GORAKH MUNDI

In vitro antioxidant studies of Sphaeranthus indicus (Linn).

Shirwaikar A, Prabhu KS, Punitha IS.

Department of Pharmacognosy, Manipal College of Pharmaceutical Sciences, Manipal 576 104, India.
annieshirwaikar@yahoo.com

Abstract

The free radical scavenging potential of the plant S. indicus was studied by using different antioxidant
models of screening. The ethanolic extract at 1000 microg/ml showed maximum scavenging of the
radical cation, 2,2-azinobis-(3-ethylbenzothiazoline-6-sulphonate) (ABTS) observed upto 41.99%
followed by the scavenging of the stable radical 1,1-diphenyl, 2-picryl hydrazyl (DPPH) (33.27%),
superoxide dismutase (25.14%) and nitric oxide radical (22.36%) at the same concentration. However,
the extract showed only moderate scavenging activity of iron chelation (14.2%). Total antioxidant
capacity of the extract was found to be 160.85 nmol/g ascorbic acid. The results justify the therapeutic
applications of the plant in the indigenous system of medicine, augmenting its therapeutic value.

PMID: 17176673 [PubMed - indexed for MEDLINE]

Immunomodulatory activity of petroleum ether extract of flower heads of Sphaeranthus indicus Linn.

Bafna AR, Mishra SH.

Pharmacy Department, Faculty of Technology and Engineering, M.S. University of Baroda, Vadodara,
Gujarat, India.

Abstract

The petroleum ether extract from the flower heads of Sphaeranthus indicus Linn. was found to be
effective in increasing phagocytic activity, hemagglutination antibody titer and delayed type
hypersensitivity when tested in mice. Activity of the petroleum extract was tested at five different
dosing levels to establish a dose-response relationship. It was found that 200 mg/kg dose was the
optimum dose, and at higher doses the activity was either reduced or showed no further increase. The
present study, therefore, reveals that the drug shows good promise as an immunomodulatory agent,
which acts by stimulating both humoral and cellular immunity as well as phagocytic function.

PMID: 17594985 [PubMed - indexed for MEDLINE]

7-hydroxyfrullanolide, a sesquiterpene lactone, inhibits pro-inflammatory cytokine production from
immune cells and is orally efficacious in animal models of inflammation.

Fonseca LC, Dadarkar SS, Lobo AS, Suthar AC, Chauhan VS, Chandrababu S, Sharma SD, Dagia NM,
Padigaru M. The Department of Pharmacology, Piramal Life Sciences Limited, Mumbai-400063,
Maharashtra, India.

Abstract

A promising therapeutic approach to reduce pathological inflammation is to inhibit the increased

production of pro-inflammatory cytokines (e.g., TNF-alpha, IL-6). In this study, we investigated the anti-
inflammatory potential of 7-hydroxyfrullanolide (7HF). 7HF is an orally bioavailable, small molecule
sesquiterpene lactone isolated from the fruit of Sphaeranthus indicus. 7HF significantly and dose-
dependently diminished induced and spontaneous production of TNF-alpha and IL-6 from freshly
isolated human mononuclear cells, synovial tissue cells isolated from patients with active rheumatoid
arthritis and BALB/c mice. Oral administration of 7HF significantly protected C57BL/6J mice against
endotoxin-mediated lethality. In the dextran sulfate sodium (DSS) model of murine colitis, oral
administration of 7HF prevented DSS-induced weight loss, attenuated rectal bleeding, improved disease
activity index and diminished shortening of the colon of C57BL/6J mice. Histological analyses of colonic
tissues revealed that 7HF attenuated DSS-induced colonic edema, leukocyte infiltration in the colonic
mucosa and afforded significant protection against DSS-induced crypt damage. 7HF was also significantly
efficacious in attenuating carrageenan-induced paw edema in Wistar rats after oral administration. In
the collagen-induced arthritis in DBA/1J mice, 7HF significantly reduced disease associated increases in
articular index and paw thickness, protected against bone erosion and joint space narrowing and
prominently diminished joint destruction, hyperproliferative pannus formation and infiltration of
inflammatory cells. Collectively, these results provide evidence that 7HF-mediated inhibition of pro-
inflammatory cytokines functionally results in marked protection in experimental models of acute and
chronic inflammation.

PMID: 20621086 [PubMed - as supplied by publisher]

Protective effect of bioactive fraction of Sphaeranthus indicus Linn. against cyclophosphamide

induced suppression of humoral immunity in mice.

Bafna AR, Mishra SH.

Department of Pharmacy, Faculty of Technology and Engineering, The M.S. University of Baroda,
Kalabhavan, Baroda 390 001, Gujarat, India.

Abstract

The bioactive fraction of Sphaeranthus indicus produced dose dependent increase in humoral immunity
and delayed type hypersensitivity (DTH) response as evidenced by increased antibody production and
increase in paw edema. The activity at higher doses, however, declines. Humoral antibody (HA) titre
lowered by cyclophosphamide (CP) (p < 0.05) was enhanced by bioactive fraction at doses of 200 (p <
0.05) and 400 mg/kg (p < 0.001). There was dose dependent increase in HA titre in normal as well as
immunosuppressed animals indicating that drug is effective in humoral immunity. Animals treated with
cyclophosphamide and receiving bioactive fraction showed significant change in DTH response, which
directly correlates with cell-mediated immunity, as compared to cyclophosphamide alone. Thus, it can
be observed that a bioactive fraction of Sphaeranthus indicus acts as potentiator of DTH. Furthermore,
the HPTLC fingerprint profile of the bioactive fraction was established to facilitate its identification and
characterization. The results suggest that bioactive fraction influences both humoral and cell-mediated
immunity and offers protection against immunosuppression induced by the cytotoxic agent
cyclophosphamide.

PMID: 16289412 [PubMed - indexed for MEDLINE]

Microbial reactions on 7alpha-hydroxyfrullanolide and evaluation of biotransformed products for

antibacterial activity.

Ata A, Betteridge J, Schaub E, Kozera DJ, Holloway P, Samerasekera R.

Department of Chemistry, The University of Winnipeg, 515 Portage Avenue, Winnipeg MB R3B2E9,
Canada. a.ata@uwinnipeg.ca

Abstract

7alpha-Hydroxyfrullanolide (1), a known sesquiterpenoid, was isolated from Sphaeranthus indicus using
an antibacterial-activity-directed fractionation method. This compound had exhibited a significant
antibacterial activity against Gram-positive bacteria. Chemical and microbial reactions were performed
to prepare eight different analogues of compound 1 in order to evaluate these newly synthesized
compounds for antibacterial activity. These compounds were 1beta,7alpha-dihydroxyfrullanolide (2),
7alpha-hydroxy-1-oxofrullanolide (3), 4,5-dihydro-7alpha-hydroxyfrullanolide (4), 11,13-dihydro-7alpha-
hydroxyfrullanolide (5), 13-acetyl-7alpha-hydroxyfrullanolide (6), 2alpha,7alpha-
dihydroxysphaerantholide (7), 4alpha,5alpha-epoxy-7alpha-hydroxyfrullanolide (8), and 4beta,5beta-
epoxy-7alpha-hydroxyfrullanolide (9). Microbial reactions on 1 using whole-cell cultures of
Cunninghamella echinulata and Curvularia lunata yielded compounds 2-4. Incubation of compound 1
with the liquid cultures of Apsergillus niger and Rhizopus circinans yielded metabolites 5-7, while 8 and 9
were prepared by carrying out an epoxidation reaction on 1 using meta-chloroperbenzoic acid (mCPBA).
Structures of compounds 2-9 were elucidated with the aid of extensive NMR spectral studies.
Compounds 2-4 were found to be new metabolites. Compounds 1-9 were evaluated for antibacterial
activity and found to exhibit a wide range of bioactivities. Antibacterial-activity data of 1-9 suggested
that the bioactivity of 1 is largely due to the presence of C4=C5, C11=C13, and a gamma-lactone moiety.

PMID: 19774607 [PubMed - indexed for MEDLINE]

Mosquito larvicidal activity of oleic and linoleic acids isolated from Citrullus colocynthis (Linn.) Schrad.
Rahuman AA, Venkatesan P, Gopalakrishnan G.

Unit of Bioactive Natural Products, P.G & Research Department of Zoology, C. Abdul Hakeem College,
Melvisharam 632 509 Vellore Dist. Tamil Nadu, India. abdulrahuman6@hotmail.com

Abstract

In mosquito control programs, botanical origin may have the potential to be used successfully as
larvicides. The larvicidal activity of crude acetone, hexane, ethyl acetate, methanol, and petroleum ether
extracts of the leaf of Centella asiatica Linn., Datura metal Linn., Mukia scabrella Arn., Toddalia asiatica
(Linn.) Lam, extracts of whole plant of Citrullus colocynthis (Linn.) Schrad, and Sphaeranthus indicus
Linn. were assayed for their toxicity against the early fourth instar larvae of Culex quinquefasciatus
(Diptera: Culicidae). The larval mortality was observed after 24 h exposure. All extracts showed
moderate larvicidal effects; however, the highest larval mortality was found in whole plant petroleum
ether extract of C. colocynthis. In the present study, bioassay-guided fractionation of petroleum ether
extract led to the separation and identification of fatty acids; oleic acid and linoleic acid were isolated
and identified as mosquito larvicidal compounds. Oleic and Linoleic acids were quite potent against
fourth instar larvae of Aedes aegypti L. (LC50 8.80, 18.20 and LC90 35.39, 96.33 ppm), Anopheles
stephensi Liston (LC50 9.79, 11.49 and LC90 37.42, 47.35 ppm), and Culex quinquefasciatus Say (LC50
7.66, 27.24 and LC90 30.71, 70.38 ppm). The structure was elucidated from infrared, ultraviolet, 1H-
nuclear magnetic resonance, 13C-NMR, and mass spectral data. This is the first report on the mosquito
larvicidal activity of the reported isolated compounds from C. colocynthis.

PMID: 18688644 [PubMed - indexed for MEDLINE]

In vitro screening of medicinal plant extracts for macrofilaricidal activity.

Nisha M, Kalyanasundaram M, Paily KP, Abidha, Vanamail P, Balaraman K.

Vector Control Research Centre (ICMR), Indira Nagar, Pondicherry, 605006, India.
nishamathew@yahoo.com

Abstract

Methanolic extracts of 20 medicinal plants were screened at 1-10 mg/ml for in vitro macrofilaricidal
activity by worm motility assay against adult Setaria digitata, the cattle filarial worm. Four plant extracts
showed macrofilaricidal activity by worm motility at concentrations below 4 mg/ml and an incubation
period of 100 min. Complete inhibition of worm motility and subsequent mortality was observed at 3, 2,
1 and 1 mg/ml, respectively, for Centratherum anthelminticum, Cedrus deodara, Sphaeranthus indicus
and Ricinus communis. 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide (MTT) reduction
assay was carried out at 1 mg ml(-1) and 4-h incubation period, and the results showed that C. deodara,
R. communis, S. indicus and C. anthelminticum exhibited 86.56, 72.39, 61.20 and 43.15% inhibition
respectively in formazan formation compared to the control.

PMID: 17013649 [PubMed - indexed for MEDLINE]

Search for antibacterial and antifungal agents from selected Indian medicinal plants.

Kumar VP, Chauhan NS, Padh H, Rajani M.

B. V. Patel Pharmaceutical Education and Research Development (PERD) Centre, Thaltej, Ahmedabad
380054, India.

Abstract

A series of 61 Indian medicinal plants belonging to 33 different families used in various infectious
disorders, were screened for their antimicrobial properties. Screening was carried out at 1000 and 500
microg/ml concentrations by agar dilution method against Bacillus cereus var mycoides, Bacillus
pumilus, Bacillus subtilis, Bordetella bronchiseptica, Micrococcus luteus, Staphylococcus aureus,
Staphylococcus epidermidis, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa,
Streptococcus faecalis, Candida albicans, Aspergillus niger and Saccharomyces cerevisiae. Twenty-eight
plant extracts showed activity against at least one of the test organisms used in the screening. On the
basis of the results obtained, we conclude that the crude extracts of Dorema ammoniacum,
Sphaeranthus indicus, Dracaena cinnabari, Mallotus philippinensis, Jatropha gossypifolia, Aristolochia
indica, Lantana camara, Nardostachys jatamansi, Randia dumetorum and Cassia fistula exhibited
significant antimicrobial activity and properties that support folkloric use in the treatment of some
diseases as broad-spectrum antimicrobial agents. This probably explains the use of these plants by the
indigenous people against a number of infections.

PMID: 16678369 [PubMed - indexed for MEDLINE]

Mast cell stabilizing effects of Sphaeranthus indicus.

Mathew JE, Srinivasan KK, Dinakaran V, Joseph A.

Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal 576

104, Karnataka, India. jessyjamesmathew@yahoo.co.in

Abstract

AIM OF THE STUDY: We investigated the effects of Sphaeranthus indicus on mast cell stabilizing activity
to provide scientific basis for the clinical use of S. indicus.

MATERIALS AND METHODS: The protective effect of different extracts of whole plant of S. indicus
against compound 48/80 and sheep serum induced mast cell degranulation was evaluated.
RESULTS: Ethanol extract of S. indicus at the doses of 150 mg/kg and 300 mg/kg and ethyl acetate
extract at the dose of 100 mg/kg, 150 mg/kg and 300 mg/kg showed slightly better protection of mast
cell degranulation (77-86%) than the standard drug ketotifen (75%) in the sheep serum model. These
extracts also showed better mast cell stabilizing activity (77-88%) than the standard drug (69%) when
peritoneal mast cells are treated with compound 48/80.

CONCLUSION: These results suggest that S. indicus has potent mast cell stabilizing effects thereby
inhibiting mediator release from mast cells.