EFSA Compendium of Botanicals

Draft - work in progress

Leonotis leonurus (L.) R.Br.

Family:: Lamiaceae
Approval state:: Approved
Number of articles retrieved:: 141
Number of processed references:: 11

Compositions

#1: Diterpene lactones #2: Tannins #3: Alkaloids #4: Saponins #5: Labdane diterpenes #6: Diterpene lactone #7: Marrubiin (labdane diterpene) #8: Labdane diterpenes #9: Labdane diterpenes #10: Stachydrine #11: Epoxides

Endpoint Studies

#1: Acute toxicity #2: Short term toxicity (histopathological changes in the lungs, mortality) #3: Subchronic toxicity (hepatotoxicity) #4: Short term toxicity (histopathological changes in the kidneys) #5: Hematological changes #6: Nephrotoxicity #7: Hepatotoxicity

Genotoxicity

Composition #1: Laonigro, Guglielmo., Lanzetta, Rosa., Parrilli, Michelangelo., Adinolfi, Matteo., Mangoni, Lorenzo. The configuration of the diterpene spiro ethers from Marrubium vulgare and from Leonotis leonurus. gazzetta chimica italiana, 1979, p. 145–150. .

Language:

English (en)
Plant part:

Unspecified (A07XD)
Extraction/Preparation method:

Solvent extraction (A0BZR)
Additional extraction description:

unspecified
Substance:

diterpene lactones (RF-00004306-PAR)
Additional substance description:

premarrubiin I and II
Analytical method code:

Nuclear Magnetic Resonance (NMR) (F061A)
Analytical method - additional description:

IR
Yes/No Qualitative:

Positive/Present (POS)
Result type:

Qualitative Value (Binary) (BIN)
Internal remarks:

Diterpene lactones

Composition #2: Bienvenu, E., Amabeoku, GJ., Eagles, PK., Scott, G., Springfield, EP. Anticonvulsant activity of aqueous extract of Leonotis leonurus. phytomedicine, 2002, vol. 9, no. 3, p. 217–223. DOI: 10.1078/0944-7113-00103. [DOI link]

Language:

English (en)
Plant part:

Leaves (as part-nature) (A0EKT)
Extraction/Preparation method:

Solvent extraction (A0BZR)
Additional extraction description:

water
Substance:

Tannins (RF-00004337-PAR)
Analytical method code:

Phytochemical screening (F604A)
Yes/No Qualitative:

Positive/Present (POS)
Result type:

Qualitative Value (Binary) (BIN)
Internal remarks:

Tannins

Composition #3: Bienvenu, E., Amabeoku, GJ., Eagles, PK., Scott, G., Springfield, EP. Anticonvulsant activity of aqueous extract of Leonotis leonurus. phytomedicine, 2002, vol. 9, no. 3, p. 217–223. DOI: 10.1078/0944-7113-00103. [DOI link]

Language:

English (en)
Plant part:

Leaves (as part-nature) (A0EKT)
Extraction/Preparation method:

Solvent extraction (A0BZR)
Additional extraction description:

water
Substance:

Alkaloids (RF-00004360-PAR)
Analytical method code:

Phytochemical screening (F604A)
Yes/No Qualitative:

Positive/Present (POS)
Result type:

Qualitative Value (Binary) (BIN)
Internal remarks:

Alkaloids

Composition #4: Bienvenu, E., Amabeoku, GJ., Eagles, PK., Scott, G., Springfield, EP. Anticonvulsant activity of aqueous extract of Leonotis leonurus. phytomedicine, 2002, vol. 9, no. 3, p. 217–223. DOI: 10.1078/0944-7113-00103. [DOI link]

Language:

English (en)
Plant part:

Leaves (as part-nature) (A0EKT)
Extraction/Preparation method:

Solvent extraction (A0BZR)
Additional extraction description:

water
Substance:

Saponins (RF-00004333-PAR)
Additional substance description:

steroid and triterpenoid saponins
Analytical method code:

Phytochemical screening (F604A)
Yes/No Qualitative:

Positive/Present (POS)
Result type:

Qualitative Value (Binary) (BIN)
Internal remarks:

Saponins

Composition #5: McKenzie, J. M., Green, I. R., Mugabo, P. Leonurun, a novel labdane diterpenoid from Leonotis leonurus. south african journal of chemistry-suid-afrikaanse tydskrif vir chemie, 2006, vol. 59, p. 114–116. .

Language:

English (en)
Plant part:

Leaves (as part-nature) (A0EKT)
Extraction/Preparation method:

Solvent extraction (A0BZR)
Additional extraction description:

aceton
Substance:

labdane diterpenes (RF-00004392-PAR)
Additional substance description:

Leonurun
Analytical method code:

Nuclear Magnetic Resonance (NMR) (F061A)
Yes/No Qualitative:

Positive/Present (POS)
Result type:

Qualitative Value (Binary) (BIN)
Internal remarks:

Labdane diterpenes

Composition #6: Obikeze, Kene C., McKenzie, Jean M., Green, Ivan R., Mugabo, Pierre. Characterization and Cardiovascular Effects of (13S)-9 alpha, 13 alpha-epoxylabda-6 beta(19), 15(14)diol Dilactone, a Diterpenoid Isolated from Leonotis leonurus . south african journal of chemistry-suid-afrikaanse tydskrif vir chemie, 2008, vol. 61, p. 119–122. .

Language:

English (en)
Plant part:

Leaves (as part-nature) (A0EKT)
Extraction/Preparation method:

Solvent extraction (A0BZR)
Additional extraction description:

methanol
Substance:

diterpene lactones (RF-00004306-PAR)
Additional substance description:

(13S)-9α,13α-epoxylabda-6β(19),15(14)diol dilactone
Analytical method code:

Nuclear Magnetic Resonance (NMR) (F061A)
Yes/No Qualitative:

Positive/Present (POS)
Result type:

Qualitative Value (Binary) (BIN)
Internal remarks:

Diterpene lactone

Composition #7: Mnonopi, N., Levendal, R-A., Mzilikazi, N., Frost, C. L. Marrubiin, a constituent of Leonotis leonurus, alleviates diabetic symptoms . phytomedicine, 2012, vol. 19, no. 6, p. 488–493. DOI: 10.1016/j.phymed.2011.12.008. [DOI link]

Language:

English (en)
Plant part:

Unspecified (A07XD)
Extraction/Preparation method:

Solvent extraction (A0BZR)
Additional extraction description:

unspecified
Substance:

labdane diterpenes (RF-00004392-PAR)
Additional substance description:

Marrubiin
Analytical method code:

Unspecified (F598A)
Yes/No Qualitative:

Positive/Present (POS)
Result type:

Qualitative Value (Binary) (BIN)
Internal remarks:

Marrubiin (labdane diterpene)

Composition #8: He, Fang., Lindqvist, Charlotte., Harding, Wayne W. Leonurenones A-C: Labdane diterpenes from Leonotis leonurus. phytochemistry, 2012, vol. 83, p. 168–172. DOI: 10.1016/j.phytochem.2012.07.014. [DOI link]

Language:

English (en)
Plant part:

Leaves (as part-nature) (A0EKT)
Extraction/Preparation method:

Solvent extraction (A0BZR)
Additional extraction description:

water
Substance:

labdane diterpenes (RF-00004392-PAR)
Additional substance description:

Leonurenones A–C
Analytical method code:

Nuclear Magnetic Resonance (NMR) (F061A)
Yes/No Qualitative:

Positive/Present (POS)
Result type:

Qualitative Value (Binary) (BIN)
Internal remarks:

Labdane diterpenes

Composition #9: Wu, Hankui., Li, Jun., Fronczek, Frank R., Ferreira, Daneel., Burandt, Charles L., Jr., Setola, Vincent., Roth, Bryan L., Zjawiony, Jordan K. Labdane Diterpenoids from Leonotis leonurus. phytochemistry, 2013, vol. 91, p. 229–235. DOI: 10.1016/j.phytochem.2012.02.021. [DOI link]

Language:

English (en)
Plant part:

Leaves (as part-nature) (A0EKT)
Extraction/Preparation method:

Solvent extraction (A0BZR)
Additional extraction description:

acetone
Substance:

labdane diterpenes (RF-00004392-PAR)
Additional substance description:

Leoleorin A-J
Analytical method code:

Nuclear Magnetic Resonance (NMR) (F061A)
Yes/No Qualitative:

Positive/Present (POS)
Result type:

Qualitative Value (Binary) (BIN)
Internal remarks:

Labdane diterpenes

Composition #10: Kuchta, K., Volk, R. B., Rauwald, H. W. Stachydrine in Leonurus cardiaca, Leonurus japonicus, Leonotis leonurus: detection and quantification by instrumental HPTLC and H-1-qNMR analyses . pharmazie, 2013, vol. 68, no. 7, p. 534–540. DOI: 10.1691/ph.2013.6527. [DOI link]

Language:

English (en)
Plant part:

Aerial part of plants (as part-nature) (A166F)
Extraction/Preparation method:

Solvent extraction (A0BZR)
Additional extraction description:

water
Substance:

stachydrine (RF-00004062-PAR)
Analytical method code:

Gelpermeation, High Performance Thin Layer Chromatography (HPTLC) (F017A)
Result unit:

Percent (G138A)
Result type:

Numerical Value (VAL)
Value (concentration, content):

13.45
Internal remarks:

Stachydrine

Composition #11: Narukawa, Yuji., Komori, Miyuki., Niimura, Akiko., Noguchi, Hitomi., Kiuchi, Fumiyuki. Two new diterpenoids from Leonotis leonurus R. Br.. journal of natural medicines, 2015, vol. 69, no. 1, p. 130–134. DOI: 10.1007/s11418-014-0868-2. [DOI link]

Language:

English (en)
Plant part:

Aerial part of plants (as part-nature) (A166F)
Extraction/Preparation method:

Solvent extraction (A0BZR)
Additional extraction description:

acetone
Substance:

epoxides (RF-00010829-PAR)
Additional substance description:

14 alpha-hydroxy-9 alpha,13 alpha-epoxylabd-5(6)-en-7-on-16,15-olide
Analytical method code:

Nuclear Magnetic Resonance (NMR) (F061A)
Yes/No Qualitative:

Positive/Present (POS)
Result type:

Qualitative Value (Binary) (BIN)
Internal remarks:

Epoxides

Endpoint study #1: Maphosa, V., Masika, P. J., Adedapo, A. A. Safety evaluation of the aqueous extract of Leonotis leonurus shoots in rats . human & experimental toxicology, 2008, vol. 27, no. 11, p. 837–843. DOI: 10.1177/0960327108099533. [DOI link]

Study relevance:

Human health
Plant part:

Roots and other underground parts (as part-nature) (A067M)
Preparation/Extraction method:

Solvent extraction (A0BZR)
Additional plant/substance description:

water
Type of toxicological test:

acute toxicity (CHD016TT)
Tested organism:

Rat (as animal) (A0CNV)
Strain of test organism:

Wistar (CHD013ST)
Sex:

Female
Route of exposure:

ORAL: FEED (OECD2230PL)
Exposure duration:

10.0
Unit of exposure duration:

Minute (G074A)
Number of organisms dosed:

6
Control groups used:

yes
Endpoint measured:

Concentration level (CHD013EP)
Concentration unit:

Milligrams per kilogram body weight (G225A)
Effect concentration:

1600-3200
Critical effect:

PULMONARY AND CARDIAC (TOX08A)
Target tissue:

Neurologic (TT004A)
Effect description:

Decreased respiratory rate, decreased motor activity, loss of righting reflex, and ataxia; one rat died 9 min after administration
Effect or parameter linked to the endpoint:

mortality (CHD010BE)
Internal remarks:

Acute toxicity

Endpoint study #2: Maphosa, V., Masika, P. J., Adedapo, A. A. Safety evaluation of the aqueous extract of Leonotis leonurus shoots in rats . human & experimental toxicology, 2008, vol. 27, no. 11, p. 837–843. DOI: 10.1177/0960327108099533. [DOI link]

Study relevance:

Human health
Plant part:

Roots and other underground parts (as part-nature) (A067M)
Preparation/Extraction method:

Solvent extraction (A0BZR)
Additional plant/substance description:

water
Type of toxicological test:

short-term toxicity (CHD017TT)
Tested organism:

Rat (as animal) (A0CNV)
Strain of test organism:

Wistar (CHD013ST)
Sex:

Female
Route of exposure:

ORAL: FEED (OECD2230PL)
Exposure duration:

14.0
Unit of exposure duration:

Day (G134A)
Number of organisms dosed:

6
Control groups used:

yes
Endpoint measured:

Concentration level (CHD013EP)
Concentration unit:

Milligrams per kilogram body weight (G225A)
Effect concentration:

1600
Critical effect:

PULMONARY AND CARDIAC (TOX08A)
Target tissue:

respiratory: Lung (TT041A)
Effect description:

Histopathological changes in lungs (hyperplasia of pulmonary arteries possibly resulting in pulmonary hypertension); 13% mortality rate; Changes in biochemical parameters (decrease in the levels of creatinine and urea)
Effect or parameter linked to the endpoint:

mortality (CHD010BE)
Internal remarks:

Short term toxicity (histopathological changes in the lungs, mortality)

Endpoint study #3: Maphosa, V., Masika, P. J., Adedapo, A. A. Safety evaluation of the aqueous extract of Leonotis leonurus shoots in rats . human & experimental toxicology, 2008, vol. 27, no. 11, p. 837–843. DOI: 10.1177/0960327108099533. [DOI link]

Study relevance:

Human health
Plant part:

Roots and other underground parts (as part-nature) (A067M)
Preparation/Extraction method:

Solvent extraction (A0BZR)
Additional plant/substance description:

water
Type of toxicological test:

subchronic (CHD013TT)
Tested organism:

Rat (as animal) (A0CNV)
Strain of test organism:

Wistar (CHD013ST)
Sex:

Female
Route of exposure:

ORAL: FEED (OECD2230PL)
Exposure duration:

35.0
Unit of exposure duration:

Day (G134A)
Number of organisms dosed:

6
Control groups used:

yes
Endpoint measured:

Concentration level (CHD013EP)
Concentration unit:

Milligrams per kilogram body weight (G225A)
Effect concentration:

200
Critical effect:

HEPATOTOXICITY (TOX02A)
Target tissue:

digestive: Liver (TT023A)
Effect description:

Histopathological changes in livers (focal necrosis and mild haemosiderosis); haemosiderosis in the spleen; Haematological changes
Effect or parameter linked to the endpoint:

histopathology non neoplastic (CHD025BE)
Internal remarks:

Subchronic toxicity (hepatotoxicity)

Endpoint study #4: Maphosa, V., Masika, P. J., Adedapo, A. A. Safety evaluation of the aqueous extract of Leonotis leonurus shoots in rats . human & experimental toxicology, 2008, vol. 27, no. 11, p. 837–843. DOI: 10.1177/0960327108099533. [DOI link]

Study relevance:

Human health
Plant part:

Roots and other underground parts (as part-nature) (A067M)
Preparation/Extraction method:

Solvent extraction (A0BZR)
Additional plant/substance description:

water
Type of toxicological test:

short-term toxicity (CHD017TT)
Tested organism:

Rat (as animal) (A0CNV)
Strain of test organism:

Wistar (CHD013ST)
Sex:

Female
Route of exposure:

ORAL: FEED (OECD2230PL)
Exposure duration:

14.0
Unit of exposure duration:

Day (G134A)
Number of organisms dosed:

6
Control groups used:

yes
Endpoint measured:

Concentration level (CHD013EP)
Concentration unit:

Milligrams per kilogram body weight (G225A)
Effect concentration:

1600
Critical effect:

NEPHROTOXICITY (TOX03A)
Target tissue:

urogenital: Kidneys (TT046A)
Effect description:

Histopathological changes in kidneys (glomerular changes suggestive of glomerulonephritis)
Effect or parameter linked to the endpoint:

histopathology non neoplastic (CHD025BE)
Internal remarks:

Short term toxicity (histopathological changes in the kidneys)

Endpoint study #5: Oyedemi, S. O., Yakubu, M. T., Afolayan, A. J. Effect of aqueous extract of Leonotis leonurus (L.) R. Br. leaves in male Wistar rats . human & experimental toxicology, 2010, vol. 29, no. 5, p. 377–384. DOI: 10.1177/0960327110363864. [DOI link]

Study relevance:

Human health
Plant part:

Leaves (as part-nature) (A0EKT)
Preparation/Extraction method:

Solvent extraction (A0BZR)
Additional plant/substance description:

water
Type of toxicological test:

short-term toxicity (CHD017TT)
Tested organism:

Rat (as animal) (A0CNV)
Strain of test organism:

Wistar (CHD013ST)
Sex:

Male
Route of exposure:

ORAL: UNSPECIFIED (OECD2234PL)
Exposure duration:

21.0
Unit of exposure duration:

Day (G134A)
Number of organisms dosed:

5
Control groups used:

yes
Endpoint measured:

Concentration level (CHD013EP)
Concentration unit:

Milligrams per kilogram body weight per day (G211A)
Effect concentration:

125-500
Critical effect:

HEMOPOIETIC (TOX10A)
Target tissue:

Cardiovascular / Haematological (TT001A)
Effect description:

Haematological changes (decreased the levels of lymphocytes, eosinophils and monocytes of the animals, the neutrophil levels increased)
Effect or parameter linked to the endpoint:

haematology (CHD023BE)
Internal remarks:

Hematological changes

Endpoint study #6: Oyedemi, S. O., Yakubu, M. T., Afolayan, A. J. Effect of aqueous extract of Leonotis leonurus (L.) R. Br. leaves in male Wistar rats . human & experimental toxicology, 2010, vol. 29, no. 5, p. 377–384. DOI: 10.1177/0960327110363864. [DOI link]

Study relevance:

Human health
Plant part:

Leaves (as part-nature) (A0EKT)
Preparation/Extraction method:

Solvent extraction (A0BZR)
Additional plant/substance description:

water
Type of toxicological test:

short-term toxicity (CHD017TT)
Tested organism:

Rat (as animal) (A0CNV)
Strain of test organism:

Wistar (CHD013ST)
Sex:

Male
Route of exposure:

ORAL: UNSPECIFIED (OECD2234PL)
Exposure duration:

21.0
Unit of exposure duration:

Day (G134A)
Number of organisms dosed:

5
Control groups used:

yes
Endpoint measured:

Concentration level (CHD013EP)
Concentration unit:

Milligrams per kilogram body weight per day (G211A)
Effect concentration:

125-500
Critical effect:

NEPHROTOXICITY (TOX03A)
Target tissue:

urogenital: Kidneys (TT046A)
Effect description:

Kidney functional alterations (kidney body weight ratio increased)
Effect or parameter linked to the endpoint:

other (CHD003BE)
Internal remarks:

Nephrotoxicity

Endpoint study #7: Oyedemi, S. O., Yakubu, M. T., Afolayan, A. J. Effect of aqueous extract of Leonotis leonurus (L.) R. Br. leaves in male Wistar rats . human & experimental toxicology, 2010, vol. 29, no. 5, p. 377–384. DOI: 10.1177/0960327110363864. [DOI link]

Study relevance:

Human health
Plant part:

Leaves (as part-nature) (A0EKT)
Preparation/Extraction method:

Solvent extraction (A0BZR)
Additional plant/substance description:

water
Type of toxicological test:

short-term toxicity (CHD017TT)
Tested organism:

Rat (as animal) (A0CNV)
Strain of test organism:

Wistar (CHD013ST)
Sex:

Male
Route of exposure:

ORAL: UNSPECIFIED (OECD2234PL)
Exposure duration:

21.0
Unit of exposure duration:

Day (G134A)
Number of organisms dosed:

5
Control groups used:

yes
Endpoint measured:

Concentration level (CHD013EP)
Concentration unit:

Milligrams per kilogram body weight per day (G211A)
Effect concentration:

125-500
Critical effect:

HEPATOTOXICITY (TOX02A)
Target tissue:

digestive: Liver (TT023A)
Effect description:

Liver functional alterations (liver body weight ratio increased)
Effect or parameter linked to the endpoint:

other (CHD003BE)
Internal remarks:

Hepatotoxicity