Substances extracted from the Annona squamosa leaf have analgesic and anti-arthritic potential, study reveals
Researchers tested the effects of the plant’s methanolic extract and an isolated alkaloid substance, palmatine, on mice. The results were promising.
Fundação de Amparo à Pesquisa do Estado de São Paulo
In Brazil, researchers have identified substances with analgesic, anti-inflammatory, anti-hyperalgesic (against persistent pain) and anti-arthritic activity in the leaves of Annona squamosa, a tree popularly known in the country as fruta-do-conde or pinha. The results of the research, supported by FAPESP through five projects (09/05992-6, 14/17436-9, 15/03726-8, 16/06407-3 and 21/09693-5), were published in the journal Pharmaceuticals.
The work involved scientists from the Federal University of Grande Dourados (UFGD), the Federal University of Mato Grosso do Sul (UFMS), the State University of Campinas (UNICAMP) and São Paulo State University (UNESP). The group evaluated the plant’s methanolic extract (methanol is used as a solvent and then removed by evaporation to obtain a dry extract) and an isolated substance called palmatine.
As the authors explain, Annona squamosa is already used medicinally in several countries and is used in folk medicine to treat pain and arthritis. Several pharmacological properties have been observed, such as gastroprotective, antibacterial, antiviral and anti-inflammatory properties. It represents a possible alternative to the main pharmacological treatments for pain, opioid analgesics and non-steroidal anti-inflammatory drugs, whose prolonged use can cause various side effects such as addiction, ulcers and cardiovascular thrombotic events. It can also be an alternative to the main anti-inflammatory drugs, such as glucocorticoid analogs and non-steroidal anti-inflammatory drugs, which in chronic treatment can lead to adrenal insufficiency and insulin resistance, among other problems.
“In view of this, the aim of the study was to investigate the analgesic, anti-arthritic and anti-inflammatory potential of the methanolic extract and palmatine obtained from Annona squamosa,” says Marcos José Salvador, full professor at the Department of Plant Biology at UNICAMP and co-author of the research.
To do this, the leaves of the plant were dried and turned into powder. The substances to be analyzed were then extracted. The methanolic extract and the alkaloid palmatine were administered orally to mice and studied in several experimental models, including pleurisy (inflammation of the pleura, the membranes that line the lungs and chest wall) induced by a substance called carrageenan; joint inflammation induced by zymosan; and mechanical hyperalgesia (increased sensitivity to painful stimuli) induced by TNF (tumor necrosis factor, a signaling protein produced by defense cells that plays a crucial role in regulating the immune response).
“The results showed that the methanolic extract and palmatine extracted from A. squamosa have analgesic and anti-inflammatory potential. Palmatine also has anti-hyperalgesic properties, which may involve inhibition of the tumor necrosis factor-mediated pathway,” explains Salvador. “We also concluded that palmatine may be one of the components responsible for the anti-arthritic properties of the plant.”
The conclusions of the analysis are very relevant and help to prove the therapeutic effects of the samples analyzed and to elucidate their mechanisms of action, which are not yet fully understood. However, further studies are needed before they can be used in practice to treat diseases.
“Further studies are needed to assess whether, in other formulations, the effects and pharmacokinetic properties of palmatine would be altered,” says the researcher, noting that more research is also needed to assess the toxicity of the compounds and the doses needed to achieve the therapeutic effect for clinical use.
About FAPESP
The São Paulo Research Foundation (FAPESP) is a public institution with the mission of supporting scientific research in all fields of knowledge by awarding scholarships, fellowships and grants to investigators linked with higher education and research institutions in the state of São Paulo, Brazil. FAPESP is aware that the very best research can only be done by working with the best researchers internationally. Therefore, it has established partnerships with funding agencies, higher education, private companies, and research organizations in other countries known for the quality of their research and has been encouraging scientists funded by its grants to further develop their international collaboration.
Journal
Pharmaceuticals
Article Title
Open AccessArticle Analgesic and Anti-Arthritic Potential of Methanolic Extract and Palmatine Obtained from Annona squamosa Leaves
Shiitake-derived functional food shows suppression of liver fibrosis progression
Early administration of AHCC at the stage of hepatitis might hold possibility of preventing onset of cirrhosis
Osaka Metropolitan University
Chronic liver damage can lead to hepatitis, which causes fibrosis of the liver. This buildup of collagen and other fibrous tissue accelerates when hepatic stellate cells become activated during hepatitis, often resulting in liver cancer or cirrhosis, both of which can be fatal. As there are no effective drugs to treat cirrhosis, suppressing the activation of the stellate cells is considered as a way of controlling the progression of liver fibrosis.
“It is estimated that one out of every 3-4 people worldwide have steatotic liver disease, when there is an abnormal accumulation of lipids, which is a precursor to fibrosis. So, it is important to prevent the progression of liver fibrosis at an early stage,” explained Dr. Hayato Urushima, an Associate Professor of the Graduate School of Medicine at Osaka Metropolitan University.
His research team investigated how AHCC (Amino Up Co., Ltd., Sapporo, Japan), a standardized extract of cultured Lentinula edodes mycelia, protects the liver and its mechanism.
The team administered AHCC to mice and found that the supplement might inhibit the activation of hepatic stellate cells through two channels.
Via the TLR2 (toll-like receptor protein) channel, AHCC induced cytoglobin that decreased reactive oxygen species, while via the TLR4 channel, the supplement suppressed the expression of collagen in the liver of the mice.
“We aim to conduct clinical trials to confirm the efficacy of AHCC in patients with liver fibrosis to build more reliable scientific evidence,” Dr. Urushima stated.
The findings were first published online on September 24, 2024, in the American Journal of Physiology-Gastrointestinal and Liver Physiology, with the final version published on November 6, 2024.
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About OMU
Established in Osaka as one of the largest public universities in Japan, Osaka Metropolitan University is committed to shaping the future of society through “Convergence of Knowledge” and the promotion of world-class research. For more research news, visit https://www.omu.ac.jp/en/ and follow us on social media: X, Facebook, Instagram, LinkedIn.
Journal
AJP Gastrointestinal and Liver Physiology
Method of Research
Experimental study
Subject of Research
Animals
Article Title
AHCC inhibited hepatic stellate cells activation by regulation of cytoglobin induction via TLR2-SAPK/JNK pathway and collagen production via TLR4-NF-κβ pathway
COI Statement
AHCC® is a trademark of Amino Up Co., Ltd., Sapporo, Japan. Dr. Urushima received a research grant from Amino Up Co., Ltd. None of the other authors has any conflicts of interests to disclose.
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