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Anticancer and Anti-Inflammatory Activities of a Standardized Dichloromethane Extract from Piper umbellatum L. Leaves
Leilane Hespporte Iwamoto1, Débora Barbosa Vendramini-Costa2, Paula Araújo Monteiro3
1Department of Pharmacology, Anaesthesiology and Therapeutics, Faculty of Dentistry, University of Campinas, Avenida Limeira 901, 13414-903 Piracicaba, SP, Brazil ; Chemical, Biological and Agricultural Pluridisciplinary Research Center (CPQBA), University of Campinas, Rua Alexandre Cazelatto 999, Vila Betel, 13148-218 Paulínia, SP, Brazil.
Abstract:
Despite the advances in anticancer drug discovery field, the worldwide cancer incidence is remarkable, highlighting the need for new therapies focusing on both cancer cell and its microenvironment. The tumor microenvironment offers multiple targets for cancer therapy, including inflammation. Nowadays, almost 75% of the anticancer agents used in chemotherapy are derived from natural products, and plants are an important source of new promising therapies. Continuing our research on Piper umbellatum species, here we describe the anticancer (in vitro antiproliferative activity and in vivo Ehrlich solid tumor model) and anti-inflammatory (carrageenan-induced paw edema and peritonitis models) activities of a standardized dichloromethane extract (SDE) from P. umbellatum leaves, containing 23.9% of 4-nerolidylcatechol. SDE showed in vitro and in vivo antiproliferative activity, reducing Ehrlich solid tumor growth by 38.7 and 52.2% when doses of 200 and 400 mg/kg, respectively, were administered daily by oral route. Daily treatments did not produce signals of toxicity. SDE also reduced paw edema and leukocyte migration on carrageenan-induced inflammation models, suggesting that the anticancer activity of SDE from Piper umbellatum leaves could involve antiproliferative and anti-inflammatory effects. These findings highlight P. umbellatum as a source of compounds against cancer and inflammation.
Insights
A standardized extract from Piper umbellatum leaves demonstrated significant anticancer and anti-inflammatory effects in preclinical models. This natural product shows promise for developing new therapies targeting both cancer cells and the tumor microenvironment.
Area of Science:
- Pharmacology
- Natural Products Chemistry
- Oncology
Background:
- Cancer incidence remains high, necessitating novel therapies targeting cancer cells and the tumor microenvironment.
- Natural products, particularly from plants, are crucial sources for anticancer drug discovery.
- Inflammation within the tumor microenvironment presents a therapeutic target.
Purpose of the Study:
- To evaluate the anticancer and anti-inflammatory activities of a standardized dichloromethane extract (SDE) from Piper umbellatum leaves.
- To investigate the potential of SDE as a source for new cancer and inflammation therapies.
Main Methods:
- In vitro antiproliferative assays.
- In vivo evaluation using an Ehrlich solid tumor model in mice.
- Assessment of anti-inflammatory effects in carrageenan-induced paw edema and peritonitis models.
- Chemical standardization of the extract for 4-nerolidylcatechol content.
Main Results:
- SDE exhibited significant in vitro and in vivo antiproliferative activity against Ehrlich solid tumors.
- Oral administration of SDE (200 and 400 mg/kg) reduced tumor growth by 38.7% and 52.2%, respectively.
- SDE demonstrated anti-inflammatory effects by reducing paw edema and leukocyte migration.
- No signs of toxicity were observed during daily oral treatments.
Conclusions:
- Piper umbellatum leaf extract possesses both anticancer and anti-inflammatory properties.
- The observed anticancer effects may be partly mediated by its anti-inflammatory actions.
- P. umbellatum is a promising source for developing novel therapeutic agents against cancer and inflammation.
