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Triple-negative breast cancer (TNBC) is the most malignant and aggressive subtype of breast cancer. Currently, the treatment options to TNBC are limited and the discovery of new drugs and novel therapeutic strategies for treatment of TNBC is urgently needed. In this study, a series of melampomagnolide B (MMB) derivatives were designed, synthesized, and evaluated for their anti-TNBC activities. Compound 7 and 13a showed highly potent activity against different TNBC cells with IC 50 values ranging from 0.37 μM to 1.52 μM, which demonstrated 3.6- to 54-fold improvement comparing to the parent compound MMB. The phenotypic effect revealed that compound 7 and 13a could inhibit metastasis, induce apoptosis and arrest cell cycle distribution of TNBC cells. Furthermore, the mechanism research indicated compounds 7 and 13a bound IKKβ and inhibited the IKKβ-mediated phosphorylation of IκB and p65, then inhibited the nuclear translocation of p65 and eventually regulated the genes related to metastasis, apoptosis and cell cycle under NF-κB control. Moreover, compound 7 inhibited the tumor growth in vivo, and the weights of spleens and livers were also reduced compared with control group which indicated that compound 7 could inhibit metastasis of TNBC in vivo. These findings indicate that compound 7 may be used as a promising lead compound for ultimate discovery of anti-TNBC drug., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023 Elsevier Masson SAS. All rights reserved.)

Three new sesquiterpene lactone dimers (1-3) were isolated from the flowers of Inula japonica together with twenty-two known sesquiterpene derivatives (4-25). Their structures were established on the basis of detailed spectroscopic analyses. All isolates were evaluated for their antiproliferative activities against paclitaxel-resistant human non-small-cell lung cancer cell line A549/PTX. The preliminary structure-activity relationship was discussed. Compound 24 exhibited the most potent effect with the IC 50 value of 0.34 ± 0.10 μM, even more active than the clinically used drug paclitaxel (PTX, IC 50  = 1.40 ± 0.52 μM). Compound 24 showed significant efficacy of arresting the cell cycle at the G2-M stage, inducing apoptosis through mitochondria-mediated pathway, and inhibiting cell migration and invasion. Furthermore, compound 24 could reverse multidrug resistance through suppressing the expression of ABC family proteins., (Copyright © 2020 Elsevier Inc. All rights reserved.)

A series of twenty-three parthenolide-5-fluorouracil (5-FU) conjugates ware synthesized and evaluated for their anti-cancer activities against human hepatocellular carcinoma cell line Bel-7402 and 5-fluorouracil resistant human hepatocellular carcinoma cell line Bel-7402/5-FU. The preliminary structure-activity relationships were discussed. The most active compound 15d showed high activity against Bel-7402/5-FU cell line with IC 50 value of 2.25 μM, which demonstrated 5.8-fold improvement compared to that of the parent compound parthenolide (IC 50  = 12.98 μM). The investigation of preliminary molecular mechanism of 15d revealed that 15d could reverse drug resistance by inhibiting MDR1, ABCC1 and ABCG2 to increase the intracellular drug accumulation and induce apoptosis of Bel-7402/5-FU cells through mitochondria mediated pathway. On the base of these results, compound 15d is deserved to be further investigated as a potential anti-HCC lead compound for ultimate discovery of pathenolide-based anti-cancer drug., (Copyright © 2019 Elsevier Masson SAS. All rights reserved.)

One new eudesmane sesquiterpenoid, 11β-hydroxy-13-chloro-eudesm-5-en-12, 8-olide (1), was isolated from the roots of Inula helenium together with nine eudesmanolides (2-10) and one germacranolide (11). Their structures were elucidated on the basis of detailed spectroscopic analyses. All isolates were evaluated for their antiproliferative activities against human leukemia stem-like cell line KG1a. Compound 10 exhibited the most potent effect with the IC 50 value of 3.36 ± 0.18 μM. A further investigation revealed that compound 10 could significantly induce apoptosis of KG1a cells. Additionally, compound 10 had an obvious effect on the levels of apoptosis-related proteins (Bcl-2, Bax, cytochrome c, caspase 9 and caspase 3), indicating that the antiproliferative effect of compound 10 on KG1a cells might be mediated through a mitochondria-dependent apoptotic pathway., (Copyright © 2019 Elsevier Inc. All rights reserved.)