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...
/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B/
C-17 BICYCLIC AMINES OF TRITERPENOIDS WITH HIV MATURATION INHIBITORY ACTIVITY
申请人：BRISTOL-MYERS SQUIBB COMPANY
公开号：US20130296554A1
公开（公告）日：2013-11-07
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 bicyclic amines of triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III:
These compounds are useful for the treatment of HIV and AIDS.
申请人：THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATE
公开号：US20180370911A1
公开（公告）日：2018-12-27
In one aspect, the invention provides a method of promoting a carbon-sulfur bond forming reaction. In certain embodiments, the reaction comprises cross-coupling of a(n) (hetero)aryl halide with a thiol to form the carbon-sulfur bond, wherein the method is promoted by light irradiation in the absence of a photocatalyst. In other embodiments, the cross-coupling reaction can be promoted through visible light irradiation, including sunlight.
C-3 ALKYL AND ALKENYL MODIFIED BETULINIC ACID DERIVATIVES
申请人：BRISTOL-MYERS SQUIBB COMPANY
公开号：US20140243298A1
公开（公告）日：2014-08-28
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, alkyl and alkenyl C-3 modified betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV:
a compound of Formula I
a compound of Formula II
a compound of Formula III
and a compound of Formula IV
These compounds are useful for the treatment of HIV and AIDS.
C-3 CYCLOALKENYL TRITERPENOIDS WITH HIV MATURATION INHIBITORY ACTIVITY
申请人：Bristol-Myers Squibb Company
公开号：US20130210787A1
公开（公告）日：2013-08-15
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-3 cycloalkenyl triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II, III and IV:
wherein X can be a C
4-8
cycloalkyl, C
4-8
cycloalkenyl, C
4-9
spirocycloalkyl, C
4-9
spirocycloalkenyl, C
4-8
oxacycloalkyl, C
4-8
dioxacycloalkyl, C
6-8
oxacycloalkenyl, C
6-8
dioxacycloalkenyl, C
6-9
oxaspirocycloalkyl, or C
6-9
oxaspirocycloalkenyl ring. These compounds are useful for the treatment of HIV and AIDS.
FORMULATIONS FOR THE DELIVERY OF ACTIVE AGENTS TO INSECTS, PLANTS, AND PLANT PATHOGENS
申请人：Preceres Inc.
公开号：US20170325457A1
公开（公告）日：2017-11-16
The present disclosure is directed to formulations comprising (1) at least one formulation transport agent, (2) at least one complexing agent, and (3) at least one active agent that modulates one or more traits of a target insect, plant, or plant pathogen. The present disclosure is also directed to methods of delivering such formulations to the target organism, as well as to formulation transport agents used to prepare such formulations.
