Background: Jingshu Keli (JSKL), a traditional Chinese medicine (TCM) formula consisting of multiple active compounds, has been officially approved by National Medical Products Administration (NMPA) for treatment of cervical radiculopathy. It relieves pain, according to TCM theory, by activating blood circulation to dissipate blood stasis. The pain mainly stems from neurogenic inflammation caused by mechanical compression of the cervical nerve root. In addition, inflammation mediators also cause the development of other joint diseases, such as osteoarthritis (OA). The purpose of this paper was to evaluate the anti-inflammatory effects of JSKL and identify the biologically active herbs and compounds in vitro. Methods: Enzyme-linked immunosorbent assay (Elisa) was used to determine the expression of pro-inflammatory cytokines, tumor necrosis factor-alpha (TNF-α), interleukin 6 (IL-6) and interleukin 8 (IL-8), in the culture medium of human MH7A cells stimulated by lipopolysaccharides (LPS). Results: JSKL and three single-herb capsules, Cinnamomum cassia Presl (C.C.), Angelica Sinensis (Oliv.) Diels (A.S.) and Carthamus tinctorius L. (C.T.), significantly inhibited the secretion of TNF-α. If one of these three herbal components was removed, suppressing effect of the single-herb-deleted JSKL on TNF-α was abolished. Cinnamaldehyde (CIN) from C.C. was the most potent ingredient that inhibited the expression of IL-6 and IL-8 in the culture medium of both LPS-stimulated MH7A cells and primary synovial cells. Conclusions: JSKL was found to possess anti-inflammatory effect in vitro; C.C., A.S. and C.T. were the principal and essential herbal components responsible for such activity; CIN from C.C. is one the most potent single compound among indicator components of JSKL recorded in 2015 Chinese pharmacopoeia. This study provided scientific evidence for the clinical application of JSKL as an agent for targeted treatment of cervical radiculopathy. Furthermore, CIN has potential to be used for the treatment of some inflammation-related orthopedic diseases, such as rheumatic arthritis and osteoarthritis.