with vinyl and isopropenyl acetates as acyl donor substrates and ethyl acetate as the solvent, yielded the aromatic aldehyde oxime esters. With Candida antarctica lipase (Novozyme 435), the conversions of oximes 1–6 into their esters were ≥ 99% according to the 1H NMR results and it was the best biocatalyst compared with others such as Candida rugosa (CRL), porcine pancreas lipase and the recombinant lipase LipMatCCR11 from the thermophilic strain Geobacillus thermoleovorans CCR11 cloned and expressed in Escherichia coli BL21 (DE3), all of which showed lower yields.
Chaetolactone, A Skeletally New Cyclopentenone from Chaetomium sp. C521
Authors: Han Wen-Bo , Li He , Zhou Hui-Yi , Meng Jia , Gao Jin-Ming , Tian Jun-Mian , Zhang An-Ling
Published: March 2019

Chaetolactone, a new polyketide with an unprecedented carbon skeleton, was constructed by Chaetomium sp. C521. Its structure was characterized by a combination of detailed spectroscopic analysis and ECD method, which facilitated the establishment of the absolute configuration for chaetolactone. The new compound was tested for anti-phytopathogenic activity against Botrytis cinerea, Alternaria solani, Gibberella saubinettii, and Magnaporthe oryzae, but exhibited negligible inhibition at a concentration of 20 μM.
Zedoary Turmeric Oil Induces Senescence and Apoptosis in Human Colon Cancer HCT116 Cells
Authors: Su Meng-Qi , Zhou Yi-Ran , Li Cheng-Qin , Wang Zhou , Wang Yue-Liang , Shen Bai-Yong , Dou Jie
Published: March 2019

Zedoary turmeric oil (ZTO) is a volatile oil that is extracted from the dry rhizome of Curcuma zedoaria with a variety of biological activities, including anti-tumor activity. However, there is a lack of knowledge about the effect and mechanism of ZTO in human colon cancer cells. The aim of this study was to examine the potential efficacy of ZTO against human colon cancer cells (HCT116) and to uncover the molecular mechanisms of its anti-tumor effects. The anti-proliferative activity of ZTO was determined by the MTT assay, cell counts and colony formation assay. Senescent cells were detected using SA-β-Gal staining, while apoptosis and the CD44+ subpopulation were evaluated by flow cytometry. The expression levels of senescence- and apoptosis-related proteins were examined using western blotting. The results showed that treatment with ZTO significantly inhibited the growth of HCT116 cells and caused senescence and apoptosis in a dose- and time-dependent manner. Western blotting revealed that ZTO significantly increased the expression of senescence- and apoptosis-related proteins p16, p21, and p53 and the phosphorylation of ERK. Moreover, ZTO treatment reduced the cancer stem-like CD44 positive cell population. These findings suggest that ZTO inhibits human colon cancer cells by inducing senescence and apoptosis.
Synthesis and Cytotoxic Evaluation of Artemisinin Derivatives Containing an Aminopropanol Group
Authors: Giang Le Nhat Thuy , Tien Doan Duy , Anh Dang Thi Tuyet , Dung Nguyen Tien , Thuong Ngo Hanh , Tan Luc Quang , Thanh Nguyen Ha , Anh Le Thi Tu , Van Tuyen Nguyen , Van Kiem Phan
Published: March 2019

Series of novel artemisinin derivatives were designed and synthesized in which the amino propanol group was bonded to the artemisinin nucleus through C-C linkage. Ten new compounds were thus successfully prepared and evaluated as cytotoxic agents, revealing an interesting anticancer activity in KB and HepG2 cancer cell lines.
Cytotoxic Evaluation of Compounds Isolated from the Aerial Parts of Hedyotis pilulifera and Methanol Extract of Inonotus obliquus
Authors: Nguyen Hoai Thi , Ho Duc Viet , Nguyen Phu Dinh Quynh , Vo Hung Quoc , Do Thao Thi , Raal Ain
Published: March 2019

The aim of this study was to evaluate the inhibitory activity of compounds isolated from the aerial parts of Hedyotis pilulifera (Pit.) T.N. Ninh toward selected cancer cell lines. The isolated compounds were identified by analyzing their nuclear magnetic resonance spectral data and physical properties, and comparison of these with reported data. The sulforhodamine B assay was used for the cytotoxic evaluation of isolates. Among twenty-one compounds isolated from H. pilulifera, compounds 2, 3, and 4 showed moderate inhibitory effect on MCF-7 with IC50 values of 63.5, 59.4, and 52.7 μg/mL, respectively, while the other compounds exhibited no effect (IC50 values > 100 μg/mL). Further investigation using HT29, LU-1, HL-60, KB, Hep G2, and SK-Mel2 cancer cell lines showed the moderate cytotoxic activity of compound 3 (IC50 values ranging from 51.7 to 78.3 μg/mL) to all cells, while compound 4 showed selective effect only against HL-60 cells (IC50 61.5 μg/mL). This is the first report of cytotoxic activity of pomolic acid 3β-acetate (3) toward all tested cancer cell lines, and also the first report of cytotoxicity of rotungenic acid (4) against LU-1, HL-60, KB, Hep G2, and SK-Mel2 cancer cell lines. The methanol extract of chaga mushroom { Inonotus obliquus (Ach. ex Pers.) Pilát} exhibited the strongest cytotoxic effects against HL-60 and LU-1 (32.2 and 38.0 μg/mL, respectively), and modest cytotoxic effects against SW480 (41.3 μg/mL), HepG2 (51.3 μg/mL), KB (57.0 μg/mL), and LNCaP (57.7 μg/mL). We conclude that compounds 3 and 4 from H. pilulifera may be useful in further investigation for anticancer agent discovery and chaga could be used as a natural anticancer remedy against promyelocytic leukemia and lung adenocarcinoma.
New Sesquiterpene Pyridine Alkaloids from Hippocratea excelsa
Authors: Furukawa Megumi , Furukawa Masakatsu , Makino Mitsuko , Uchiyama Taketo , Fujimoto Yasuo , Matsuzaki Keiichi
Published: March 2019

In total, three sesquiterpene pyridine alkaloids, including two new compounds and a triterpene, were isolated from the n-hexane extract of the stem barks of Hippocratea excelsa. The structures of these compounds were elucidated by spectroscopic methods. Pristimerin, a naturally occurring triterpenoid, exhibited cytotoxicity against L1210 cells.
Flavonoids from Milletia leucantha and Their Cytotoxicity
Authors: Sriphana Uraiwan , Yenjai Chavi , Tungnoi Siriporn , Srirapa Jongjai , Junsongduang Auemporn
Published: March 2019

Two known chalcones (1–2), five known flavonol derivatives (3 and 5–8) and one flavone (4) were isolated for the first time from fruits of Millettia leucantha Kurz. In addition, 5 was found for the first time from this genus. Their structures were elucidated on the basis of IR, MS, 1D and 2D NMR techniques. Chalcone 1 exhibited moderate cytotoxicity against the MCF-7 cell line with an IC50 value of 50.93 μM, whereas this compound showed inactive cytotoxicity against Vero cells. Compound 2 exhibited cytotoxicity against the KB, NCI-H187 and Vero cell lines with IC50 values of 63.64, 114.44 and 28.44 μM, respectively. Compound 8 only showed cytotoxic activity against the KB cell line with an IC50 value of 110.23 μM.
Terpenes and n-Alkanes in Needles of Pinus cembra
Authors: Nikolić Biljana , Todosijević Marina , Ratknić Mihajlo , Đorđević Iris , Stanković Jovana , Cvetković Mirjana , Marin Petar D. , Tešević Vele
Published: March 2019

Simultaneous hydrodistillation and extraction of Pinus cembra needles from Slovakia was done (via Likens Nickerson apparatus) for the first time. In essential oil extracts 55 compounds were identified, comprising 99.6% of the extract. The most abundant were monoterpene hydrocarbons (71.0%). In the terpene profile α-pinene, limonene/β-phellandrene, germacrene D, β-pinene, and δ-cadinene dominated (53.2%, 11.4%, 9.4%, 4.6%, and 4.3%, respectively). Seven new compounds for P. cembra, such as methyl daniellate (0.5%), 1,8 cineole (0.2%) and trans-cadina-1(6),4-diene (0.2%), etc. were found. In needle cuticular wax of P. cembra the amount of nonacosan-10-ol was 75.8%. n-Alkanes ranged from C20 to C35 with the most dominant C31, C 29 and C33 (33.4%, 16.9%, and 9.6%, resp.). Differences in terpene profiles between Slovakian and Greece from one side and Romanian and Polish cembran pines on the other side could be the consequence of its disjuncted areal in Carpathian Mountains caused by glaciation and survival of species in different ecological niches. Obtained differences in n-alkane profiles among our and literature results could be the consequence of different age of trees.
Evaluation of Antipneumonic Effect of Philippine Essential Oils Using Broth Microdilution Volatilization Method and Their Lung Fibroblasts Toxicity
Authors: Houdkova Marketa , Doskocil Ivo , Urbanova Klara , Tulin Ea Kristine Clarisse B. , Rondevaldova Johana , Tulin Anabella B. , Kudera Tomas , Tulin Edgardo E. , Zeleny Vaclav , Kokoska Ladislav
Published: March 2019

Essential oils isolated from six Philippine plant species, namely Alpinia brevilabris C. Presl, Alpinia cumingii K. Schum., Alpinia elegans (C. Presl) K. Schum., Callicarpa micrantha Vidal, Cinnamomum mercadoi S. Vidal, and Piper quinqueangulatum Miq. were assessed for their in vitro growth-inhibitory effect against pneumonia causing bacteria ( Haemophilus influenzae, Streptococcus pneumoniae, and Staphylococcus aureus) using the broth microdilution volatilization method. Additionally, a modified thiazolyl blue tetrazolium bromide assay was performed for evaluation of their cytotoxic activity to human lung cells. All essential oils exhibited some antibacterial efficacy in liquid phase; however, only A. cumingii oil was active in the vapour as well. Both A. cumingii and A. elegans oils showed the most effective antibacterial potential against H. influenzae in liquid medium with the minimum inhibitory concentration of 256 μg/mL. Using dual-column/dual-detector system GC/MS analysis, hedycaryol, β-pinene, caryophyllene epoxide, aristolochene, borneol, and linalool were identified as the major components of A. brevilabris, A. cumingii, A. elegans, C. micrantha, C. mercadoi, and P. quinqueangulatum leaves oils, respectively.
Craft Beers made with Addition of Umbrian Legumes: Healthy and Nutritional Characterization
Authors: Luneia Stefano , Zannoli Riccardo , Farchioni Marco , Sensidoni Michele , Luneia Roberto
Published: March 2019

Legumes are very rich in phytochemicals and in particular isoflavones. In this work we have developed techniques to get the brewing craft beers made with the addition of Umbrian legumes (chickling and lentils), to verify if the healthy and nutritional characteristic of these product change. The results obtained show that probably during the processes of cooking and fermentation a transfer of the biologically active substances from the “special ingredients” to the finished beer takes place. From healthy and nutritional characterization of the beers important results emerged: an interesting mineral profile and a large content of molecules with antioxidant activity like phenolic compounds (350–630 mg/L). It should also be noted that within the group of phenolic compounds present in these beers were also found interesting amount of isoflavones in particular genistin and daidzin, which in addition to being powerful antioxidants have other beneficial effects and therefore can act in the prevention of cancer, inflammatory, cardiovascular, postmenopausal, cognitive, and immune diseases.
Dithiosulfinates and Sulfoxides with Antifungal Activity from Bulbs of Allium sativum L. var. Voghiera
Authors: de Falco Bruna , Bonanomi Giuliano , Lanzotti Virginia
Published: March 2019

A bioassay guided phytochemical analysis of the bulbs of Allium sativum L. var. Voghiera, typical of Voghiera, Ferrara (Italy), allowed the isolation of six new sulfur compounds with dithiosulfinates and sulfoxides functionalities. Structure elucidation of the isolated compounds was carried out by spectroscopic analyses, including NMR spectroscopy and MS spectrometry. Compounds showed significant antimicrobial activity towards two fungal species, the air-borne pathogen Botrytis cinerea and the beneficial fungus Trichoderma harzianum.
Essential Oil of Achillea ligustica (Asteraceae) as an Antifungal Agent against Phytopathogenic Fungi
Authors: Giamperi Laura , Bucchini Anahi Elena Ada , Ricci Donata , Papa Fabrizio , Maggi Filippo
Published: March 2019

The essential oil from the inflorescences of Ligurian yarrow ( Achillea ligustica All., Asteraceae) naturalized in Central Italy was investigated in order to evaluate the antifungal activity against five phytopathogenic fungi. The composition of the essential oil characterized by GC-FID and GC-MS, revealed linalool (24.8%), viridiflorol (9.6%), β-pinene (6.4%), 1,8-cineole (5.8%) and terpinen-4-ol (5.3%) as the major constituents. The antifungal activity was evaluated by the in vitro disc agar diffusion test and Agar vapor assay on 5 microbial strains. The essential oil showed a good antifungal activity against all fungal strains, being a valid candidate in the fight against plant pathogens that harm many traditional crops. The possible incorporation of this essential oil into antifungal preparations with a low environmental impact is hypothesized.
New Diterpene Glycosides from Stevia rebaudiana Bertoni: Rebaudioside VIII and Rebaudioside IXd
Authors: Ma Gil , Bechman Allison , Bunders Cynthia , Devkota Krishna P. , Charan Romila D. , Ramirez Catherine , Snyder Tara M. , Priedemann Christopher , Prakash Indra
Published: March 2019

With our interest of new diterpene glycosides with better taste profile than Rebaudioside M, we isolated and characterized two steviol glycosides with three additional glucose attached at the C-13 of Rebaudioside M or Rebaudioside D from an extract of Stevia rebaudiana Bertoni. Here we report the complete structure elucidations of diterpene glycosides on the basis of NMR experiments (1H, 13C, COSY, HSQC-DEPT, HMBC, 1D TOCSY, NOESY) and mass spectral data. Steviol glycosides that possess eight or nine glucose units are rarely reported in literature and could have an impact on the natural sweetener catalog.
A New Limonoid from Chisocheton paniculatus Fruit Collected in Vietnam and Its NO Production Inhibitory Activity
Authors: Hoai Nguyen Thi , Duc Ho Viet , Raal Ain , Morita Hiroyuki
Published: March 2019

A new limonoid, 6α,7α-diacetoxy-3-oxo-24,25,26,27-tetranorapotirucalla-1,14,20(22)-trien-21,23-lactam (1), was isolated from the fruits of Chsocheton paniculatus Hiern collected in Vietnam, together with two known 5α,8α-epidioxysterols, (22 E,24 R)-5α,8α-epidioxy-24-methyl-cholesta-6,22-dien-3β-ol (2) and (22 E,24 R)-5α,8α-epidioxy-24-methyl-cholesta-6,9(11),22-trien-3β-ol (3) Their structures were elucidated by spectroscopic analyses, including D- and 2D-NMR and HRESIMS, and comparisons with the reported data in the literature. Compounds 1–3 exhibited the NO production inhibitory activities against the LPS stimulated BV2 cells with 69.0 ± 2.7 %, 69.5 ± 2.2 %, and 70.6 ± 1.6 %, at concentration of 20.0 μM, respectively.
Structure – Anti-influenza Type a Activity Relationship among a Series of Nitrogen Lupane Triterpenoids
Authors: Smirnova Irina E. , Kazakova Oxana B.
Published: March 2019

Fifty-one derivatives of lupeol, betulin, betulonic and acanthochlamic acids modified at C3, C20 and C28 of the lupane core including four new ones (37, 49 –51) and forty-seven previously synthesized derivatives (1 – 36, 36 – 48) were screened for their in vitro anti-influenza type A (H1N1, H3N2 and H5N1) activity at the NIAID. The selectivity index (SI) against Flu A for tested triterpenoids ranged from > 20 to 0. Betulonic acid 2-aminopyridinylamide was a leader being active against H1N1, H3N2 and H5N1 with SI > 20, 1.8 and 5.3, respectively. The betulonic acid methoxy- and nitro-substituted benzalhydrazides showed selectivity only against H5N1, while lupeol and 3-oximino-betulonic acid benzalhydrazides were active against three types of Flu A. A-seco-aminoderivatives were more effective than the initial acanthochlamic acid against H1N1, but practically inactive against H3N2, with bis- N-methylpiperazinylamide as a leader in this series. Triterpenoids with a long-chain substituent at C17 containing amide or hydrazide bonds with aromatic or heterocyclic fragments exert positive influence on the activity.
Biological Activities of Extracts from Different Parts of two Cultivars of Prunus persica ‘Akatsuki’ and ‘Fastigiata’
Authors: Nakagawa Toshinori , Allam Ahmed E. , Ohnuki Koichiro , Shimizu Kuniyoshi
Published: March 2019

We investigated the antioxidant, anti-lipase and anti-dementia activities of peach ( Prunus persica (L.) Batsch) fruit and its by-products. The ethanol extracts of branch showed relatively high activity in all biological activities. Then, the extract was fractionated, and eight compounds were isolated from the ethyl acetate fraction. Results showed 4,2’,4'-trihydroxy-6'-methoxychalcone 4'- O-β-D-glucopyranoside (5) and quercetin 3- O-β-D-glucopyranoside (7) as newly identified compounds in P. persica. From the biological investigation, it was considered that quercetin 3- O-β-D-glucopyranoside (7) was the main active compound of antioxidant activity. The main active compound of anti-lipase activity in these was oleanolic acid (1). In addition, (+)-4'- O-methylcatechin (4), 4,2’,4'-trihydroxy-6'-methoxychalcone 4'- O-β-D-glucopyranoside (5) and ferulic acid (6) were the main active compounds of anti-dementia activity with acetylcholinesterase inhibitory assay. The results obtained suggested that these active compounds from peach branches of P. persica could be exploited as natural antioxidants, anti-lipase and anti-dementia materials in the future.
Antibiotic Mycotoxins from an Endophytic Fusarium acuminatum Isolated from the Medicinal Plant Geum macrophyllum
Authors: Clark Trevor N. , Carroll Madison , Ellsworth Katelyn , Guerrette Roxann , Robichaud Gilles A. , Johnson John A. , Gray Christopher A.
Published: March 2019

An extract of the endophytic fungus Fusarium acuminatum (TC2-084) isolated from the Canadian medicinal plant Geum macrophyllum exhibited significant antimycobacterial activity against Mycobacterium tuberculosis H37Ra when fermented in both malt extract and potato dextrose broths. However, significant differences observed in the NMR spectra of the respective extracts led us to further investigate both. Bioassay guided fractionation revealed that lateropyrone was solely responsible for the bioactivity observed when TC2-084 was fermented in malt extract broth, while the antimycobacterial activity of the extract derived from the isolate fermented in potato dextrose broth was augmented by the presence of enniatins B, B1, and B4 in addition to lateropyrone.
Free Radical Scavenging Activity of Synthetic and Naturally Occurring Polyhydroxy-, Aminohydroxynaphthazarins and Related Compounds
Authors: Polonik Nikita S. , Sabutskii Yuri E. , Polonik Sergey G.
Published: March 2019

Fifty natural and synthetic hydroxy-, aminohydroxynaphthazarins and related quinones were tested for their antiradical activities using 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonate) (ABTS) scavenging assay. The main features of structure-antiradical activity relationship of amino- and hydroxyquinones were determined for the first time. It was found that naphthazarins (5,8-dihydroxy-1,4-naphthoquinones) are much more active against ABTS-radical than related 1,4-naphthoquinones and 5-hydroxy-1,4-naphthoquinones. Natural aminonaphthazarins (spinamine E, echinamine A) and polyhydroxylated naphthazarins (spinazarin, echinochrome, spinochrome D and E) revealed high antiradical properties. In most cases, the presence of long chained O-alkoxy substituent in benzenoid part of naphthazarin core enhanced their antiradical activity.
Lanostane-type Triterpenoids from Ganoderma lucidum and G. multipileum Fruiting Bodies
Authors: Binh Pham Thanh , Thao Nguyen Phuong , Luyen Nguyen Thi , Trang Duong Thu , Binh Phung Thi Xuan , Nguyen Nguyen Phuong Dai , Hiep Nguyen Tuan , Dang Nguyen Hai , Tri Tran Manh , Dat Nguyen Tien
Published: March 2019

Sixteen lanostane-type triterpeneoids were isolated from the fruiting bodies of wild Ganoderma lucidum and G. multipileum. The new structures 3 S,24 S,25,26-tetrahydroxy-5α-lanost-8-en-11-one (1) and ganodermanondiol 24,25-acetonide (10) were elucidated by means of spectroscopic data and Mosher's experiments. Lanosta-7,9(11)-dien-3β-ol (9) strongly inhibited α-glucosidase with the IC50 values of 198.8 μM in compared with acarbose (IC50 712.4 μM).
Two New Steroidal Alkaloid Saponins from the Whole Plants of Solanum nigrum
Authors: Tai Bui Huu , Van Doan Vu , Yen Pham Hai , Nhiem Nguyen Xuan , Cuc Nguyen Thi , Trang Do Thi , Hang Dan Thi Thuy , Dung Duong Thi , Yen Duong Thi Hai , Quang Tran Hong , Dang Nguyen Hai , Mai Nguyen Thi , Van Minh Chau , Van Kiem Phan
Published: March 2019

Two new steroidal alkaloid saponins, solanigrosides Q and R (1 and 2), together with four known compounds khasianine (3), solamargine (4), solasonine (5), and soladulcoside A (6) were isolated from the whole plants of Solanum nigrum. The structures of new compounds (1 and 2) were determined by interpretation of HR-ESI-MS, 1D and 2D NMR spectra, and chemical transformation. Compound 4 exhibited potent cytotoxic activity against MDA-MB-231, A549, Hep3B, PC3 human cancer cell lines with IC50 values of 1.86 ± 0.45, 2.24 ± 0.15, 0.78 ± 0.11, 5.13 ± 1.34 μM, respectively.
Phytochemical Analysis and Antimicrobial Efficacy of Macleaya cordata against Extensively Drug-Resistant Staphylococcus aureus
Authors: Khin Manead , Jones Alan M. , Cech Nadja B. , Caesar Lindsay K.
Published: March 2019

The antibiotic resistant threat is continuing to grow, due in part to the overuse of antibiotics in livestock feed. Many nations in Europe have banned the use of antibiotics in feed, leading to higher rates of infection in livestock animals and reduced productivity for the food market. Increasingly, researchers are looking into the efficacy of phytopreparations to replace antibiotics in feed, allowing for increased animal health without the development of resistance. Macleaya cordata, or Chinese plume poppy, shows promise as a food additive. To evaluate the antimicrobial efficacy of this plant, we tested in vitro activity of M. cordata extract, as well as pure compounds sanguinarine and chelerythrine against wild-type, methicillin-resistant, and multiply-resistant strains of Staphylococcus aureus (SA1199, AH1263, and IA116, respectively). Combination tests to evaluate synergy, additivity, and antagonism within the extract were also completed for the first time. Sanguinarine and chelerythrine showed complete growth inhibition of all strains of S. aureus at concentrations ranging from 3–10 μg/mL, and were equal in activity or were more potent than the reference compound chloramphenicol. Combination studies of pure sanguinarine and chelerythrine with M. cordata extract revealed additivity or indifference of mixture components with these compounds. Because sanguinarine and chelerythrine represent the major active constituents of M. cordata, the pooled amounts of these two compounds may be useful for establishing potency for quality control purposes. This is the first report of activity of chelerythrine and sanguinarine against methicillin-resistant S. aureus AH1263 and multiply-resistant S. aureus IA116, and illustrates the promise of M. cordata extract as an alternative to antibiotics in feed additives.
A Review of Common Medicinal Plants in Chin State, Myanmar
Authors: Thu Zaw Min , Aye Mya Mu , Aung Hnin Thanda , Sein Myint Myint , Vidari Giovanni
Published: March 2019

Promising sources of novel bioactive compounds include plants growing in several third-world countries where the local flora is still largely uninvestigated. A paradigmatic example is represented by medicinal plants growing in Myanmar, especially in Chin State, in northwestern Myanmar. This is one of the least developed areas of the country where the people still use natural remedies derived from a rich biodiversity. This review mainly covers the investigations done on phytochemical constituents and biological activities of 20 medicinal plants, namely Alangium chinense, Anemone obtusiloba, Anneslea fragrans, Antidesma bunius, Croton oblongifolius, Embelia tsjeriam-cottam, Ficus heterophylla, Gaultheria fragrantissima, Hydnocarpus kurzii, Leea macrophylla, Leucas cephalotes, Millingtonia hortensis, Myrica nagi, Olax scandens, Pimpinella heyneana, Pterospermum semisagittatum, Ruellia tuberosa, Smilax zeylanica, Stemona burkillii, and Tadehagi triquetrum, that have long been used in the Chin State for curing various diseases. These plants have been selected on the basis of their medicinal uses not only in Myanmar but also in the related Ayurvedic healing system. Moreover, besides their medicinal importance, most of them grow in the Chin State more abundantly than in other regions of Myanmar. Although the efficacy of some of these plants have been verified scientifically, the chemical constituents and biological activities of most of them still need to be investigated to confirm the claimed therapeutic effects.
A New Antibacterial Polyketide from the Endophytic Fungi Aspergillus fumigatiaffinis
Authors: Ola Antonius R. B. , Tawo Bibiana D , Belli Henderiana L. L , Proksch Peter , Tommy Dhana , Hakim Euis Holisotan
Published: March 2019

A new antibacterial polyketide (-) palitantin was isolated from Aspergillus fumigatiaffnis, an endophytic fungi from a medicinal plant Tribulus terestris. The structure of the antibacterial metabolite was established using 1D and 2D NMR together with mass spectroscopy. (-) Palitantin was found to inhibit the growth of Enterococcus faecalis UW 2689 and Streptococcus pneumoniae with MIC value of 64μg/mL.
Antiviral Activities of Curcuma Genus against Hepatitis C Virus
Authors: Wahyuni Tutik Sri , permatasari Adita Ayu , Widiandani Tri , Fuad Achmad , Widyawaruyanti Aty , Aoki-Utsubo Chie , Hotta Hak
Published: March 2019

Hepatitis C virus (HCV) infection is one of the major public health problems in the world. Even though the new agents are shown to increase the sustained virology response, however, there are still many people who cannot access the therapy due to the high cost. Moreover, the emergence of resistance and side effects presented the necessity to develop alternative treatment agents for HCV infection. Plants of the genus of curcuma are popular among traditional medicines in the world, including Indonesia. They have been used for many herb remedies and reported to possess many biological activities. Several plants from the curcuma genus were known as treatment agents in liver disease and jaundice. Our current study determines antiviral activities of Curcuma domestica, Curcuma xanthorrhiza, and Curcuma heyneana against HCV and further examines the mechanism of actions. Antiviral activity was performed by in vitro culture cells using Huh 7.5it cells and treated with the mixture of extract and virus JFH1. The effects of extracts in HCV life cycle were determined by mode of action analysis to examine the action of substances in the entry or post entry steps. The results revealed that ethanol extract of C. domestica, C. xanthorrhiza, and C. heyneana showed strong anti-HCV activities with IC50 values of 1.68 ± 0.05, 4.93 ± 0.42 and 5.49 ± 0.59 μg/mL, respectively without any cytotoxicity effect. Mode of action analysis demonstrated that of C. domestica and C. heyneana exhibit HCV in the entry step, while C. xanthorrhiza inhibit in the entry and post entry steps of HCV life cycle. Docking analysis to predict the interaction of curcumin, the main compound of curcuma genus, revealed a strong interaction between curcumin and 4GAG receptor, a protein involved in the entry step of HCV infection. Moreover, it was also reported to possess good interaction with 4EAW, an HCV NS5B, which plays an important role in HCV replication. These results suggested that C. domestica, C. xanthorrhiza, and C. Heyneana possessed strong inhibition against hepatitis C virus, therefore they may be good candidates for anti-HCV agents.
Psolusosides C1, C2, and D1, Novel Triterpene Hexaosides from the Sea CucumberPsolus fabricii (Psolidae, Dendrochirotida)
Authors: Silchenko Alexandra S. , Avilov Sergey A. , Kalinovsky Anatoly I. , Kalinin Vladimir I. , Andrijaschenko Pelageya V. , Dmitrenok Pavel S.
Published: March 2019

Three new triterpene glycosides, psolusosides C1 (1), C2 (2) and D1 (3) have been isolated from the sea cucumber Psolus fabricii collected in the Sea of Okhotsk in the shallow waters of Onekotan Island (Kurile Islands). Five known glycosides: cladolosides B, M1, P2, isolated earlier from the sea cucumbers of genus Cladolabes and holotoxin A1 with 27- nor-25-oxo-holotoxin A1, isolated earlier from Apostichopus japonicus have also been found. The glycoside structures were elucidated by 2D NMR spectroscopy and HR mass-spectrometry. Compounds 1–3 possess hexasaccharide carbohydrate chains, identical for 1 and 2 and different in the third monosaccharide residue for 3. All the glycosides comprise holostane type aglycones with a 9(11)-double bond and a 16-keto-group and differ from each other in the side chains structures.
Flavonoids from three Wild Glycine Species in Japan and Taiwan
Authors: Iwashina Tsukasa , Kokubugata Goro , Nakamura Koh , Mizuno Takayuki , Devkota Hari Prasad , Yokota Masatsugu , Murai Yoshinori , Saito Yukiko
Published: March 2019

Fourteen flavonols, four flavones and six isoflavones were isolated from the aerial parts of two Japanese Glycine species, G. tabacina and G. koidzumii, and the leaves of Taiwanese G. max subsp. formosana. Of their flavonoids, twelve flavonols were identified as kaempferol 3- O-sophoroside (1), 3- O-rutinoside (2), 3- O-robinobioside (3) and 3- O-rhamnosyl-(1→4)-[rhamnosyl-(1→6)-galactoside] (4), quercetin 3- O-gentiobioside (5), 3- O-glucoside (6), 3- O-galactoside (7), 3- O-rutinoside (8), 3- O-robinobioside (9) and 3- O-rhamnosyl-(1→4)-[rhamnosyl-(1→6)-galactoside] (10), and isorhamnetin 3- O-rutinoside (11) and 3- O-robinobioside (12). Other two flavonols were characterized as isorhamnetin 3- O-rhamnosylrhamnosylglucoside (13) and 3- O-rhamnosylrhamnosylgalactoside (14). Four flavones and six isoflavones were estimated as schaftoside (15), apigenin 6,8-di- C-arabinoside (16), luteolin 7- O-glucoside (17) and chrysoeriol 7- O-glucoside (18), and daidzein 7- O-glucoside (19), 4'- O-glucoside (20) and 7- O-xylosylglucoside (21), genistein 7- O-glucoside (22) and 4'- O-glucoside (23), and 3'- O-methylorobol 7- O-glucoside (24). Although flavonoid composition of G. tabacina and G. koidzumii was similar to each other, that of G. max subsp. formosana was different with those of two Japanese Glycine species described above. Flavonoids of their Glycine species were reported for the first time except for those of G. tabacina.
Synergistic Anticancer Effects of Curcumin and Hinokitiol on Gefitinib Resistant Non-Small Cell Lung Cancer Cells
Authors: Lee Tae-Bok , Seo Eun-Ju , Lee Ji-Yun , Jun Jin Hyun
Published: March 2019

This study evaluated the synergistic effect of curcumin (diferuloylmethane) and hinokitiol (β-thujaplicin), natural product derived phytochemicals, on gefitinib (Iressa) resistant non-small cell lung cancer (NSCLC) cells. Gefitinib, a tyrosine kinase inhibitor targeting epidermal growth factor receptor (EGFR), is widely used for lung cancer treatment. However, gefitinib resistance is easily acquired by NSCLC and followed by the development of progressive disease. Curcumin and hinokitiol are well-known bioactive compounds demonstrating anti-inflammation, anti-bacteria and anticancer effects. However, the effects of co-treatment of curcumin and hinokitiol on cancer cells have not been reported. Here, we postulated, for the first time, the possibility of combination therapy with curcumin and hinokitiol for treatment of gefitinib resistant NSCLC via increment of apoptosis and lysosomal enlargement.
Screening of Biological Activities of Ligustrum lucidum Berries: A Comparative Approach
Authors: Delgado Teresa , Paula Vanessa B. , Campos Maria Graça , Farinha Nelson , Caeiro André , Estevinho Leticia M. , Anjos Ofélia
Published: March 2019

Ligustrum lucidum Aiton including its berries have been used in Chinese Traditional Medicine for around 2000 years. Scientific studies developed on the last decades provided evidence on some biological properties of these products, mostly from particular geographic origins. In the present study, L. lucidium berries harvested in two regions of Portugal were considered. Extracts obtained with 100% ethanol, with 50% ethanol/water (v/v) and in boiled water were prepared and several parameters were assessed: antioxidant activity (using two methodologies), antimicrobial activity and phenolic profile. Results suggest that the different biological activities varied according to the region where samples were collected but also with the extraction methodology. Superior antioxidant potential was observed in water extracts, according to both assays, while for the remaining activities the ethanol 50% extracts had the highest activity. In these regions, the L. lucidum berries showed promising biological activities and may be interesting sources of compounds for the development of new drugs for diseases where oxidant reactive species and enzymatic disruption are believed to play a role as well as adjuvants for current antibiotic therapy.
Eduscho Coffee Extract Effectively Inhibits the Formation of Amyloid-like Fibrils by Trypsin in Aqueous Ethanol
Authors: Kasi Phanindra Babu , Borics Attila , Molnár Kinga , László Lajos , Kotormán Márta
Published: March 2019

In this work we used an in vitro trypsin aggregation model to show that certain commercial coffee extracts can inhibit protein aggregation. Aggregation experiments were performed using several spectroscopic methods and a dye binding assay, such as turbidity, Congo red (CR) and electronic circular dichroism (ECD), that was further supported by transmission electron microscopy (TEM). A correlation was found between the anti-aggregation properties and the total phenolic content of the coffee extracts. The results revealed that the greatest effect was exerted by the Eduscho coffee extract. It was found that the inhibitory effect of this extract was concentration dependent. Using size exclusion chromatography, we demonstrated that the inhibitory effect of the Eduscho coffee extract on the formation of amyloid-like fibrils was due to its capacity to stabilize the oligomeric form of the protein.
Ameliorating Effects of Jixueteng in a Mouse Model of Porphyromonas gingivalis-Induced Periodontitis: Analysis Based on Gingival Microcirculatory System
Authors: Suzuki Mitsuo , Toyama Toshizo , Watanabe Kiyoko , Sasaki Haruka , Sugiyama Shuta , Yoshino Fumihiko , Yoshida Ayaka , Takahashi Shun-suke , Wada-Takahashi Satoko , Matsuo Masato , Todoki Kazuo , Hamada Nobushiro
Published: March 2019

Jixueteng, the dried stem of Spatholobus suberectus Dunn (Leguminosae), is a traditional Chinese herbal medicine that promotes blood circulation and can be used to treat blood stasis. In this study, we aimed to investigate the potential of Jixueteng as a preventive and therapeutic drug for periodontitis. We investigated the inhibitory effects of Jixueteng on Porphyromonas gingivalis ( P. gingivalis)-induced gingival circulatory disturbances in mice. Seventy-two male C57BL/6N mice (4-week-old) were randomly divided into the following four groups of 12 mice each. Group 1 served as the P. gingivalis noninfected control (control group). Group 2 was administered Jixueteng extract in drinking water to P. gingivalis noninfected control mice. Group 3 was infected orally with P. gingivalis; and group 4 was administered Jixueteng extract in drinking water and then infected with P. gingivalis. To evaluate the effect of Jixueteng on gingival microcirculation systems, we examined gingival blood flow (GBF) in oral microcirculation in vivo in a mouse model of periodontitis. Gingival reactive hyperemia (GRH) was determined using laser Doppler flowmetry. GRH was elicited by the release of occlusive gingival compression by the laser Doppler probe (diameter 1.0 mm) for 1 min. GRH was estimated by basal blood flow, maximum response (Peak), the time taken for the maximum response to fall to one half (T1/2) and increased total amount of blood flow (Mass). Furthermore, to determine the effect of an oral application of P. gingivalis and/or Jixueteng on GBF and gingival microvessel ultrastructure, morphological analysis of gingival microvessels was performed by using a vascular resin cast model. Administration of Jixueteng to P. gingivalis-infected animals significantly reduced GRH, especially T1/2 and Mass, compared to that in P. gingivalis-infected animals. Alternatively, in the morphological analysis, reduction of the gingival capillary network which resulted from P. gingivalis-infection was improved by Jixueteng administration. Since Jixueteng ameliorates P. gingivalis infection-induced gingival circulatory disturbance, it may be useful in the treatment of P. gingivalis-induced periodontitis.
Reading border-crossing Japanese comics/anime in China: Cultural consumption, fandom, and imagination
Authors: Fung Anthony , Pun Boris , Mori Yoshitaka
Published: March 2019

Differences in cultural consumption are well recognized as potential forces for changing the cultural identity of consumers. Based on this logic, our hypothesis posits that Chinese readers, who comprise the largest fan community of Japanese comics/anime, are culturally influenced by this foreign product. To examine this hypothesis, we question whether the global values and worldviews of freedom, peaceful coexistence, justice, companionship, and humanity, which are embedded in Japanese comics/anime, influence the values and ideology of Chinese readers. This study was aimed to examine the reading strategies and patterns in legally or illegally imported border-crossing cultural products to assess the potential cultural impact of their consumption on young Chinese readers. Their differences in passion could affect their devotion, their identity, and their worldviews. In this study, focus groups in Japan and China, in-depth interviews, and textual analyses of Japanese comic/amine were conducted to examine the reading, fandom, and cultural impact of comics/anime on Chinese urban youth. The significance of this study is that it explores new models of active reading that affect the long-term shape of and changes in the values and identities of Chinese youth. The findings of this study shed light on whether imported cultural products could transform, change, and dilute the ideologies of the state and nationalism, thereby allowing new and alternative imaginings of values and global citizenship, which are emerging areas of interest in global communication studies.
User-generated news: Netizen journalism in China in the age of short video
Authors: Xiang Yu
Published: March 2019

As media technology advances, and with increasingly rapid development, there has been an unprecedented growth in the number of new media platforms emerging in China—and throughout the world—that are changing the procedures of how news is assembled and disseminated by effectively and efficiently adopting user-generated content that has injected new blood into the very nature of journalism. While essentially this is encouraging the productive use of social media platforms, it is also having an impact on users, transforming vast numbers into what are now recognized as “netizen journalists.” This leads us to inquire just how the journalistic outputs of short video platforms of such media outfits like Pear Video and Kwai are framed and also to explore how the roles of the “ordinary” users of such platforms are now defined by their participation in the actual production of news and information. This research aims to contribute to the many discussions on the above questions based on the journalistic study on three different news platforms: Xinhua News Agency’ as adopted and adapted content from Kwai, Kwai Insight, and Pear Video.
Cloaking as a Community: Re-imagining the White Coat Ceremony With a Medical School Learning Community
Authors: Tamai Robert , Koyawala Neel , Dietrick Barbara , Pain Debanjan , Shochet Robert
Published: March 2019

The Johns Hopkins School of Medicine’s Learning Community–White Coat Ceremony (LC-WCC) is held each spring as a learning community (LC) event. Learning communities (LCs) connect people to learn and work across boundaries to achieve a shared goal. The LC-WCC invites first-year students to collaborate with school leaders, define the class professional values, and innovate with community members. Class-elected student leaders recruit peers to join committees to plan and lead several aspects of the ceremony, including a class-nominated speaker, a personal statements presentation, a patient inclusion presentation, a class-authored statement of values, and artistic performances. Student cloaking is performed by LC advisors in their LC small groups. A 2015 post-LC-WCC survey asking students to compare experiences of a traditional Stethoscope Ceremony (SC) with the LC-WCC found that the latter significantly increased students’ sense of accomplishment (38% vs 68%, P < .001), sense of connection to the school (59% vs 82%, P < .001), to classmates (71% vs 93%, P < .001), and to the event (42% vs 76%, P < .001). Cloaking as a community is an effective way for a medical school LC to instill a greater sense of community and student leadership in this milestone celebration of humanistic values in medicine.
PD-L1 gene alterations identify a subset of diffuse large B-cell lymphoma harboring a T-cell–inflamed phenotype
Authors: Godfrey James , Tumuluru Sravya , Bao Riyue , Leukam Michael , Venkataraman Girish , Phillip John , Fitzpatrick Carrie , McElherne James , MacNabb Brendan W. , Orlowski Robert , Smith Sonali M. , Kline Justin
Published: March 2019

Programmed death-ligand 1 (PD-L1) expression on malignant cells is a dominant immune escape mechanism across a variety of human cancers. A unique genetic mechanism underlying PD-L1 upregulation has been uncovered in classical Hodgkin lymphoma (cHL), in which copy gains of the chromosomal region (9p24.1) containing the programmed death-1 (PD-1) ligands PD-L1 and PD-L2 are recurrently observed. While chromosome 9p24.1 copy-number alterations are ubiquitous in cHL, they also occur in diffuse large B-cell lymphoma (DLBCL), albeit with a lower incidence. Here, fluorescence in situ hybridization was used to identify DLBCLs harboring PD-L1 gene alterations, thereby enabling a characterization of the immunogenomic landscape of these lymphomas. Among 105 DLBCL cases analyzed, PD-L1 alterations were identified in 27%. PD-L1 alterations were highly enriched among non–germinal center DLBCLs and exhibited robust PD-L1 protein expression. These lymphomas were heavily infiltrated by clonally restricted T cells and frequently downregulated human leukocyte antigen expression. RNA sequencing of PD-L1–altered DLBCLs revealed upregulation of genes involved in negative T-cell regulation and NF-κB pathway activation, while whole-exome sequencing identified frequent mutations in genes involved in antigen presentation and T-cell costimulation. Many of these findings were validated in a large external data set. Interestingly, DLBCL patients with PD-L1 alterations had inferior progression-free survival following front-line chemoimmunotherapy; however, in the relapsed/refractory setting, PD-L1 alterations were associated with response to anti-PD-1 therapy. Collectively, our results indicate that PD-L1 alterations identify a unique biological subset of DLBCL in which an endogenous antilymphoma immune response has been activated, and that is associated with responsiveness to PD-1 blockade therapy.
Cancer Control in Low- and Middle-Income Countries: Is It Time to Consider Screening?
Authors: Shah Shailja C. , Kayamba Violet , Peek Richard M. , Heimburger Douglas
Published: March 2019

The rising prevalence of noncommunicable diseases globally, with a strikingly disproportionate increase in prevalence and related mortality in low- and middle-income countries (LMICs), is a major threat to sustainable development. The epidemiologic trend of cancers in LMICs is of particular concern. Despite a lower incidence of cancer in LMICs compared with high-income countries, total cancer-related mortality is significantly higher in LMICs, especially in people younger than 65 years of age. The enormous economic impact of premature mortality and lost productive life years highlights the critical importance of galvanizing cancer prevention and management to achieve sustainable development. The rising burden of cancer in LMICs stresses an already weak health care and economic infrastructure and poses unique challenges. Although the WHO acknowledges that the effective management of cancer relies on early detection, accurate diagnosis, and access to appropriate multimodal therapy, the placement of priority on early detection cannot be assumed to be effective in LMICs, where limited downstream resources may be overwhelmed by the inevitable increases in number of diagnoses. This review discusses several factors and considerations that may compromise the success of cancer control programs in LMICs, particularly if the focus is only on early detection through screening and surveillance. It is intended to guide optimal implementation of cancer control programs by accentuating challenges common in LMICs and by emphasizing the importance of cancer prevention where relevant so that communities and stakeholders can work together to devise optimal means of combatting the growing burden of cancer.