Abstract
Introduction: Ursolic acid (UA), belongs to a group of pentacyclic triterpenoids and is known to possess some very interesting biological properties. Protocols have been developed in order to synthesize bioactive UA analogs which have resulted in numerous ursolic acid analogs being synthesized during the period 2012–2016. Ursolic acid and its analogues can be employed to treat various cancers, inflammatory diseases, diabetes, Parkinson’s disease, Alzheimer’s disease, hepatitis B, hepatitis C and AIDS to mention but a few. Areas covered: This review covers patents on therapeutic activities of ursolic acid (UA) and its synthetic derivatives published during the four year period 2012–2016. A discussion about structure-activity relationships (SAR) of these analogs is also included. Expert opinion: Ursolic acid and its synthetic derivatives demonstrated excellent anticancer, antidiabetic, antiarrhythmic, anti-hyperlipidemic, antimicrobial, anti-hypercholesterolemic, and anti-cardiovascular properties. Additionally, various ursolic acid analogues have been synthesized through modification at positions C2-OH, C3-OH and C17-CO2H. It is noteworthy that the C-17 amide and amino analogs of UA possessed better anticancer activity compared to the parent compound (UA). Most importantly, UA has the potential to conjugate with other anticancer drugs or be transformed into its halo derivatives since this will greatly facilitate scientists to get lead compounds in cancer drug discovery.
| Original language | English |
|---|---|
| Pages (from-to) | 1061-1072 |
| Number of pages | 12 |
| Journal | Expert Opinion on Therapeutic Patents |
| Volume | 27 |
| Issue number | 9 |
| DOIs | |
| Publication status | Published - Sep 2 2017 |
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Keywords
- anti-inflammatory
- anticancer
- diabetes
- in vitro
- in vivo
- Ursolic acid
ASJC Scopus subject areas
- Pharmacology
- Drug Discovery
Cite this
Ursolic acid derivatives for pharmaceutical use : a patent review (2012-2016). / Hussain, Hidayat; Green, Ivan R.; Ali, Iftikhar; Khan, Ikhlas A.; Ali, Zulfiqar; Al-Sadi, Abdullah M.; Ahmed, Ishtiaq.
In: Expert Opinion on Therapeutic Patents, Vol. 27, No. 9, 02.09.2017, p. 1061-1072.Research output: Contribution to journal › Review article
}
TY - JOUR
T1 - Ursolic acid derivatives for pharmaceutical use
T2 - a patent review (2012-2016)
AU - Hussain, Hidayat
AU - Green, Ivan R.
AU - Ali, Iftikhar
AU - Khan, Ikhlas A.
AU - Ali, Zulfiqar
AU - Al-Sadi, Abdullah M.
AU - Ahmed, Ishtiaq
PY - 2017/9/2
Y1 - 2017/9/2
N2 - Introduction: Ursolic acid (UA), belongs to a group of pentacyclic triterpenoids and is known to possess some very interesting biological properties. Protocols have been developed in order to synthesize bioactive UA analogs which have resulted in numerous ursolic acid analogs being synthesized during the period 2012–2016. Ursolic acid and its analogues can be employed to treat various cancers, inflammatory diseases, diabetes, Parkinson’s disease, Alzheimer’s disease, hepatitis B, hepatitis C and AIDS to mention but a few. Areas covered: This review covers patents on therapeutic activities of ursolic acid (UA) and its synthetic derivatives published during the four year period 2012–2016. A discussion about structure-activity relationships (SAR) of these analogs is also included. Expert opinion: Ursolic acid and its synthetic derivatives demonstrated excellent anticancer, antidiabetic, antiarrhythmic, anti-hyperlipidemic, antimicrobial, anti-hypercholesterolemic, and anti-cardiovascular properties. Additionally, various ursolic acid analogues have been synthesized through modification at positions C2-OH, C3-OH and C17-CO2H. It is noteworthy that the C-17 amide and amino analogs of UA possessed better anticancer activity compared to the parent compound (UA). Most importantly, UA has the potential to conjugate with other anticancer drugs or be transformed into its halo derivatives since this will greatly facilitate scientists to get lead compounds in cancer drug discovery.
AB - Introduction: Ursolic acid (UA), belongs to a group of pentacyclic triterpenoids and is known to possess some very interesting biological properties. Protocols have been developed in order to synthesize bioactive UA analogs which have resulted in numerous ursolic acid analogs being synthesized during the period 2012–2016. Ursolic acid and its analogues can be employed to treat various cancers, inflammatory diseases, diabetes, Parkinson’s disease, Alzheimer’s disease, hepatitis B, hepatitis C and AIDS to mention but a few. Areas covered: This review covers patents on therapeutic activities of ursolic acid (UA) and its synthetic derivatives published during the four year period 2012–2016. A discussion about structure-activity relationships (SAR) of these analogs is also included. Expert opinion: Ursolic acid and its synthetic derivatives demonstrated excellent anticancer, antidiabetic, antiarrhythmic, anti-hyperlipidemic, antimicrobial, anti-hypercholesterolemic, and anti-cardiovascular properties. Additionally, various ursolic acid analogues have been synthesized through modification at positions C2-OH, C3-OH and C17-CO2H. It is noteworthy that the C-17 amide and amino analogs of UA possessed better anticancer activity compared to the parent compound (UA). Most importantly, UA has the potential to conjugate with other anticancer drugs or be transformed into its halo derivatives since this will greatly facilitate scientists to get lead compounds in cancer drug discovery.
KW - anti-inflammatory
KW - anticancer
KW - diabetes
KW - in vitro
KW - in vivo
KW - Ursolic acid
UR - http://www.scopus.com/inward/record.url?scp=85028015219&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=85028015219&partnerID=8YFLogxK
U2 - 10.1080/13543776.2017.1344219
DO - 10.1080/13543776.2017.1344219
M3 - Review article
C2 - 28637397
AN - SCOPUS:85028015219
VL - 27
SP - 1061
EP - 1072
JO - Expert Opinion on Therapeutic Patents
JF - Expert Opinion on Therapeutic Patents
SN - 1354-3776
IS - 9
ER -