Potential lipase inhibitors from Chinese medicinal herbs

Figures & data

Table 1. PPL inhibitory activities of various Chinese medicinal herbs.

No	Scientific name	Plant part	Family	Inhibition%
1	Atractylodes macrocephala Koidz	Rhizome	Compositae	11.0 ± 0.7
2	Panax notoginseng (Burk) F.H.Chen	Root	Araliaceae	58.1 ± 0.5
3	Pueraria lobata (Willd.) Ohwi	Root	Leguminosae	7.4 ± 1.1
4	Salvia miltiorrhiza Bunge	Root	Labiatae	12.4 ± 0.3
5	Alisma plantago-aquatica Linn	Tuber	Alismataceae	12.3 ± 0.5
6	Phellodendron chinense Schneid	bark	Rutaceae	11.5 ± 0.8
7	Rubia cordifolia L.	Root	Rubiaceae	5.7 ± 1.2
8	Paeonia lactiflora Pall.	Root	Ranunculaceae	14.4 ± 0.4
9	Astragalus membranaceus (Fisch) Bge. var. mongholicus (Bge.) Hsiao	Root	Leguminosae	5.2 ± 1.1
10	Ligusticum chuanxiong Hort.	Rhizome	Umbelliferae	1.1 ± 0.3
11	Acorus tatarinowii	Rhizome	Araceae	13.6 ± 0.7
12	Liquidambar formosana Hance	Ripe fruit	Hamamelidaceae	12.6 ± 0.5
13	Gleditsia sinensis Lain.	Spines	Leguminosae	10.0 ± 1.4
14	Eugenia caryophyllata Thunb.	Bud	Myrtaceae	16.4 ± 0.9
15	Clinopodium polycephalum (Vaniot) C. Y. Wu et Hsuan	Aboveground	Labiatae	5.7 ± 0.7
16	Trichosanthes kiriowii Maxim.	Ripe fruit	Cucurbitaceae	3.8 ± 0.8
17	Allium macrostemon Bge.	Bulbs	Liliaceae	6.4 ± 1.6
18	Arnebia euchroma (Royle) Johnst.	Root	Boraginaceae	28.3 ± 0.8
19	Erigeron breviscapus (Vant.) Hand.-Mazz	The whole plant	Compositae	2.2 ± 0.4
20	Glycyrrhiza uralensis Fisch.	Root	Leguminosae	9.5 ± 1.1
21	Citrus aurantium L.	Young fruit	Rutaceae	12.5 ± 1.4
22	Epimedium brevicornu Maxim.	leaf	Berberidaceae	12.2 ± 1.7
23	Prunus persica (L.)Batsch	Mature seeds	Rosaceae	28.7 ± 1.4
24	Eucommia ulmoides Oliv.	Bark	Eucommiaceae	8.6 ± 0.8
25	Curculigo orchioides Gaertn.	Rhizome	Amaryllidaceae	16.0 ± 0.9
26	Magnolia officinalis Rehd. et Wils	Bark	Magnoliaceae	44.2 ± 1.2
27	Corydalis yanhusuo W. T. Wang ex Z. Y. Su et C. Y. Wu	Tubers	Papaveraceae	9.1 ± 1.5
28	Carthamus tinctorius L.	Flower	Compositae	14.7 ± 0.5
29	Ligustrum lucidum Ait.	Fruit	Oleaceae	18.6 ± 1.3
30	Cistanche deserticola Ma	Stems	Orobanchaceae	16.0 ± 1.4
31	Eclipta prostrata (L.) L.	The whole plant	Compositae	9.7 ± 0.1
32	Angelica sinensis (Oliv.) Diels	Root	Umbelliferae	4.4 ± 0.4
33	Paeonia suffruticosa Andr.	Root bark	Ranunculaceae	20.4 ± 1.1
34	Dipsacus asperoides C. Y. Cheng et T. M. Ai	Root	Dipsacaceae	15.6 ± 1.8
35	Evodia rutaecarpa (Juss.) Benth.	Fruit	Rutaceae	17.7 ± 0.5

Three measurements were carried out per elution. Data were expressed as an average ± standard deviation (n = 3). The final concentration of the elutions used in the screening was 200 μg/mL.

Figure 1. PPL inhibitory activities of 22 sub-fractions from Panax notoginseng and Magnolia officinalis. Three measurements were carried out per sub-fraction. Data were expressed as an average ± standard deviation (n = 3). The final concentration of the sub-fractions was 200 μg/mL.

Figure 2. PPL inhibitory activity of 20(S)-ginsenoside Rg3. (a) Chromatograms of (A) reference substance 20(S)-ginsenoside Rg3, (B) mixture sub-fraction PN-17 including (1) ginsenoside Rh4, (2) 20(S)-ginsenoside Rg3, (3) 20(R)-ginsenoside Rg3 at 210 nm. (b) PPL inhibitory activity of three compound components of PN-17. The final concentration of three compound components was 50 μg/mL. (c) Concentration dependent inhibition of PPL by 20(S)-ginsenoside Rg3. The inhibition rate was plotted against the log of the cumulative doses of 20(S)-ginsenoside Rg3 (Mean ± SD, n = 3).

Figure 3. PPL inhibitory activity of honokiol. (a) Chromatograms of (A) reference substance honokiol, (B) sub-fraction MO-19 at 230 nm. (b) The structure of honokiol. (c) Concentration dependent inhibition of PPL by honokiol. The inhibition rate was plotted against the log of the cumulative doses of honokiol (Mean ± SD, n = 3).

Table 2. ESI mass analysis of PN-17-2 and MO-19.

				Molecular ions, m/z
Identified compounds	TR/min	Molecular formula	Molecular weight	(+)	(−)
PN-17-2	28.56	C42H72O13	784.49	807.48[M + Na]^+ 767.49[M + H-H2O]^+ 749.48[M + H-2H2O]^+	897.48[M + TFA-H]^− 829.49[M + HCOOH-H]^– 783.49[M-H]^−
MO-19	56.09	C18H18O2	266.14	267.14[M + H]^+ 284.16[M + NH4]^+ 289.12[M + Na]^+	265.14[M-H]^−