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Background: The beautyberry (Callicarpa arborea Roxb.) is member of the family Lamiaceae and is native to Asia. It is used in different traditional medicines for the treatment of debilitating ailments including cancer, dermatitis, diabetes mellitus, gastritis, helminthiasis, and pyrexia. A couple of pentacyclic triterpenes and phytosterols have been reported from this plant. Objective: We aimed to investigate the antiparasitic potentials of C. arborea bark extract. We used an intestinal tapeworm, Raillietina echinobothrida, for its convenience in handling and established nature as a model helminth parasite. Materials and Methods: The extract of the stem bark was prepared using methanol. Tapeworms were treated in vitro with varying concentrations of the extract. Survival values were statistically analysed. Treated tapeworms were fixed and processed for scanning electron microscopy. Results: C. arborea bark extract showed dose-dependent antiparasitic similar to that of albendazole. Scanning electron microscopy revealed damaging effects all over the body of the tapeworm. There was general shrinkage of the tegument on the scolex, neck region and strobila. Microtriches were completely removed throughout the tegument. Suckers and rostellum on the scolex were also deformed. Conclusion: Our data shows that C. arborea is a promising source of antiparasitic principles. [ABSTRACT FROM AUTHOR]

Background Despite the availability of synthetic antidiabetic drugs, diabetes mellitus is still affecting millions of people with increasing rate of disease incidence and mortality throughout the world. Ethnomedicinal survey documents the traditional usefulness of Callicarpa arborea Roxb. stem bark in the management of diabetes mellitus. Materials and methods In our study, hydro-alcoholic extract ( HAE ) of Callicarpa arborea stem bark was prepared according to WHO guidelines for herbal drugs, and screened for antidiabetic activity in streptozotocin (STZ)-induced diabetic rats. Acute oral toxicity and in vitro antioxidant activity studies along with phytochemical analyses of HAE were also carried out. Results Acute oral toxicity study indicated that HAE was safe up to a dose of 2000 mg/kg body weight of rats. Results of antidiabetic activity study revealed that HAE of C. arborea stem bark possesses significant ( p < 0.05) hypoglycemic activity compared to normal control group in experimental rats. Histological observations of treated pancreas and liver tissues confirmed the antidiabetic efficacy of HAE . In antioxidant activity, HAE exhibited significant radical scavenging activity. Conclusion From results, it can be concluded that HAE of C. arborea stem bark may have possible role as herbal antioxidants in the prevention and/or treatment of oxidative stress-induced diabetes mellitus. The antioxidant property of plant phenolic and flavonoid contents present in HAE might be responsible for the antidiabetic efficacy of C. arborea stem bark. [ABSTRACT FROM AUTHOR]

[Display omitted] • 66 ent -clerodane diterpenoids, including 52 new compounds, were isolated from Callicarpa arborea. • Their bioactivity against pyroptosis were evaluated, and the typical α,β-unsaturated-γ-hemiacetal lactone ring was a key active segments from SAR analysis. • Compound 1 showed potent inhibitory activity against pyroptosis by blocking NLRP3 inflammasome activation. • Compound 1 treatment markedly reduced infiltration of CD11b+F4/80+ macrophages into lung and protected lung injury in LPS- induced septic mice. Pyroptosis is a programmed-inflammatory cell death, which leads to release of inflammatory cellular contents and formation of inflammation. Uncontrollable pyroptosis can result in serious immune diseases, such as cytokine release syndrome (CRS), sepsis, disseminated intravascular coagulation (DIC), and acute organ damage, including acute respiratory distress syndrome (ARDS) and acute kidney injury (AKI). Members of the Callicarpa genus are significant raw materials for traditional Chinese medicine, widely used for analgesia, hemostasis, and anti-inflammation. Previously, we have reported some ent -clerodane diterpenoids from Callicarpa arborea , shown potent inhibitory effects against pyroptosis. In this study, we went on investigating this kind of diterpenoids, and yielded 66 ent -clerodane diterpenoids, including 52 new compounds, from Callicarpa arborea. Their structures featured with a 5/6- (1 – 25) or a 6/6- (26 – 66)-fused double-ring scaffolds, were elucidated using spectroscopic data, electrostatic circular dichroism (ECD) and X-ray diffraction analyses. Screening for the inhibitory activity against pyroptosis by detecting of IL-1β secretion in J771A.1 cells, revealed 28 compounds with an IC 50 below 10.5 μM. Compound 1 was the most potent with an IC 50 of 0.68 μM and inhibited the J774A.1 macrophage pyroptosis by blocking the NLR pyrin domain containing 3 (NLRP3) inflammasome activation. An in vivo study further revealed that compound 1 decreased infiltration of CD11b + F4/80 + macrophages into lung and attenuated the lipopolysaccharide (LPS)-induced lung injury. Taken together, this study indicated the potential of compound 1 as a candidate for pyroptosis-related inflammation treatment, as well as provided the chemical and pharmacological basis for the further development of Callicarpa genus as a herbal medicine. [ABSTRACT FROM AUTHOR]