Non-steroidal anti-inflammatory drugs (NSAIDs) inhibit prostanoid formation and represent prevalent therapeutics for treatment of inflammatory disorders. However, NSAIDs are afflicted with severe side effects, which might be circumvented by more selective suppression of pro-inflammatory eicosanoid biosynthesis. This concept led to dual inhibitors of microsomal prostaglandin E₂ synthase (mPGES)-1 and 5-lipoxygenase that are crucial enzymes in the biosynthesis of pro-inflammatory prostaglandin E₂ and leukotrienes. The potential of their dual inhibition in light of superior efficacy and safety is discussed. Focus is placed on natural products, for which direct inhibition of mPGES-1 and leukotriene biosynthesis has been confirmed.

非甾体类抗炎药（NSAIDs）抑制前列腺素的形成，代表了治疗炎症性疾病的流行疗法。然而，NSAIDs遭受严重的副作用，这可以通过更选择性地抑制促炎性类二十烷酸生物合成来避免。该概念导致了微粒体前列腺素E ₂合酶（mPGES）-1和5-脂氧合酶的双重抑制剂，它们是促炎性前列腺素E ₂和白三烯生物合成中的关键酶。鉴于其优越的功效和安全性，对其双重抑制的潜力进行了讨论。重点放在天然产物上，已证实其直接抑制了mPGES-1和白三烯的生物合成。