Aim. Traditionally, C. sappan medicine was the heartwood, which needs to be cut down as a whole. In this research, the antitumor activity and mechanisms of the leaves and stems were compared with the roots of Caesalpinia sappan; it was in order to investigate whether stems and leaves of C. sappan could be used to replace heartwood for antitumor treatment, thereby reducing resource destruction. Methods. MTT assays were used to identify the active sites of C. sappan based on the application of human liver cancer (HuH-7) cells. High-performance liquid chromatography (HPLC) was used to analyze polar extracts. We also established a H22 hepatoma-bearing mouse model by administering intraperitoneal injections of petroleum ether extracts from the leaves and stems (SY②) at doses of 20 and 65 mg/kg. Mice in the i.g. group were administered intragastrically with the same extracts (at doses of 100 and 325 mg/kg) at the same time (12 days). Results. The antitumor site of C. sappan was the petroleum ether extract. The IC50 for the petroleum ether extract of roots (SG②) was 56.10 μg/ml, while that for the leaves and stems (SY②) was 77.20 μg/ml. Grey relational analysis indicated 11 active fraction peaks that were closely related to antitumor activity. The size of tumors in H22 hepatoma-bearing mice was reduced significantly in mice administered with petroleum ether extracts from the leaves and stems (inhibition rates of high doses were 55.31% and 60.56%). Fibrous tissue proliferation, inflammatory cell infiltration, tumor cell necrosis, and the expression of proliferating cell nuclear antigen (PCNA) and vascular endothelial growth factor (VEGF) were all lower than in the control group (VEGF < 0.001 and PCNA < 0.05). Conclusion. Petroleum ether extracts of the roots, leaves, and stems of C. sappan exhibit certain antitumor effects. Our data indicate that the mechanisms underlying these effects may relate to a reduction in the expression of PCNA and VEGF and the inhibition of angiogenesis. Our findings indicate that we can expand the medicinal use of C. sappan to the leaves and stems, thus improving resource utilization and reducing resource damage.
Miao medicine Tiekuaizi (Radix Chimonanthi) has been successfully used by Guizhou Miao ethnic physicians in clinical treatments, demonstrating significant curative effects. The research progress on the resource distribution, traditional uses, phytochemistry, and pharmacology of Tiekuaizi was reviewed by collecting related literature from traditional Chinese medicine books and various databases. Based on the comprehensive review and centered around the principles of traditional Chinese medicine quality marker (Q-Marker) theory, nine secondary metabolites (scopoletin, scopolin, isofraxidin, fraxin, scoparone, calycanthoside, 6, 7, 8-trimethoxycoumarin, tomenin, and calycanthine) are suggested as potential Q-markers for Tiekuaizi to establish quality control standards. This can provide a valuable reference for the collection and processing, pharmaceutical production, and effectiveness and safety of clinical applications of Miao medicine Tiekuaizi.
C 19 H 16 O 6 , triclinic, P 1 ‾ $\overline{1}$ (no. 2), a = 8.248(2) Å, b = 9.657(3) Å, c = 11.753(4) Å, α = 69.300(8)°, β = 79.359(8)°, γ = 65.703(8)°, V = 797.3(4) Å 3 , Z = 2, Rgt ( F ) = 0.0676, w Rref ( F2 ) = 0.1629, T = 296 K.
The BMP2-Smad signaling pathway serves as a central regulator of osteoblast differentiation and bone formation, rendering it a promising target for the discovery of osteogenic agents from natural sources. Nonetheless, direct BMP2-binding ligands derived from complex herbal extracts remain poorly characterized. In the present study, surface plasmon resonance (SPR)-based target fishing against BMP2, in conjunction with UPLC-Q-TOF-MS identification, was employed to screen for bioactive ligands from Periploca forrestii, a traditional Miao medicinal plant used for bone-related conditions. Six caffeoylquinic acid derivatives, namely neochlorogenic acid (NCA), 3-O-caffeoyl-4-O-sinapoylquinic acid, chlorogenic acid (CA), cryptochlorogenic acid (CCA), isochlorogenic acid B (IB), and isochlorogenic acid C (IC), were captured as direct BMP2-binding ligands. All six compounds promoted osteoblast differentiation and mineralization in MC3T3-E1 Subclone 14 cells, with IB displaying the strongest binding affinity and bioactivity. Mechanistically, IB failed to rescue the osteogenic suppression induced by the BMP type I receptor inhibitor LDN-193189, indicating its dependence on BMP signaling. In an LPS-induced inflammatory model, IB significantly reversed the downregulation of key proteins in the BMP2-Smad pathway (p-Smad1, Smad4, and Runx2) and osteogenic marker genes (Osterix, COL1A1, and OCN), demonstrating its capacity to restore osteogenic function under compromised conditions. Collectively, these findings establish that caffeoylquinic acid derivatives, particularly IB, function as BMP2-targeting osteogenic constituents of P. forrestii that activate BMP2-Smad signaling to promote osteoblast differentiation, thereby offering a pharmacological basis for the development of natural product-derived osteogenic agents.