Batimastat (BB-94) is a potent broad-spectrum inhibitor of matrix metalloproteinases (MMPs), capable of inhibiting MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, with IC50 values of 3nM, 4nM, 4nM, 6nM and 20nM, respectively[1]. Batimastat (BB-94) belongs to the hydroxamic acid class of compounds, which can chelate zinc ions, thereby inhibiting the activity of MMPs[2]. Batimastat (BB-94) can cause cell cycle disturbances in ovarian cancer cells[3].
In vitro, Batimastat (BB-94) (5μM) treatment of hematological tumor cell lines (HL-60, F36P, H929 cells) for 48h reduced cell viability and cell density, and significantly increased intracellular ERK1/2 phosphorylation[4].
In vivo, Batimastat (BB-94) (5, 10, 20mg/kg) treated with intraperitoneal injection in rats with colitis improved the inflammation score and reduced myeloperoxidase (MPO) activity in a dose-dependent manner[5]. Batimastat (BB-94) (30mg/kg) treated with intraperitoneal injection in rats with periodontal disease significantly increased periodontal bone destruction and had a deleterious effect on the progression of periodontal disease[6].
References:
[1] Yin Z, Sada A A, Reslan O M, et al. Increased MMPs expression and decreased contraction in the rat myometrium during pregnancy and in response to prolonged stretch and sex hormones[J]. American Journal of Physiology-Endocrinology and Metabolism, 2012, 303(1): E55-E70.
[2] Ferry G, Boutin J A, Hennig P, et al. A zinc chelator inhibiting gelatinases exerts potent in vitro anti-invasive effects[J]. European journal of pharmacology, 1998, 351(2): 225-233.
[3] Erba E, Ronzoni S, Bassano L, et al. The metalloproteinase inhibitor batimastat (BB-94) causes cell cycle phase perturbations in ovarian cancer cells[J]. Annals of Oncology, 1999, 10(5): 589-591.
[4] Alves R, Pires A, Jorge J, et al. Batimastat Induces Cytotoxic and Cytostatic Effects in In Vitro Models of Hematological Tumors[J]. International Journal of Molecular Sciences, 2024, 25(8): 4554.
[5] Di Sebastiano P, Di Mola F F, Artese L, et al. Beneficial effects of Batimastat (BB-94), a matrix metalloproteinase inhibitor, in rat experimental colitis[J]. Digestion, 2001, 63(4): 234-239.
[6] Björnsson M J, Havemose‐Poulsen A, Stoltze K, et al. Influence of the matrix metalloproteinase inhibitor batimastat (BB‐94) on periodontal bone destruction in Sprague‐Dawley rats[J]. Journal of periodontal research, 2004, 39(4): 269-274.
Batimastat (BB-94)是一种有效的广谱基质金属蛋白酶（MMPs）抑制剂，能够抑制MMP-1，MMP-2，MMP-9，MMP-7和MMP-3，IC50值分别为3nM，4nM，4nM，6nM和20nM[1]。Batimastat (BB-94)属于羟肟酸类化合物，能够螯合锌离子，从而抑制MMPs的活性[2]。Batimastat (BB-94)能够引起卵巢癌细胞的细胞周期扰动[3]。
在体外，Batimastat (BB-94)（5μM）处理血液肿瘤细胞系（HL-60, F36P, H929细胞）48h，降低了细胞活力和细胞密度，显著增加了细胞内ERK1/2磷酸化[4]。
在体内，Batimastat (BB-94)（5, 10, 20mg/kg）通过腹腔注射治疗结肠炎大鼠，以剂量依赖性方式改善了炎症评分，降低了髓过氧化物酶（MPO）活性[5]。Batimastat (BB-94)（30mg/kg）通过腹腔注射治疗牙周病大鼠，显著增加了牙周骨破坏，对牙周病的进展具有有害影响[6]。