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INNOSC Theranostics and
Pharmacological Sciences Therapeutic value of terpenes

angiogenesis and metastasis, and (v) induce autophagy Terpenoids have demonstrated anticancer effects in
305
(e.g., through MAPK/ERK/JNK, PI3K/AKT/mTOR, several liver cancer cell lines through different mechanisms.
AMPK, and NF-κB signaling pathways). 298-302 For example, geraniol reduced the expression of HMG-CoA
306
Taxol (paclitaxel), a diterpenoid-based chemotherapy reductase to inhibit HepG2 cell growth, while asiatic
2+
drug, is widely used to treat solid-tumor cancers (e.g., lung, acid-induced apoptosis through increased intracellular Ca
307,308
prostate, breast, ovarian, esophageal, and melanoma) release and expression of p53.
303
and is considered one of the most effective terpenoid-based Oleanolic acid, ursolic acid, echinocystic acid,
310
309
309
chemotherapeutic drugs. Taxol exhibits its anticancer effect lupeol, and betulinic acid reportedly promoted
312
311
by destabilizing microtubules, resulting in mitotic arrest, apoptosis of cancer cells, while the anticancer property of
inhibition of cancer cell division, and ultimately cancer β-carotene is attributed to an antioxidant mechanism.
313
cell death. Taxol also indirectly promotes apoptosis by Various terpenes and their derivatives (e.g., geraniol and
304
binding to and inhibiting B-cell lymphoma 2 (Bcl-2) which neral) are natural inhibitors of the NF-κB signaling pathway
prevents cell death. 304 that plays a significant role in the pathological development
Table 7. Mechanisms of action of terpenes and terpenoids for treating various cancers
Terpene/ Origin Type of cancer Mechanism(s) of action Reference(s)
terpenoid (cell line)
Taxol N/A Female breast cancer Destabilizes microtubules to arrest cancer cell division and 304,316
induce cancer cell death; promotes apoptosis through binding
to Bcl-2
Geraniol N/A HCC Inhibits HepG2 cell growth through reducing HMG-CoA 305,306
(monoterpene) reductase production
Geraniol N/A Colon Cancer Inhibits polyamine biosynthesis and metabolism 317-321
(i.e., increased in cancer growth); apoptosis; DNA damage;
cell cycle arrest; disruption of cell membrane
Andrographolide Andrographis paniculata HCC Inhibits Hep3B cell growth (increase apoptosis, MAP kinases, 305,306,322
(diterpene) ERK1/2, and pJNK); inhibits MMP-7 expression
Limonene Lemon, orange, grapefruit, Human bladder cancer Inhibits human bladder cancer cell growth through apoptosis, 124
caraway, bergamot, cell (T24 cell line) caspase activation, and G2/M-phase cell cycle arrest
peppermint, spearmint, Colon, mammary, Induces apoptosis; inhibits the post-translational 299,323,324
dill, and tomato pancreatic, and isoprenylation of cell growth-regulating proteins
prostate cancers
Bladder cancer Induces cellular apoptosis; caspase activation; G2/M-phase 124
cell cycle arrest; inhibits cancer metastasis
Retinol Carrot, spinach, pumpkin, Prostate cancer Induces apoptosis; inhibits premalignant cell growth; 325-331
broccoli, mango, suppresses carcinogens through retinoid nuclear receptors,
papaya, cherry, tomato, retinoic acid receptors (RARs), and retinoid X receptors
corn, orange, cabbage, (RXRs)
watermelon, and lettuce
Lycopene Tomato, orange, carrot, Colon cancer Suppresses Akt signaling and non-phosphorylated β-catenin 299,332,333
pea, sprout, green, bean, protein levels; G-phase cell cycle arrest
and corn Prostate cancer N/A 334,335

Latilagascenes Extract from the Gastric (EPG85-257), N/A 336
C and D; Euphorbia species pancreatic
3β-acetoxy- (EPP85-181), and
helioscopinolide colon (HT-29)
B and E carcinomas
Geraniol Zingiber officinale (ginger) Endometrial cancer Promoted apoptosis by p53 activation 337
and neral (in cells
combination)
β-Caryophyllene Cannabis Sativa and Taxol-resistant model Activates apoptotic cascade; reduces cellular invasion 338
Pamburus missionis (SV1) of breast cancer
Abbreviations: HCC: Hepatocellular carcinoma; N/A: Not available.

Volume 7 Issue 3 (2024) 10 doi: 10.36922/itps.0332