Monday, February 22, 2021

Artemisia plant extracts show potential anti-SARS-CoV-2 activity in vitro

A team of scientists from Germany and the USA recently explored the effectiveness of traditional plant medicines in treating severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection. Their findings reveal that various extracts of two medicinal plants, namely Artemisia annua and Artemisia afra, can potentially inhibit SARS-CoV-2 replication in vitro without causing any cytotoxicity. The study is currently available on the bioRxiv* preprint server.

Study: In vitro efficacy of Artemisia extracts against SARS-CoV-2. Image Credit: Scisetti Alfio / Shutterstock Background
Study: In vitro efficacy of Artemisia extracts against SARS-CoV-2. Image Credit: Scisetti Alfio / Shutterstock Background

Background

The recent outbreak of coronavirus disease 2019 (COVID-19), caused by the SARS-CoV-2 pathogen, has put a large burden on the healthcare systems of many countries globally. Although about 80% of COVID-19 patients develop only mild symptoms or remain asymptomatic, the disease has claimed more than 2.4 million lives worldwide since its emergence in December 2019. In the initial phase of the pandemic, many antiviral medicines already approved for other diseases have been repurposed to treat critically ill COVID-19 patients. Many vaccines with good efficacy and safety levels have also been developed and approved in record time to curb the pandemic's growth.

Various synthetic derivatives (artesunate) of artemisinin, which is a bioactive natural compound found in Artemisia annua plants, are typically being used as antimalarial medicines. The antimicrobial properties of these bioactive compounds have been recognized clinically. Different extracts of Artemisia annua containing high amount of artemisinin are currently undergoing phase 2 clinical trials to treat COVID-19 patients. Since April 2020 in Madagascar, Covid-Organics drinks containing mainly Artemisia annua extracts are being used as a miracle intervention to treat and prevent COVID-19.     

In the current study, the scientists have explored the efficacy of Artemisia annua and Artemisia afra extracts and Covid-Organics in preventing SARS-CoV-2 infection in vitro. Using various animal cell lines, they specifically examined whether these plant products are able to inhibit replication of SARS-CoV-2 and feline coronavirus.

Important observations

Both water and ethanolic extracts of dried leaves of Artemisia annua and Artemisia afra were used in this study. In addition, 500 mg of pure artemisinin and dried form of 50 ml of Covid-Organics were dissolved in dimethyl sulfoxide and tested for activity using various in vitro experimentations.

To determine its antiviral activity, the scientists first incubated feline coronavirus with different concentrations of plant extracts and pure artemisinin solution on a monolayer of feline kidney cells. Using plaque formation assay, they observed that all tested extracts significantly inhibited viral replication in a dose-dependent manner. Specifically, they observed that at a concentration range of 5 – 10 mg/ml, all tested extracts significantly inhibited viral replication, whereas no inhibition was observed at less than 2 mg/ml concentration. Based on these findings, they selected the most potent extracts with the highest antiviral activity for further experimentations on SARS-CoV-2.

A set of experiments conducted using the monkey kidney cell line revealed that the extracts at a concentration of less than 2 mg/ml had potent antiviral activity against SARS-CoV-2. The strongest SARS-CoV-2 inhibitory effects were observed for water extracts of Artemisia annua and Artemisia afra and an ethanolic extract of Artemisia annua. Since Artemisia afra does not contain artemisinin, the scientists believe that other bioactive compounds present in the plant may be responsible for the observed anti-SARS-CoV-2 activity.  

Using a separate set of experiments, the scientists estimated that these extracts could induce cytotoxic effects at a concentration range of 10 – 20 mg/ml, which was significantly higher than the concentrations required for antiviral activities. This observation indicates that these extracts can potently inhibit SARS-CoV-2 replication without affecting cell viability.

The preparations made from Covid-Organics drink showed higher antiviral activity against SARS-CoV-2 compared to Feline coronavirus. However, the selectivity index (the window between cytotoxicity and antiviral activity) of Covid-Organics drink was estimated to be 5.2, making it less promising as an antiviral medicine.

(a) Images of the SARS-CoV-2 plaques incubated with different dilutions of Covid- Organics. The dose is expressed by percentage of the raw drink. (b) Concentrationdependent inhibition SARS-CoV-2 replication using different extracts. Values are expressed as mean ±SD,
(a) Images of the SARS-CoV-2 plaques incubated with different dilutions of Covid- Organics. The dose is expressed by percentage of the raw drink. (b) Concentrationdependent inhibition SARS-CoV-2 replication using different extracts. Values are expressed as mean ±SD, n=3.

Study significance

The study reveals that various extracts of Artemisia annua and Artemisia afra have potential antiviral activities against SARS-CoV-2. However, the scientists mention that further studies are required to check whether appropriate serum levels of Artemisia compounds needed to inhibit SARS-CoV-2 can be achieved in patients. Moreover, further animal and human clinical trials are required to determine whether these in vitro observations can be translated for actual clinical use.

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Tuesday, February 06, 2018

Methylene blue can be used for treating malaria

Methylene blue — used as medication and dye — could act as a safe anti-malarial that kills malaria parasites at an unprecedented rate, results from a clinical trial have revealed. Every year, malaria infects more than 200 million people and causes more than 430,000 deaths across the globe.  Methylene blue is a blue dye that is used in laboratories to distinguish dead cells from living cells. Malaria patients who were treated with a combination of the blue dye and artemisinin-based combination therapy were cured of the disease within two days, the study, published in a journal showed. The patients no longer transmitted the parasite if they are bitten again by a mosquito. 

“Methylene blue is very promising, because it can prevent the spread of malaria within such a short time following treatment,” said a researcher.  “There are also indications that methylene blue also works well in species that are resistant to certain medicines,” he added.

Malaria parasites are increasingly resistant to the artemisinin-based combination therapies that are currently used.


In addition, these medicines do very little to stop the spread of malaria, as the parasites remain in the blood for a long time, with the chance that other mosquitoes are infected if they feed on the patient.  However, adding the dye to the anti-malaria medicine ensured that patients no longer infected other mosquitoes, within as little as 48 hours.  Patients who were not given methylene blue were able to infect other mosquitoes for at least a week.  “We noted that the male parasites disappeared from the bloodstream more quickly than the female parasites,” he said, adding that the dye was found to be safe and was tolerated well by patients.  However, it turns the urine bright blue, which could stop people from using it, the researchers said. 


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Sunday, April 09, 2017

Solution for obesity in medicinal herb? Chinese scientists discover magical compound!

The fact that obesity is a step toward long term health problems is not unknown.

It can negatively affect most of your organs – especially the heart – make you vulnerable to diabetes, joint pains, arthritis, make it difficult for women during pregnancy – basically, impact your overall health.

Obesity is one of the biggest problems that is swiftly becoming a part of everyone's life. The rising number of obese people around the world just goes to show how we are allowing a particular lifestyle to dictate us into an unhealthy state of being.

Various diets, numerous forms of exercise are supremely helpful, but these things will bear fruit only if they are offered pure dedicated and devoted effort.

Now, to help you in your weight loss journey, Chinese scientists have discovered a compound from the extract of a medicinal herb which targets cell metabolism and may help prevent obesity.

The new compound Celastrol was extracted from thunder god vine, a natural extract that reduces pain and inflammation, and artemisinin developed from sweet wormwood.

The research team led by Zhang Xiaokun, professor with the College of Medicine at Xiamen University, found that Celastrol could clear inflamed mitochondria from cells to alleviate inflammation, state-run Xinhua news agency reported.

Mitochondria plays an integral role in cell death, immunity and inflammation. By affecting inflamed mitochondria, Celastrol can help control cell metabolism.

Zhang said his team would continue to research how Celastrol regulates metabolism to explore new drugs with low toxicity and high efficiency to help people lose weight.

The team carried out the research on mice and found that Celastrol could effectively control weight increases in mice feeding on high fat food.

Like sweet wormwood, thunder god vine is native to China though it also grows in other East Asian countries.

The herb has been used in traditional Chinese medicine for treating arthritis and autoimmune diseases, the report said.

However, the whole plant is extremely toxic and in modern research has been used in clinical trials on AIDS treatment.

Its compounds have been found to have the potential to treat joint pain and rheumatoid arthritis, the report said.



The discovery of artemisinin had won Chinese scientist Tu Youyou the Nobel Prize in 2015.

The research was published in science journal Molecular Cell on Thursday.

The research has been supported by the National Nature and Science Foundation and Xiamen South Sea Center.


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Wednesday, April 25, 2012

A synthetic anti-malaria drug

 India has developed a powerful new malaria drug - an alternative to the global drug of choice Artemisinin - that promises to be a major boost to India's pharmaceutical research.

What is most exciting about this new drug is that its raw materiel is synthetic (derived chemically in the lab) as against Artemisinin, which is derived from a plant.


 A Dr.  from the National Institute of Malaria Research (NIMR) said this new once-a-day therapy for three days contains Arterolane and Piperaquine.

"Clinical trials conducted by NIMR comparing the Arterolane and Piperaquine combination has shown it to be as effective and as safe as artemisinin combinations like Artesunate and Sulphadoxine which is used in the national malaria programme," said the Dr, who was the principal investigator of the trials.

Artemisinin derivatives are most rapid acting and effective anti-malarial medicines, according to the.  Dr.

Artemisinin is the only high-volume drug that continues to be produced from a plant-based source. China and Vietnam provide 70% and East Africa 20% of the raw material. Seedlings are grown in nurseries and then transplanted into fields. It takes about eight months for them to attain full size. The plants are harvested, leaves dried and sent to facilities where artemisinin is extracted. The market price for artemisinin has fluctuated widely, between $120 and $1,200 per kg from 2005 to 2008.


However, they are plant derived and, therefore, there can be mismatch in demand and supply. It is used in combination with different drugs (artemisinin-based combination therapy). Now, five combinations are recommended by WHO. On the other hand, since this new drug is synthetic, its raw materials are created chemically in the lab. This will ensure constant supply of raw material and standardize costs," added the Dr .


Arterolane in combination with long acting piperaquine has been studied in phase II and III clinical trials in India, Bangladesh and Thailand. Most malaria parasites have become resistant to anti-malarial drugs.

To protect artemisinin from developing resistance, it is recommended that it should only be used in combination with partners and oral artemisinin should never be used as monotherapy. The Drugs Controller General of India has imposed a ban on use of oral artemisinin monotherapy for uncomplicated falciparum malaria.

Artemisinin resistance is characterized by slow parasite clearance. Artemisinin Combination Therapies (ACT) kills malaria parasite in a human bloodstream within 24-36 hours. With the drug-resistant strain, ACT needs up to 120 hours to kill the parasite.

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