Phytochemical constituents and toxicological, anti-inflammatory, and antinociceptive assessment of Baliospermum effusum Pax et Hoffm.

Baliospermum effusum Pax et Hoffm., a shrub known as "Baodongdian" in Dai folk medicine, has been traditionally employed for treating traumatic injuries, rheumatism, and jaundice. The present study investigated the acute toxicity, anti-inflammatory and antinociceptive properties, and phytochemical constituents of the 95 % ethanolic extract of B. effusum (EEBe). The toxicity assessment revealed that EEBe (2000 mg/kg) induced no adverse effects in behavior, mortality, body/organ weights, histopathology, or biochemical parameters over 14 d. Pharmacological assays on EEBe (150, 300, and 600 mg/kg) revealed that it effectively inhibited carrageenan-induced paw edema (n = 10), xylene-stimulated ear edema (n = 8), and acetic acid-triggered writhes (n = 8), while showing no significant antinociceptive activity in the hot-plate test (n = 8). ELISA (n = 8) showed that EEBe modulated serum IL-1β, IL-6, and IL-10 levels, while qRT-PCR (n = 5) demonstrated the downregulation of IL-1β and IL-6 mRNA expression. Furthermore, eight compounds including 4-hydroxy-2,3-dimethyl-2-nonen-4-olide (1), 22-dehydroclerosterol (2), β-sitosterol (3), vanillin (4), 1-linolenoylglycerol (5), 1-O-stearoyl-glycerol (6), bis(2,3-dihydroxypropyl)nonanedioate (7), and (3S,5S)-diverniciaoid A (8) were isolated from EEBe, with compounds 5 and 7 suppressing NO production in LPS-induced RAW 264.7 macrophages. These data revealed that EEBe was non-toxic at 2000 mg/kg and exhibited anti-inflammatory and antinociceptive properties, and that 5 and 7, reported for the first time from this species, showed anti-inflammatory activity in vitro, collectively supporting the folk use of B. effusum for inflammatory and pain-related disorders. To our knowledge, this is the first report on the in vivo pharmacological activities and toxicity of B. effusum.