Antiproliferative Aporphine Alkaloids from Litsea glutinosa and Ethnopharmacological Relevance to Kuuku I’yu Traditional Medicine

2016 ◽  
Vol 69 (2) ◽  
pp. 145 ◽  
Author(s):  
Chi P. Ndi ◽  
Matthew J. Sykes ◽  
David J. Claudie ◽  
Ross A. McKinnon ◽  
Susan J. Semple ◽  
...  
Keyword(s):  
Topoisomerase Ii ◽  
Aboriginal People ◽  
Human Keratinocytes ◽  
Primary Human Keratinocytes ◽  
Methylenedioxy Group ◽  
In Silico Docking ◽  
History Of ◽  
Plausible Mechanism ◽  
Cape York ◽  
Litsea Glutinosa

Australian Aboriginal people have a long history of relying on plants for the treatment of various ailments and illnesses. Our ongoing collaborative research project initiated by Chuulangun Aboriginal Corporation (Cape York, Australia) has recently focussed on revealing whether Kuuku I’yu plant medicines possess anticancer-related activities and the chemistry responsible for this. Here, we present results from a study of the plant Litsea glutinosa, used traditionally for the treatment of gastrointestinal disorders. Four known aporphine alkaloids N-methylactinodaphnine (1), boldine (2), N-methyllaurotetanine (3), and isoboldine (4) were isolated by activity-guided fractionation and tested for cytotoxicity against HT29, SKMEL28, and primary human keratinocytes. Compound 1 was the most cytotoxic and this observation may be explained by the presence of a 1,2-methylenedioxy group. In silico docking revealed that a plausible mechanism for the observed cytotoxicity is the stabilization of a topoisomerase II (β) DNA–enzyme complex. The ethnopharmacological relevance of this study is discussed in the context of researching and using traditional knowledge in biomolecular discovery.

Towards gene therapy for haemophilia B using primary human keratinocytes

1993 ◽  
Vol 3 (2) ◽  
pp. 180-183 ◽  
Author(s):  
Ann J. Gerrard ◽  
David L. Hudson ◽  
George G. Brownlee ◽  
Fiona M. Watt
Keyword(s):  
Gene Therapy ◽  
Human Keratinocytes ◽  
Primary Human Keratinocytes ◽  
Haemophilia B

‘Japan Fight. Aboriginal People Fight. European People Fight’: Yolngu Stories from World War II

2008 ◽  
Vol 37 (S1) ◽  
pp. 65-72
Author(s):  
Noah Riseman
Keyword(s):  
World War Ii ◽  
Aboriginal People ◽  
Northern Territory ◽  
Oral Histories ◽  
World War ◽  
Prisoner Of War ◽  
War Effort ◽  
History Of ◽  
The Rich ◽  
Australian Soil

Abstract Did you know that a Bathurst Islander captured the first Japanese prisoner of war on Australian soil? Or that a crucifix saved the life of a crashed American pilot in the Gulf of Carpentaria? These are excerpts from the rich array of oral histories of Aboriginal participation in World War II. This paper presents “highlights” from Yolngu oral histories of World War II in Arnhem Land, Northern Territory. Using these stories, the paper begins to explore some of the following questions: Why did Yolngu participate in the war effort? How did Yolngu see their role in relation to white Australia? In what ways did Yolngu contribute to the security of Australia? How integral was Yolngu assistance to defence of Australia? Although the answers to these questions are not finite, this paper aims to survey some of the Yolngu history of World War II.

scholarly journals Synthesis, Bioactivity, Pharmacokinetic and Biomimetic Properties of Multi-Substituted Coumarin Derivatives

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5999
Author(s):  
Annita Katopodi ◽  
Evangelia Tsotsou ◽  
Triantafylia Iliou ◽  
Georgia-Eirini Deligiannidou ◽  
Eleni Pontiki ◽  
...  
Keyword(s):  
Cell Viability ◽  
Oral Absorption ◽  
Radical Scavenging ◽  
Human Keratinocytes ◽  
Docking Studies ◽  
Hydroxyl Group ◽  
Coumarin Derivatives ◽  
In Silico Docking ◽  
A375 Cells

A series of novel multi-substituted coumarin derivatives were synthesized, spectroscopically characterized, and evaluated for their antioxidant activity, soybean lipoxygenase (LOX) inhibitory ability, their influence on cell viability in immortalized human keratinocytes (HaCaT), and cytotoxicity in adenocarcinomic human alveolar basal epithelial cells (A549) and human melanoma (A375) cells, in vitro. Coumarin analogues 4a–4f, bearing a hydroxyl group at position 5 of the coumarin scaffold and halogen substituents at the 3-phenyl ring, were the most promising ABTS•+ scavengers. 6,8-Dibromo-3-(4-hydroxyphenyl)-4-methyl-chromen-2-one (4k) and 6-bromo-3-(4,5-diacetyloxyphenyl)-4-methyl-chromen-2-one (3m) exhibited significant lipid peroxidation inhibitory activity (IC50 36.9 and 37.1 μM). In the DCF-DA assay, the 4′-fluoro-substituted compound 3f (100%), and the 6-bromo substituted compounds 3i (80.9%) and 4i (100%) presented the highest activity. The 3′-fluoro-substituted coumarins 3e and 4e, along with 3-(4-acetyloxyphenyl)-6,8-dibromo-4-methyl-chromen-2-one (3k), were the most potent lipoxygenase (LOX) inhibitors (IC50 11.4, 4.1, and 8.7 μM, respectively) while displaying remarkable hydroxyl radical scavenging ability, 85.2%, 100%, and 92.9%, respectively. in silico docking studies of compounds 4e and 3k, revealed that they present allosteric interactions with the enzyme. The majority of the analogues (100 μΜ) did not affect the cell viability of HaCaT cells, though several compounds presented over 60% cytotoxicity in A549 or A375 cells. Finally, the human oral absorption (%HOA) and plasma protein binding (%PPB) properties of the synthesized coumarins were also estimated using biomimetic chromatography, and all compounds presented high %HOA (>99%) and %PPB (60–97%) values.

scholarly journals Contested homelands: Darwin’s ‘itinerant problem’

2005 ◽  
Vol 11 (1) ◽  
pp. 174-197 ◽  
Author(s):  
Steve Spencer
Keyword(s):  
Indigenous Population ◽  
Aboriginal People ◽  
Historical Context ◽  
Remote Communities ◽  
Cultural Genocide ◽  
Visiting Friends And Relatives ◽  
History Of ◽  
People First ◽  
Cultural Constructions ◽  
The City

Darwin has the largest Aboriginal population of any Australian city at nearly nine per cent, and the Northern Territory has nearly 28 per cent of the indigenous population. While the greater majority of the indigenous population in Darwin lives in circumstances not unlike their non-indigenous neighbors, a number are, out of necessity, more transient, moving between remote communities and the city, visiting friends and relatives who may be in hospital or prison, seeking work or escaping uneviable conditions in the interior. It is important to preface the present study with a word on social and historical context, as the representation of indigenous issues in 'the Territory' is founded upon historical and cultural constructions of Aboriginality. What underpins this long-running moral panic about homeless indiginous people? First, the history of Aboriginal people in Australia has been one of the disposession, cultural genocide and displacement. 

Expression profiling of vitamin D treated primary human keratinocytes

2007 ◽  
Vol 100 (3) ◽  
pp. 574-592 ◽  
Author(s):  
Pamela Renate Moll ◽  
Veronika Sander ◽  
Anna-Maria Frischauf ◽  
Klaus Richter
Keyword(s):  
Vitamin D ◽  
Expression Profiling ◽  
Human Keratinocytes ◽  
Primary Human Keratinocytes

scholarly journals HaCaT Cells as a Reliable In Vitro Differentiation Model to Dissect the Inflammatory/Repair Response of Human Keratinocytes

2017 ◽  
Vol 2017 ◽  
pp. 1-12 ◽  
Author(s):  
Irma Colombo ◽  
Enrico Sangiovanni ◽  
Roberta Maggio ◽  
Carlo Mattozzi ◽  
Stefania Zava ◽  
...  
Keyword(s):  
Cell Density ◽  
Skin Diseases ◽  
Inflammatory Responses ◽  
Human Keratinocytes ◽  
Suitable Model ◽  
Hacat Cells ◽  
Primary Human Keratinocytes ◽  
Proinflammatory Mediators ◽  
Cytokines And Chemokines

Cultured primary human keratinocytes are frequently employed for studies of immunological and inflammatory responses; however, interpretation of experimental data may be complicated by donor to donor variability, the relatively short culture lifetime, and variations between passages. To standardize the in vitro studies on keratinocytes, we investigated the use of HaCaT cells, a long-lived, spontaneously immortalized human keratinocyte line which is able to differentiate in vitro, as a suitable model to follow the release of inflammatory and repair mediators in response to TNFα or IL-1β. Different treatment conditions (presence or absence of serum) and differentiation stimuli (increase in cell density as a function of time in culture and elevation of extracellular calcium) were considered. ELISA and Multiplex measurement technologies were used to monitor the production of cytokines and chemokines. Taken together, the results highlight that Ca2+ concentration in the medium, cell density, and presence of serum influences at different levels the release of proinflammatory mediators by HaCaT cells. Moreover, HaCaT cells maintained in low Ca2+ medium and 80% confluent are similar to normal keratinocytes in terms of cytokine production suggesting that HaCaT cells may be a useful model to investigate anti-inflammatory interventions/therapies on skin diseases.

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