Lupeol is a useful AR mold for developing new therapeutics to cure human elk cancer (CaP). After 48 hours of treatment, lupeol (10-50 μM) inhibited the proliferation of androtrophic phenotype (ADPC) cells, namely LAPC4 and LNCaP cells, with IC50 values of 15.9 and 17.3 μM. Lupeol reduced the development of 22Rv_1 with an IC50 of 19.1 μM. Lupeol inhibits C4-2b cell growth at an IC50 of 25 μM. Lupeol has the ability to inhibit ADPC and CRPC. Phenotypic CaP cell growth capacity. Androgens, through AR activation, are known to promote CaP cell proliferation [1].

One powerful medication that may reduce the tumorigenicity of CaP cells in the stroma is lupeol. Total circulatory PSA levels (via stromal tumor cell apoptosis) were assessed on day 56 of the research. At poststromal day 5 56, PSA levels in control rats with LNCaP and C4-2b tumors varied from 11.95 to 12.79 ng/mL, respectively. Conversely, rats treated with lopezol showed lower serum PSA levels, ranging from 4.25-7.09 ng/mL. Serum PSA levels were lower in tumor tissue from animals given lopeol than in control subjects [1].

Interactions
In in vivo studies, using an orthotopic metastatic nude mouse model of oral tongue squamous cell carcinoma, lupeol at a dose of 2 mg/animal dramatically decreased tumor volume and suppressed local metastasis, which was more effective than cisplatin alone. Lupeol exerted a significant synergistic cytotoxic effect when combined with low-dose cisplatin without side effects....
... The present study ... investigated the effects of lupeol on 7,12-dimethylbenz[a]anthracene (DMBA), induced DNA strand breaks in mouse skin, using an alkaline unwinding assay. Increasing doses of lupeol (50-200 ug/mouse) were given topically, prior or after the single topical application of DMBA (100 ug/mouse) with the sampling time of 24, 48, 72 and 96 hr, respectively. Both pre and post treatment of lupeol showed significant (p<0.001) preventive effects in DMBA induced DNA strand breaks in dose and time dependent manner. The pre-treatment of lupeol at the dose of 200 ug/mouse showed 56.05% prevention, and post-treatment at the same dose showed 43.26% prevention, at 96 hr time interval, against DMBA induced DNA strand breakage...
... The antigenotoxic potential of lupeol, a triterpene, and mango pulp extract (MPE) was evaluated in Swiss albino mice. Benzo[a]pyrene (B[a]P), a well-known mutagen, was given at a single dose of 100 mg/kg body weight intraperitoneally. Pretreatment with lupeol (1 mg/animal) and MPE (1 mL, 20%) was given through oral intubation for 7 days prior to B[a]P administration. Animals from all the groups were killed at sampling time of 24 hr and their bone marrow tissue was analyzed for chromosomal damage and micronuclei induction. In B[a]P-treated animals a significant induction of chromosomal aberration and micronuclei was recorded, with a decrease in mitotic index. In lupeol- or MPE-supplemented groups, a significant decrease in B[a]P-induced clastogenicity was recorded. The incidence of aberrant cells and micronuclei was found to be reduced by both lupeol and MPE when compared to the B[a]P-treated group. The anti-cytotoxic effects of lupeol or MPE were also evident, as observed by significant increase in mitotic index. Thus, results of the present investigation revealed that lupeol and MPE have protective effects against B[a]P-induced clastogenic changes in Swiss albino mice.
To investigate antioxidant potential of lupeol/mango pulp extract (MPE) in testosterone induced oxidative stress in prostate of male Swiss albino mice. .... lupeol (1 mg/animal) and MPE (1 mL [20% w/v]/animal) was given /orally/ to animals along with subcutaneous injection of testosterone (5 mg/kg body weight) consecutively for 15 days. At the end of the study period, the prostate was dissected out for the determination of reactive oxygen species (ROS) levels, lipid peroxidation and antioxidant enzymes status (catalase, superoxide dismutase, glutathione reductase, glutathione-S-transferase). RESULTS: In testosterone treated animals, increased ROS resulted in depletion of antioxidant enzymes and increase in lipid peroxidation in mouse prostate. However, lupeol/MPE treatment resulted in a decrease in ROS levels with restoration in the levels of lipid peroxidation and antioxidant enzymes. ... The results of the present study demonstrate that lupeol/MPE are effective in combating oxidative stress-induced cellular injury of mouse prostate...
For more Interactions (Complete) data for LUPEOL (14 total), please visit the HSDB record page.

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Non-Human Toxicity Values
LD50 Rat oral >2 g/kg /from table/
LD50 Mouse oral >2 g/kg /from table/

[1]. Lupeol, a novel androgen receptor inhibitor: implications in prostate cancer therapy. Clin Cancer Res. 2011 Aug 15;17(16):5379-91.

Lupeol is a pentacyclic triterpenoid that is lupane in which the hydrogen at the 3beta position is substituted by a hydroxy group. It occurs in the skin of lupin seeds, as well as in the latex of fig trees and of rubber plants. It is also found in many edible fruits and vegetables. It has a role as an anti-inflammatory drug and a plant metabolite. It is a secondary alcohol and a pentacyclic triterpenoid. It derives from a hydride of a lupane.
Lupeol has been investigated for the treatment of Acne.
Lupeol has been reported in Camellia sinensis, Acanthus ilicifolius, and other organisms with data available.
See also: Calendula Officinalis Flower (part of).

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Mechanism of Action
Lupeol, a triterpene found in fruits and vegetables, selectively induced substantial head and neck squamous cell carcinoma (HNSCC) cell death but exhibited only a minimal effect on a normal tongue fibroblast cell line in vitro. Down-regulation of NF-kappaB was identified as the major mechanism of the anticancer properties of lupeol against HNSCC. Lupeol alone was not only found to suppress tumor growth but also to impair HNSCC cell invasion by reversal of the NF-kappaB-dependent epithelial-to-mesenchymal transition. Lupeol exerted a synergistic effect with cisplatin, resulting in chemosensitization of HNSCC cell lines with high NF-kappaB activity in vitro.

C30H50O

426.729

426.386

545-47-1

259846

White to off-white solid powder

1.0±0.1 g/cm3

488.1±14.0 °C at 760 mmHg

215-216ºC

216.9±12.4 °C

0.0±2.8 mmHg at 25°C

1.516

10.98

1

1

1

31

766

10

CC(=C)[C@@H]1CC[C@]2([C@H]1[C@H]3CC[C@@H]4[C@]5(CC[C@@H](C([C@@H]5CC[C@]4([C@@]3(CC2)C)C)(C)C)O)C)C

MQYXUWHLBZFQQO-QGTGJCAVSA-N

InChI=1S/C30H50O/c1-19(2)20-11-14-27(5)17-18-29(7)21(25(20)27)9-10-23-28(6)15-13-24(31)26(3,4)22(28)12-16-30(23,29)8/h20-25,31H,1,9-18H2,2-8H3/t20-,21+,22-,23+,24-,25+,27+,28-,29+,30+/m0/s1

Lup-20(29)-en-3-ol, (3-beta)-

NSC 90487Monogynol BLupeol β-ViscolClerodol Fagarasterol Lupenol

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Ethanol : ~14.29 mg/mL (~33.49 mM)
DMSO : ~2 mg/mL (~4.69 mM)

Solubility in Formulation 1: ≥ 1.43 mg/mL (3.35 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear EtOH + stock solution to 900 μL of corn oil and mix well.

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Solubility in Formulation 2: 20 mg/mL (46.87 mM) in Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

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 (Please use freshly prepared in vivo formulations for optimal results.)