全 文 ： 230 Chin J Nat Med May 2012 Vol. 10 No. 3 2012 年 5 月 第 10 卷 第 3 期

Chinese Journal of Natural Medicines 2012, 10(3): 0230−0233
doi: 10.3724/SP.J.1009.2012.00230
Chinese
Journal of
Natural
Medicines







Cytotoxic sesquiterpene lactones from Vernonia bockiana
LIAO Shang-Gao, WANG Zhen, LI Jing, LIU Ying, LI Yue-Ting, ZHANG Li-Juan,
LONG Qing-De, WANG Yong-Lin *
Provincial Key Laboratory of Pharmaceutics in Guizhou Province, School of Pharmacy, Guiyang Medical University, Guiyang 550004,
China
Available online 20 May 2012
[ABSTRACT] AIM: To investigate antitumor compounds from Vernonia bockiana. METHODS: The compounds were isolated by
column chromatography and preparative HPLC. Their structures were elucidated by 1H and 13C NMR spectroscopic methods and MS
experiments. The antitumor activity was evaluated by testing their cytotoxicity against the human promyelomonocyte leukemic cell line
HL-60 by the MTT method. RESULTS: Six sesquiterpene lactones, 8α-(4-hydroxymethacryloyloxy)-10α-hydroxy-13-me-
thoxyhirsutinolide (1), 8α-methacryloyloxy-10α-hydroxy-13-O-methylhirsutinolide (2), piptocarphin A (3), 8α-[4-hydroxymethacry-
loyloxy]-10α-hydroxyhisutinolide-13-O-acetate (4), piptocarphin F (5), and 8α-acetoxy-10α-hydroxy-13-O-methylhirsutinolide (6), and
one known inone glycoside, saussureosides B (7), were isolated from the whole plant of V. bockiana. The six sesquiterpene lactones
showed cytotoxic activity (IC50 3.87–12.5 μmol·L-1) against the human leukemic cell line HL-60 while the inone glycoside 7 was
inactive in the test. CONCLUSION: Compounds 1, 2, 6, and 7 were obtained for the first time from this plant; The sesquiterpene
lactones present in V. bockiana were active as antitumor agents against the human leukemic cell line HL-60.
[KEY WORDS] Vernonia bockiana; Compositae; Sesquiterpene lactone; Anti-tumor activity
[CLC Number] R284; R965 [Document code] A [Article ID] 1672-3651(2012)03-0230-04

1 Introduction
Most of the Chinese medicinal plants of the genus
Vernonia (Compositae) have been used in the folk medicines
to eradicate worms and for the treatment of malaria, bruises,
and rheumatism [1]. Chemical and pharmacological investiga-
tions have shown that the sesquiterpene lactones present in
these plants possessed anti-tumor activities, and some of
these sesquiterpene lactones exhibited strong cytotoxicity
against tumor cell lines such as mouse lymphoid tumor cell
line P388, human leukemic cell line HL-60, and human
breast carcinoma line MCF-7 [1-2]. V. bockiana is a perennial

[Received on] 09-Oct.-2011
[Research funding] This project was supported by the Science and
Technology Department of Guizhou Province (Nos. J2008-2139,
2009-4001), Guiyang Medical College (No. C-2007-7), Guiyang
Municipal Science and Technology Bureau of China (No. 20099304),
and by Program of the Ministry of Education for Construction of the
Engineering Research Center for TCM and Ethnic Medicines.
[*Corresponding author] WANG Yong-Lin: Prof., Tel/Fax: 86-851-
6908899, E-mail: ylwang_gmc@163.com
These authors have no any conflict of interest to declare.
herb (Compositae) distributed mainly in Southwest China [3].
In the previous study, we isolated seven sesquiterpene lac-
tones cytotoxic against P388 from the aerial parts of V.
bockiana [4-5]. As a continuation of the project aiming at the
antitumor agents, the whole plants of V. bockiana have been
reinvestigated. As a result, six sesquiterpene lactones and one
inone glycoside (Fig. 1) have been isolated. Cytotoxic activ-
ity evaluation showed that all the sesquiterpene lactones pos-
sessed cytotoxic activities against the human promyelo-
monocyte leukemic cell line HL-60.

Fig. 1 Structures of compounds 1–7
LIAO Shang-Gao, et al. /Chinese Journal of Natural Medicines 2012, 10 (3): 230−233
2012 年 5 月 第 10 卷 第 3 期 Chin J Nat Med May 2012 Vol. 10 No. 3 231

2 Experimental
2.1 General experimental procedures
Semi-preparative HPLC: Agilent-1100 MWD; Hedera-
C18 column (ODS-2, 250 mm × 30.0 mm, 5 μm). UV: Shi-
madzu UV-2401PC. Optical rotations: Rudolph Autopol II.
IR: Bruker Vector-22. NMR: Bruker AM-400 spectrometer
with TMS as an internal standard. ESI-MS: Waters
ACQUITY UPLC-TQD. All solvents used for separation
were of analytical grade (Shanghai Chemical Plant). Silica
gel (200–300 mesh), silica gel H, D-101 macroporous ab-
sorption resin, and MCI gel (CHP20P, 75–150 μm, Mitsubi-
shi Chemical Industries Ltd.) were used for column chroma-
tography. Pre-coated silica gel GF254 plates (Qingdao Marine
Chemical Plant, Qingdao, China) were used for TLC. The
following materials and reagents were used for cell culture
and assay of cytotoxic activity: microplate reader (model 680;
Bio-Rad); 96-well flat-bottom microplate (Costar, NY, USA);
HL-60 cells (The Key Laboratory of Chemistry for Natural
Products of Guizhou Province and Chinese Academy of Sci-
ences); RPMI 1640 medium, GIBCO BRL (Gland Island, NY,
USA); MTT, Sigma (St. Louis, MO, USA). All other chemi-
cals used were of biochemical reagent grade.
2.2 Plant material
V. bockiana Diels (Compositae) was collected from
Guizhou Province, China in July 2010, and authenticated by
one of the authors, Prof. LONG Qin-De (Guiyang Medical
College). A voucher specimen (No. VB20100725) was de-
posited at the School of Pharmacy, Guiyang Medical College,
China.
2.3 Extraction and isolation
The dried whole plants of V. bockiana (11 kg) were
coarsely powdered and extracted with 92% a.q. EtOH (55 L)
two times (10 days for the first time and 4 days for the sec-
ond). After filtration and removal of the solvent under re-
duced pressure, the residue (800 g) was transferred to D101
macroporous resin column chromatography (CC) eluted with
85% a.q. EtOH. Solvent of the 85% EtOH fraction was re-
moved under reduced pressure and the residue was suspended
in water, and then partitioned successively with EtOAc and
n-BuOH to give an EtOAc-soluble extract (315.5 g) and an
n-BuOH-soluble extract (231.5 g). The EtOAc-soluble ex-
tract was subjected to MCI CC eluted with a gradient of a.q.
MeOH (30%–90%) to give three fractions, E1–E3. Fraction
E2 (45.3 g) was further separated by silica gel CC gradiently
eluted with petroleum ether-EtOAc (3 : 1–1 : 2) to yield 5
sub-fractions (E2a–E2e). Fraction E2c (3.9 g) was further
separated by silica gel CC eluted with a gradient of petroleum
ether-Me2CO (7 : 1–1 : 2) to afford four fractions,
E2c1–E2c4. Purification of fraction E2c1 by silica gel CC
eluted with CHCl3 afforded fraction E2c1a, which was then
purified by semi-preparative HPLC eluted with 75% a.q.
MeOH to yield 2 (20 mg). E2c2 was separated by silica gel
CC eluted with CHCl3 to give fraction E2c2a, further purifi-
cation of which by semi-preparative HPLC eluted with 75%
a.q. MeOH yielded 3 (27 mg). Separation of E2c3 by silica
gel CC eluted with CHCl3 gave a new fraction, E2c3a,
semi-preparative HPLC of which eluted with 70% a.q.
MeOH afforded 4 (30 mg). Separation of fraction E2c4 by
semi-preparative HPLC eluted with 72% a.q. MeOH gave 6
(15 mg). Purification of fraction E2d by semi-preparative
HPLC eluted with 70% a.q. MeOH afforded compound 1 (3.5
mg), while that of fraction E2e by Sephadex LH-20 CC
(MeOH) yielded 5 (50 mg). Successive separation of the
n-BuOH-soluble extract by MCI CC (10%–60% a.q. MeOH),
Sephadex LH-20 (MeOH), silica gel CC (CHCl3-MeOH 5 : 1)
and semi-preparative HPLC (15% a.q. MeOH) afforded 7
(7.9 mg).
2.4 Identification
Compound 1 Amorphous powder. ESI-MS m/z 409 [M
– H]–, 433 [M + Na]+, 393 [M + H – H2O]+. 1H NMR (400
MHz, CDCl3) δ: 6.67 (1H, d, J = 10.8 Hz, H-8), 6.38 (1H, br
s, H-3′a), 5.86 (1H, br s, H-5), 5.82 (1H, br s, H-3′b), 4.53
(1H, d, J = 11.2 Hz, H-13a), 4.39 (1H, br d, J = 12.8 Hz,
H-4′a), 4.29 (1H, d, J = 12.0 Hz, H-13b), 4.21 (1H, br d, J =
13.6 Hz, H-4′b), 3.42 (3H, s, -OCH3), 2.65 (1H, dd, J = 15.6,
11.2 Hz, H-9a), 2.35-2.47 (1H, m, H-3a), 2.13 (1H, br d, J =
17.6 Hz, H-9b), 1.93-2.10 (2H, m, H2-2), 1.83-1.90 (1H, m,
H-3b), 1.59 (3H, s, H-15), 1.21 (3H, s, H-14); 13C NMR (100
MHz, CDCl3) δ: 167.5 (C-12), 165.0 (C-1′), 150.5 (C-7),
144.0 (C-6), 139.0 (C-2′), 133.0 (C-11), 129.4 (C-3′), 125.3
(C-5), 110.0 (C-1), 82.5 (C-4), 77.5 (C-10), 65.3 (C-8), 63.5
(C-13), 62.5 (C-4′), 58.5 (-OCH3), 38.0 (C-9), 37.8 (C-3),
32.0 (C-2), 28.7 (C-15), 26.0 (C-14). Compound 1 was char-
acterized as 8α-(4-hydroxymethacryloyloxy)-10α- hy-
droxy-13-methoxyhirsutinolide by comparison of the spectral
data with those reported in the literature [6].
Compound 2 Amorphous powder. ESI-MS m/z 395 [M
+ H]+, 393 [M – H]–. 1H NMR (400 MHz, CDCl3) δ: 6.57
(1H, d, J = 10.4 Hz, H-8), 6.29 (1H, s, H-3′a), 5.85 (1H, s,
H-5), 5.69 (1H, s, H-3′b), 4.59 (1H, d, J = 11.8 Hz, H-13a),
4.27 (1H, d, J = 11.8 Hz, H-13b), 4.15 (br s, -OH), 3.85 (br s,
-OH), 3.44 (3H, s, -OCH3), 2.60 (1H, dd, J = 15.2, 12.0 Hz,
H-9a), 2.44 (1H, dt, J = 12.0, 7.2 Hz, H-2), 2.11 (1H, br d, J
= 15.6 Hz, H-9b), 1.95 (3H, s, H-4′), 1.80-1.90 (m, H-2), 1.57
(3H, s, H-14), 1.22 (3H, s, H-15); 13C NMR (100 MHz,
CDCl3) δ: 167.6 (C-12), 165.9 (C-1′), 150.5 (C-6), 144.1
(C-7), 135.9 (C-2′), 133.2 (C-11), 127.3 (C-3′), 125.9 (C-5),
108.7 (C-1), 82.1 (C-4), 77.5 (C-10), 66.3 (C-8), 63.7 (C-13),
59.1 (-OCH3), 38.1 (C-9), 37.8 (C-2), 31.8 (C-3), 29.7 (C-15),
25.6 (C-14), 18.2 (C-4′). Compound 2 was characterized as
8α-methacryloyloxy-10α-hydroxy-13-O-methylhirsutinolide
by comparison of the spectral data with those reported in the
literature [7].
Compound 3 Amorphous powder. ESI-MS m/z 423 [M
+ H]+, 421 [M – H]–. 1H NMR (400 MHz, CDCl3) δ: 6.60
(1H, d, J = 9.2 Hz, H-8), 6.29 (1H, s, H-3′a), 5.91 (1H, s,
LIAO Shang-Gao, et al. /Chinese Journal of Natural Medicines 2012, 10 (3): 230−233
232 Chin J Nat Med May 2012 Vol. 10 No. 3 2012 年 5 月 第 10 卷 第 3 期

H-5), 5.70 (1H, s, H-3′b), 5.32 (1H, d, J = 12.4 Hz, H-13a),
4.90 (1H, d, J = 12.8 Hz, H-13b), 4.14 (s, -OH), 3.86 (s, -OH),
2.63 (1H, dd, J = 13.6, 12.8 Hz, H-9a), 2.45 (1H, dt, J = 12.8,
11.6 Hz, H-2), 2.10 (1H, m, H-9b), 2.08 (3H, s, -OOCCH3),
1.95 (3H, s, H-4′), 1.58 (3H, s, H-15), 1.24 (3H, s, H-14); 13C
NMR (100 MHz, CDCl3) δ: 170.2 (-OOCCH3), 166.5 (C-12),
165.4 (C-1′), 149.3 (C-6), 143.7 (C-7), 135.5 (C-2′), 130.8
(C-11), 127.0 (C-3′), 126.3 (C-5), 108.0 (C-1), 82.1 (C-4),
77.4 (C-10), 65.9 (C-8), 55.2 (C-13), 37.9 (C-9), 37.1 (C-2),
32.1 (C-3), 28.9 (C-15), 25.2 (C-14), 20.5 (-OOCCH3), 17.7
(C-4). Compound 3 was characterized as piptocarphin A by
comparison of the spectral data with those reported in the
literature [8].
Compound 4 Amorphous powder. ESI-MS m/z 439 [M
+ H]+, 437 [M – H]–. 1H NMR (400 MHz, CD3OD) δ: 6.33
(1H, br s, H-3′a), 6.19 (1H, s, H-5), 5.93 (1H, br s, H-3′b),
4.89 (1H, d, J = 11.0 Hz, H-13a), 4.87 (1H, d, J = 11.0 Hz,
H-13b), 4.29 (1H, brd, J = 13.5 Hz, H-4′a), 4.23 (1H, br d, J
= 14.0 Hz, H-4′b), 2.48 (1H, dd, J = 14.7, 5.5 Hz, H-9a), 2.14
(1H, br d, J = 15.0 Hz, H-9b), 2.04 (3H, br s, -OOCCH3),
1.46 (3H, s, H-15), 1.18 (3H, s, H-14); 13C NMR (100 MHz,
CD3OD) δ: 167.7 (C-12), 165.2 (C-1′), 139.9 (C-2′), 130.2
(C-11), 125.6 (C-3′), 125.4 (C-5), 108.6 (C-1), 82.5 (C-4),
77.3 (C-10), 68.8 (C-4′), 66.6 (C-8), 55.4 (C-13), 43.1
(-OCH2CH3), 38.9 (C-9), 38.5 (C-2), 34.7 (C-3), 29.8 (C-15),
24.8 (C-14), 19.1 (-OCH2CH3). Compound 4 was charac-
terized as 8α-[4-hydroxymethacryloyloxy]-10α-hydroxyhisu-
tinolide-13-O-acetate by comparison of the spectral data with
those reported in the literature [9].
Compound 5 Amorphous powder. ESI-MS m/z 425 [M
+ H]+, 423 [M – H]–. 1H NMR (400 MHz, CDCl3) δ: 6.58
(1H, d, J = 9.5 Hz, H-8), 6.27 (1H, m, H-3′a), 5.82 (1H, s,
H-5), 5.66 (1H, s, H-3′b), 4.58 (1H, d, J = 12.2 Hz, H-13a),
4.30 (1H, d, J = 12.2 Hz, H-13b), 4.07 (1H, br s, OH), 3.77
(1H, br s, OH), 3.57 (2H, q, J = 7.0 Hz, -OCH2CH3),
1.90–2.75 (6H, m, H2-9, H2-3, H2-2), 1.93 (3H, m, H-4′),
1.55 (3H, s, H-15), 1.23 (3H, s, H-14), 1.21 (3H, t, J = 7.0 Hz,
-OCH2CH3); 13C NMR (100 MHz, CDCl3) δ: 167.6 (C-12),
165.9 (C-1′), 139.9 (C-2′), 130.2 (C-11), 125.6 (C-3′), 125.4
(C-5), 109.6 (C-1), 82.5 (C-4), 77.3 (C-10), 66.6 (C-8), 55.4
(C-13), 43.1 (-OCH2CH3), 38.9 (C-9), 38.5 (C-2), 34.7 (C-3),
29.8 (C-15), 24.8 (C-14), 19.1 (-OCH2CH3), 18.8 (C-4′).
Compound 5 was characterized as piptocarphin F by com-
parison of the spectral data with those reported in the litera-
ture [8].
Compound 6 Amorphous powder. ESI-MS m/z 367 [M
– H]–, 391 [M + Na]+. 1H NMR (400 MHz, CDCl3) δ: 6.43
(1H, br s, H-8), 5.87 (1H, br s, H-5), 4.49 (1H, d, J = 11.2 Hz,
H-13a), 4.24 (1H, d, J = 11.6 Hz, H-13b), 4.07 (br s, -OH),
3.96 (br s, -OH), 3.39 (3H, s, -OCH3), 2.53 (1H, m, H-9a),
2.40 (1H, dd, J = 12.0, 11.6 Hz, H-2a), 2.15 (1H, m, H-9b),
2.11 (3H, s, -OAc), 1.70-1.95 (1H, m, H-2b), 1.58 (3H, s,
H-14), 1.23 (3H, s, H-15); 13C NMR (100 MHz, CDCl3) δ:
169.5 (C-1′), 167.7 (C-12), 150.5 (C-6), 144.2 (C-7), 133.2
(C-11), 125.8 (C-5), 108.5 (C-1), 82.0 (C-4), 76.8 (C-10),
66.7 (C-8), 63.4 (C-13), 59.0 (-OCH3), 38.1 (C-9), 37.7 (C-2),
31.4 (C-3), 29.7 (C-15), 25.4 (C-14), 21.1(C-2′). Compound
6 was characterized as 8α-acetoxy-10α-hydroxy-13-O-me-
thylhirsutinolide by comparison of the spectral data with
those reported in the literature [7].
Compound 7 Amorphous powder. ESI-MS m/z 385 [M
– H]–, 431 [M + HCOO]–. 1H NMR (400 MHz, CD3OD) δ:
7.26 (1H, d, J = 16.4 Hz, H-7), 6.13 (1H, d, J = 16.4 Hz, H-8),
4.50 (1H, d, J = 7.6 Hz, H-1′), 4.11 (1H, d, J = 2.8 Hz, H-4),
4.00 (1H, ddd, J = 12.8, 3.4, 3.0 Hz, H-3), 3.85 (1H, d, J =
11.6 Hz, H-6′a), 3.66 (1H, dd, J = 11.2, 3.6 Hz, H-6′b), 3.50
(1H, m, H-3′), 3.40 (1H, m, H-2′), 3.36 (1H, m, H-5′), 3.25
(1H, dd, J = 8.8, 8.0 Hz, H-4′), 2.31 (3H, s, H-10), 1.93 (1H,
d, J = 12.4 Hz, H-2β), 1.88 (3H, s, H-11), 1.63 (1H, dd, J =
12.4, 2.8 Hz, H-2α), 1.14 (3H, s, H-12), 1.09 (3H, s, H-13);
13C NMR (100 MHz, CD3OD) δ: 201.2 (C-9), 144.5 (C-7),
141.5 (C-6), 135.0 (C-8), 132.7 (C-5), 103.2 (C-1′), 78.5
(C-5′), 78.4 (C-3′), 76.1 (C-4), 75.7 (C-2′), 72.0 (C-4′), 70.4
(C-3), 63.1 (C-6′), 40.5 (C-2), 38.3 (C-1), 30.6 (C-13), 28.2
(C-12), 27.6 (C-10), 20.4 (C-11). Compound 7 was charac-
terized as saussureosides B by comparison of the spectral
data with those reported in the literature [10].
2.5 Cytotoxicity assay
The assays were performed using the MTT method [11].
Doxorubicin was used as a positive control with IC50 value of
0.24 μmol·L-1 against the HL-60 cell line.
3 Results and Discussion
The compounds isolated from V. bockiana were identi-
fied as six sesquiterpene lactones (1–6) and one inone glyco-
side (7) by comparing their spectral data to those reported in
the literature. Among these compounds, compounds 1, 2, 4, 6,
and 7 were obtained from this plant for the first time.
All of the compounds isolated were evaluated for their
cytotoxic effects. All the six sesquiterpene lactones (1–6)
showed cytotoxicity (IC50 3.87–12.5 μmol·mL-1) against the
human promyelomonocyte leukemic cell line HL-60 (Table
1). Since the cytotoxic activity of compounds 1 and 4 were
weaker than their respective 4′-deoxyproducts 2 and 3, intro-
duction of a hydroxyl to C-4′ seems to be detrimental to the
cytotoxicity.
Table 1 Cytotoxicity of the compounds against human
promyelomonocyte leukemic cell line HL-60
Compounds
1 2 3 4 5 6 7 Doxorubicin
IC50
/(μmol·L–1) 12.5 5.69 3.87 5.69 5.69 5.96 >100 0.24
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南川斑鸠菊中的抗肿瘤倍半萜内酯
廖尚高, 王 珍, 李 靖, 刘 影, 李月婷, 张丽娟, 龙庆德, 王永林*
贵阳医学院药学院贵州省药物制剂重点实验室, 贵阳 550004
【摘 要】 目的：研究南川斑鸠菊中的抗肿瘤活性成分 方法：采用层析柱和制备高效液相进行化合物分离, 运用 1H 和 13C
NMR 及 MS 等波谱分析技术鉴定化合物结构; 采用 MTT 法进行 7 个化合物对人骨髓白血病细胞(HL-60)的体外细胞毒实验。
结果：分离得到 6 个倍半萜内酯 [8α-(4-hydroxymethacryloyloxy)-10α-hydroxy-13-methoxyhirsutinolide (1), 8α-methacry-
loyloxy-10α-hydroxy-13-O-methylhirsutinolide (2), piptocarphin A (3), 8α-[4-hydroxymethacryloyloxy]-10α-hydroxyhisutinolide-13-
O-acetate (4), piptocarphin F (5)以及 8α-acetoxy-10α-hydroxy-13-O-methylhirsutinolide (6)]和 1 个 inone 苷 saussureosides B (7); 6
个倍半萜内酯(1–6)具有抑制人骨髓白血病细胞(HL-60)的活性(IC50 3.87–12.5 μmol·L-1), 但 inone 苷 saussureosides B (7) 对 HL-60
没有抑制活性。结论：化合物 1, 2, 6 和 7 首次从该植物中得到; 南川斑鸠菊中的倍半萜内酯类化合物具有抗肿瘤活性。
【关键词】 南川斑鸠菊; 菊科; 倍半萜内酯; 抗肿瘤活性

【基金项目】 贵州省科技厅项目(Nos. J2008-2139, 2009-4001), 贵阳医学院博士基金(No. C-2007-7), 贵阳市科技局项目(No.
20099304), 教育部民族药、中药工程研究中心建设项目