Studies on the Anti-Inflammatory Activity of Rhizomes ofNelumbo nucifera

Abstract

The anti-inflammatory activity of the methanol extract of Nelumbo nucifera rhizome as well as of betulinic acid, a steroidal triterpenoid isolated from it, were evaluated on carrageenin and serotonin induced rat paw edema. Methanol extract at doses of 200 and 400 mg/kg and betulinic acid at doses of 50 mg/kg and 100 mg/kg p.o., showed significant anti-inflammatory activity in both the models of inflammation in rats. The effects produced were comparable to that of phenylbutazone and dexamethasone, two prototype anti-inflammatory drugs.

Toxicity of betulin derivatives and in vitro effect on promastigotes and amastigotes of Leishmania infantum and L. donovani

“…Some compounds did not show any noticeable toxicity with this method (2, 7, 16, 17 and 20), and no apparent structure-activity relationship was observed between toxicity for the J774 cells and the compound subgroup (that is, derivatives having C-3 ketone carbonyl: compounds 10 and 11 were toxic, but L-aspartyl amide of betulinic acid 12 was non-toxic). However, all betulin derivatives having both hydroxyl groups acetylated (6,16,17,18) were non-toxic to J774 cells. It is noticeable that even betulin 1 exhibited certain toxicity (18.4 ± 0.4% inhibition).…”

“…In the subgroup of heterocyclic betulin derivatives (16)(17)(18)(19)(20), clearer structure-activity relationship trend could be observed. Compounds with sterically less bulky R3 and R4 groups showed better activity, when compared with more hindered derivatives.…”

“…On the other hand, 28-O-cinnamoylbetulin 2 was less active against amastigotes. From the subgroup of heterocyclic betulin derivatives (16)(17)(18)(19)(20), compounds 16, …”

“…14,15 It has been suggested that betulinic acid has anticancer, anti-HIV and antimicrobial properties. 16,17 Some related compounds have shown antileishmanial activity against L. donovani (promastigotes and amastigotes) 18 and L. amazonensis. 19 More recently, studies have been carried out on the effect of a high number of betulinic derivatives on axenic amastigotes and amastigotes of L. donovani in the THP-1 cell line.…”

Effect of 3β, hydroxy-lup-20(29)-en-28-oic acid on 7,12-Dimethylbenz(a) anthracene impaired cellular homeostasis in extrahepatic organs of Sprague Dawley rats

“…[15][16][17] Betulinic acid is known for various biological activities including anti-inflammatory, anti-viral, anti-neoplastic, anti-tumor, and anti-HIV. [18][19][20][21][22] Its anti-tumor activity has also been reported in human neoplastic cell lines including lung, ovarian, cervical, colorectal, breast and prostate. 23 Induction of apoptosis via direct mitochondrial alterations, formation of reactive oxygen species, modulation of BCL-2 and BAX levels and topoisomerases Iα and IIα have been suggested as its possible mechanism of action.…”