Benzofurans

Publication Title: 
Neurobiology of Aging

Epidemiological evidence implies a role for chronic stress and stress-related disorders in the etiopathogenesis of sporadic Alzheimer's disease (AD). Although chronic stress exposure during various stages of life has been shown to exacerbate AD-related cognitive deficits and neuropathology in AD mouse models, the role of stress exposure during the prenatal period on AD development and progression remained to be investigated.

Author(s): 
Sierksma, Annerieke S. R.
Prickaerts, Jos
Chouliaras, Leonidas
Rostamian, Somayeh
Delbroek, Lore
Rutten, Bart P. F.
Steinbusch, Harry W. M.
van den Hove, Daniel L. A.
Publication Title: 
ChemMedChem

Au naturel! (+)-Usnic acid (green) is a weak antimalarial agent, however, in conjugation with known antimalarial scaffolds and drugs, such as dihydroartemisinin (blue), potent activity against the blood-stage parasite can be seen both in vitro and in vivo. The compound shown exhibits an IC(50) value of 1.4 nM against Plasmodium falciparum in vitro and proved nearly as efficacious as artesunate in a mouse model of infection.

Author(s): 
Bruno, Michela
Trucchi, Beatrice
Monti, Diego
Romeo, Sergio
Kaiser, Marcel
Verotta, Luisella
Publication Title: 
Cancer Prevention Research (Philadelphia, Pa.)

The protein kinase Akt plays an important role in cell proliferation and survival in many cancers, including prostate cancer. Due to its kinase activity, it serves as a molecular conduit for inhibiting apoptosis and promoting angiogenesis in most cell types. In most of the prostate tumors, Akt signaling is constitutively activated due to the deletion or mutation of the tumor suppressor PTEN, which negatively regulates phosphatidylinositol 3-kinase through lipid phosphatase activity.

Author(s): 
Kumar, Raj
Srinivasan, Sowmyalakshmi
Koduru, Srinivas
Pahari, Pallab
Rohr, Jürgen
Kyprianou, Natasha
Damodaran, Chendil
Publication Title: 
The Journal of Organic Chemistry

A base-catalyzed condensation of phenyl acetate with acid chloride, followed by intramolecular cyclization and microwave-assisted cross-metathesis reaction, leads to the first total synthesis of psoralidin, a natural product with a broad range of biological activities, in a highly convergent and regioselective manner.

Author(s): 
Pahari, Pallab
Rohr, Jürgen
Publication Title: 
Apoptosis: An International Journal on Programmed Cell Death

The tumor necrosis factor (TNF) receptor super family comprises of members that induce two distinct signaling cascades, leading to either cell survival or apoptosis. However, in prostate cancer (PCa), TNF-mediated prosurvival signaling is the predominant pathway that leads to cell survival and resistance to therapy. Although inhibition of TNF signaling by pharmacological agents or monoclonal antibodies has gained importance in the field of cancer therapy, toxicity to normal cells has impaired their extensive use for cancer treatment.

Author(s): 
Srinivasan, Sowmyalakshmi
Kumar, Raj
Koduru, Srinivas
Chandramouli, Aaditya
Damodaran, Chendil
Publication Title: 
Molecular Cancer Therapeutics

Epidermal growth factor receptor (EGFR) activation is an important event that regulates mitogenic signaling, such as the Raf, mitogen-activated protein kinase (MAPK), and extracellular signal-regulated kinase 1/2 cascades. EGFR activation has been implicated in the transition of prostate cancer from androgen dependence to independence. Therefore, inhibition of EGFR may effectively suppress prostate cancer growth and progression.

Author(s): 
Kumar, Raj
Srinivasan, Sowmyalakshmi
Pahari, Pallab
Rohr, Jürgen
Damodaran, Chendil
Publication Title: 
Bioscience, Biotechnology, and Biochemistry

Eisenia arborea is an edible brown alga occasionally used as a folk medicine in gynecopathy in Japan. A new phlorotannin was isolated from the alga during our search for naturally occurring anti-allergic compounds from edible algae guided by the inhibitory effect on histamine release from rat basophile leukemia (RBL)-2H3 cells. The phlorotannin was called "phlorofucofuroeckol-B." Its structure was determined by spectral analysis and chemical conversion.

Author(s): 
Sugiura, Yoshimasa
Matsuda, Kohji
Yamada, Yasuhiro
Nishikawa, Masashi
Shioya, Kazufumi
Katsuzaki, Hirotaka
Imai, Kunio
Amano, Hideomi
Publication Title: 
Toxicology in vitro: an international journal published in association with BIBRA

Usnic acid (UA) is the most common and abundant lichenic secondary metabolite with potential therapeutic application. Anti-inflammatory and antitumour properties have already been reported and UA-enriched extracts are widely used to treat several diseases in the folk medicine. First, we performed in silico evaluation of UA interactions with genes/proteins and important compounds for cellular redox balance and NO pathway.

Author(s): 
Rabelo, Thallita Kelly
Zeidán-Chuliá, Fares
Vasques, Laura Milán
dos Santos, João Paulo Almeida
da Rocha, Ricardo Fagundes
Pasquali, Matheus Augusto de Bittencourt
Rybarczyk-Filho, José Luiz
Araújo, Adriano Antunes Souza
Moreira, José Cláudio Fonseca
Gelain, Daniel Pens
Publication Title: 
Canadian Journal of Gastroenterology = Journal Canadien De Gastroenterologie

Globally, people are struggling with obesity. Many effective, nonconventional methods of weight reduction, such as herbal and natural dietary supplements, are increasingly being sought. Fat burners are believed to raise metabolism, burn more calories and hasten fat loss. Despite patient perceptions that herbal remedies are free of adverse effects, some supplements are associated with severe hepatotoxicity.

Author(s): 
Yellapu, Radha K.
Mittal, Vivek
Grewal, Priya
Fiel, Mariaisabel
Schiano, Thomas
Publication Title: 
Canadian Journal of Gastroenterology = Journal Canadien De Gastroenterologie

Globally, people are struggling with obesity. Many effective, nonconventional methods of weight reduction, such as herbal and natural dietary supplements, are increasingly being sought. Fat burners are believed to raise metabolism, burn more calories and hasten fat loss. Despite patient perceptions that herbal remedies are free of adverse effects, some supplements are associated with severe hepatotoxicity.

Author(s): 
Yellapu, Radha K.
Mittal, Vivek
Grewal, Priya
Fiel, Mariaisabel
Schiano, Thomas

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