Compound from medicinal herb kills brain-eating amoebae in lab studies — ScienceDaily

Primary amoebic meningoencephalitis (PAM), a deadly disease caused by the “brain-eating amoeba” Naegleria fowleri, is becoming more common in some areas of the world, and it has no effective treatment. Now, researchers reporting in ACS Chemical Neuroscience have found that a compound isolated from the leaves of a traditional medicinal plant, Inula viscosa or “false yellowhead,” kills the amoebae by causing them to commit cell suicide in lab studies, which could lead to new treatments.

PAM, characterized by headache, fever, vomiting, hallucinations and seizures, is almost always fatal within a couple of weeks of developing symptoms. Although the disease, which is usually contracted by swimming in contaminated freshwater, is rare, increasing cases have been reported recently in the U.S., the Philippines, southern Brazil and some Asian countries. Amphotericin B is the most common therapy given to those with the infection. It can kill N. fowleri in the lab, but it isn’t very effective when given to patients, likely because it cannot cross the blood-brain barrier. Ikrame Zeouk, José Piñero, Jacob Lorenzo-Morales and colleagues wanted to explore whether compounds isolated from I. viscosa, a strong-smelling plant that has long been used for traditional medicine in the Mediterranean region, could effectively treat PAM.

The researchers first made an ethanol extract from the herb’s leaves, finding that it could kill N. fowleri amoebae. Then, they isolated and tested specific compounds from the extract. The most potent compound, inuloxin A, killed amoebae in the lab by disrupting membranes and causing mitochondrial changes, chromatin condensation and oxidative damage, ultimately forcing the parasites to undergo programmed cell death, or apoptosis. Although inuloxin A was much less potent than amphotericin B in the lab, the structure of the plant-derived compound suggests that it might be better able to cross the blood-brain barrier. More studies are needed to confirm this hypothesis, the researchers say.

The authors acknowledge funding from the European Regional Development Fund, the Spanish Ministry of Economic Affairs and Digital Transformation, the Spanish Ministry of Science, Innovation and Universities, the University of La Laguna and the Augustin de Betancourt Foundation.

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Talk show host Ellen DeGeneres sells her Montecito compound for $45.7 million

Talk-show host Ellen DeGeneres may have had a tough year on the professional front, but she’s proven she still has the touch when it comes to selling houses.

The serial property flipper and her wife, the actress Portia de Rossi, have offloaded their sprawling LA compound, located in the exclusive enclave of Montecito, for $45.7 million (US$33.3 million), Variety reports.

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The sale price is lower than the star couple had been hoping for however, with the property hitting the market a month ago with $56 million (US$40 million) price hopes.

The new buyer has yet to be identified, but they reportedly purchased the entire property in cash, records reveal.

Dengeres and De Rossi originally bought the hilltop residence early in 2019 for $38 million (US$27 million), and hastily got to work expanding and modernising the showstopping house.

They then dropped another US$1.9 million on the smaller adjacent home that was also included in the sale.

The nearly 1,000 sqm m property boasts a 760 sqm three-bedroom main house, a one-bedroom guesthouse, a cabana with a gym, and a security office, according to Realtor.

The total offering – set behind large gates and looking out onto the Pacific Ocean – has multiple structures, five bedrooms, five full bathrooms, and five half-baths, on 9.3 acres of land.

Ellen selling her latest LA house. Picture: Realtor

The home has gated entry. Picture: Realtor

The couple also added a new state-of-the-art security system, featuring multiple cameras and infra-red lasers, following a widely reported burglary at the property.

The sprawling grounds include a koi pond, sports court, many lush plants and sprawling lawns.

Built in 2011, the main house opens onto a veranda with a fire pit, dining area, and seating, and looks out to a vanishing edge pool that juts over the hillside.

Ellen selling her latest LA house. Picture: Realtor

The dramatic main room with walls of glass. Picture: Realtor

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Entering directly into the great room with bamboo ceilings and walls of glass, the large space includes living and dining areas that lead outside.

Ellen selling her latest LA house. Picture: Realtor

Ellen used one of the bedrooms as an office. Picture: Realtor

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The luxurious main bedroom includes a spalike bath with a built-in stone tub that looks out to the mountain and ocean views, and also contains two sinks and a separate shower.

The showbiz couple have bought and sold multiple properties over the years across California.

Ellen selling her latest LA house. Picture: Realtor

The bathroom has a large built-in stone tub. Picture: Realtor

The couple also own a posh Beverly Hills mansion they bought from Adam Levine, another home-flipping celeb, which they picked up last year for nearly $60 million (US$42.5 million).

DeGeneres has been the cause of much negative publicity this year, contending with reports of a negative work environment at her show, leading to the ousting of several top executives.

In April, the talk show host also compared being in coronavirus lockdown to being in prison, when she was filming one of her ‘at-home editions’ of her show.

“One thing that I’ve learned from being in quarantine is that people — this is like being in jail, is what it is,” DeGeneres said in the video.

Ellen selling her latest LA house. Picture: Realtor

The kitchen opens to outdoor dining space. Picture: Realtor

“It’s mostly because I’ve been wearing the same clothes for 10 days and everyone in here is gay. The jokes that I have. I feel bad for the kids at home, all the college students, all the parents. I feel bad for a lot of people. But I think that a lot of people out there need words of encouragement, and that’s what I want to do.”

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Scientists develop a lead compound to fight chemotherapy-resistant prostate cancer

Scientists of Far Eastern Federal University (FEFU), together with German and Russian colleagues, have developed a lead compound to fight chemotherapy-resistant prostate cancer. The original design comes out as scientists combine biologically active molecules from the chemically modified pigment of sea urchins with glucose molecules to deliver the active drug substance inward the tumor cells. A related article recently was published in Marine Drugs.

To cure prostate cancer scientists decided to capitalize on the Warburg effect, which turns as tumor cells inclination to eat lots of “sugar”, i.e. consume glucose compounds more intensively comparing to the majority of normal cells.

Researchers took active molecules analogous to the molecules isolated from sea urchins pigment and “sewed” on a sugar tail to them using Sulfur linker to tie up. The resulted compound was introduced to the cell culture of prostate cancer sustainable to Docetaxel, a standard chemotherapeutic drug. The outcome was cancer cells died more efficiently.

The scientific breakthrough comes out as the result of the close cooperation of teams from Russia and Germany that includes collaborators from FEFU School of Natural Sciences (Vladivostok Russia), University Medical Center Hamburg-Eppendorf (Germany), G.B. Elyakov Pacific Institute of Bioorganic Chemistry (PIBOC FEB RAS, Vladivostok, Russia), and University of Greifswald (Germany).

The Russian-German scientific paper was recognized as a best research article of the current issue of Marine Drugs.

In our study, we benefit from the chance to combine the ideas and experience of specialists from different countries. Firstly, we had at our disposal analogues of biologically active compounds from sea urchins which antitumor potential had been increased via chemical modification by Far Eastern colleagues from PIBOC FEB RAS. Secondly, we used the broad experience of German colleagues in the field of prostate cancer to establish and explain the mechanism that makes tumor cells more sensitive to glucose-related molecules. It turned out that prostate cancer cells have a large number of receptors responsible for the uptake of glucose and associated molecules into the cell.”

Dr. Sergey Dyshlovoy, senior researcher at the Laboratory of Biologically Active Compounds of FEFU School of Natural Science

The scientist went on that although new drug compound effectively targets prostate cells culture there is a good prospect it might cure other types of cancer if the outcome of the first clinical trials is positive. The majority of tumor cells consume more glucose than healthy cells of the body.

The research outcomes not only in the new compound of sea urchins molecules tagged with glucose but also in the new way of conjugating them via Sulfur, instead of Oxygen, as it used to be early. The reason for the new method of molecules connection is a looking for the drug not breaking up by enzymes in the bloodstream before it hits a tumor target. Previous experiments confirm that compounds joined via Oxygen molecules are not as stable as needed.

Fall 2020, researchers plan to start the study possible side effects of the new drug, first on mice and then on other laboratory animals. Before this, the molecule of the drug compound will be further modified to assure its even greater stability in the bloodstream. The patent will secure the rights to a new generation molecule.

Considering the time spent on laboratory and subsequent clinical trials, as well as in case of these trials’ success, a new on-the-shelf drug should approach the market in the next 10 years.

Prostate cancer is the second most deadly cancer for men living in developed countries.


Journal reference:

Dyshlovoy, S.A., et al. (2020) Inspired by Sea Urchins: Warburg Effect Mediated Selectivity of Novel Synthetic Non-Glycoside 1,4-Naphthoquinone-6S-Glucose Conjugates in Prostate Cancer. Marine Drugs.

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