Malaria remains a global problem in the light of chloroquine-resistant strains of Plasmodium falciparum. New compounds are needed for the development of novel antimalarial drugs. Seed, leaf, and fruit skin extracts of Lansium domesticum, a common fruit tree in South-East Asia, are used by indigenous tribes in Sabah, Malaysia for treating malaria. The skin and aqueous leaf extracts of the tree were found to reduce parasite populations of the drug sensitive strain (3D7) and the chloroquine-resistant strain (T9) of P. falciparum equally well. The skin extracts were also found to interrupt the lifecycle of the parasite. The data reported here indicate that extracts of L. domesticum are a potential source for compounds with activity towards chloroquine-resistant strains of P. falciparum.
The plant, Typhonium flagelliforme (Araceae), commonly known as the "rodent tuber" in Malaysia, is often used as an essential ingredient of herbal remedies for alternative cancer therapies. The hexane extract of this plant was evaluated for cytotoxic activity against in vitro culture on P388 murine leukaemia cells and showed weak IC(50) of 15 microg/ml. The partial chemical constituents were identified as methyl esters of hexadecanoic acid, octadecanoic acid, 9-octadecenoic acid and 9,12-octadecadienoic acid. In addition, several common aliphatics were identified as dodecane, tridecane, tetradecane, pentadecane, hexadecane, heptadecane, octadecane, nonadecane and eicosane. The unique methyl ester of 13-phenyltridecanoic acid was isolated and positively identified using spectroscopic methods. None of the identified compounds showed or are known to have cytotoxic behaviour.
Nine naturally occurring xanthones were investigated for their platelet activating factor (PAF) receptor binding inhibitory effects using rabbit platelets. 2-(3-methylbut-2-enyl)-1,3,5-trihydoxyxanthone, macluraxanthone, 1,3,5-trihydroxy-6,6'-dimethylpyrano(2',3':6,7)-4-(1,1-dimethylprop-2-enyl)xanthone, 6-deoxyjacareubin and 2-(3-methylbut-2-enyl)-1,3,5,6-terahydroxyxanthone showed strong inhibition with IC50 values of 4.8, 11.0, 21.0, 29.0 and 44.0 microM, respectively. The prenyl group at C-2, the dimethylprop-2-enyl group at C-4 and the hydroxyl group at C-5 are all beneficial to the binding of xanthones to the PAF receptor. The results revealed that xanthones can represent a new class of natural PAF receptor antagonists.
Five aqueous extracts from three plant species, i.e., dried husks (HX), dried seeds (SX) and dried leaves (LX) of Xylocarpus granatum (Meliaceae), dried stems (ST) of Tinospora crispa (Menispermaceae) and dried leaves (LA) of Andrographis paniculata (Acanthaceae) were tested in vitro against adult worms of subperiodic Brugia malayi. The relative movability (RM) value of the adult worms over the 24-h observation period was used as a measure of the antifilarial activity of the aqueous extracts. SX extract of X. granatum demonstrated the strongest activity, followed by the LA extract of A. paniculata, ST extract of T. crispa, HX extract and LX extract of X. granatum.
In vitro and in vivo studies revealed that Malaysian medicinal plants, Piper sarmentosum, Andrographis paniculata and Tinospora crispa produced considerable antimalarial effects. Chloroform extract in vitro did show better effect than the methanol extract. The chloroform extract showed complete parasite growth inhibition as low as 0.05 mg/ml drug dose within 24 h incubation period (Andrographis paniculata) as compared to methanol extract of drug dose of 2.5 mg/ml but under incubation time of 48 h of the same plant spesies. In vivo activity of Andrographis paniculata also demonstrated higher antimalarial effect than other two plant species.
Channa striatus, a fresh water snakehead fish, is reported to enhance dermal wound healing. Biochemical components such as amino acids and fatty acids are important for the synthesis of collagen fibers during wound healing. Arachidonic acid, a precursor of prostaglandin plays a vital role in healing the wounds. Haruan (C. striatus) contains all the essential amino acids for wound healing particularly glycine as well as high contents of arachidonic acid and polyunsaturated fatty acids that can promote prostaglandin synthesis. In the present work we have studied the wound healing effect of C. striatus in Sprague-Dawley rats. Cream formulations having different haruan fish extract concentrations as the active ingredient were prepared and stabilized, and they were applied to the wounds. The healing of wounds was characterized by an increase in the tensile strength of the skin, determined on the 7th post-operative day in each case. Haruan treatment of wounds promotes remodeling of collagen, by the synthesis of inter- and intra-molecular protein crosslinking and thus produces a marked increase (P<0.05) in tensile strength as compared to the cetrimide treated group. On the basis of our experiment we conclude that C. striatus helps in wound healing as indicated by the increase in tensile strength. We hypothesise that this effect may be due to its high content of arachidonic acid, glycine and polyunsaturated fatty acids. The mechanism of wound healing will be investigated in future studies.
Crude ethanol and water extract of leaves and barks from Cassia alata were tested in vitro against fungi, (Aspergillus fumigatus and Microsporum canis), yeast (Candida albicans) and bacteria (Staphylococcus aereus and Escherichia coli). C. albicans showed concentration-dependent susceptibility towards both the ethanol and water extracts from the barks, but resistant towards the extracts of leaves. The degree of susceptibility varied, the water extract from barks showed bigger inhibition zone than the ethanol extracts (12-16 and 10-14 mm, diameter respectively). The growth of Aspergillus fumigatus and Microsporum canis were not affected by all types of the plant extracts. Results were comparable to standard antifungal drug Tioconazole (18 mm diameter) at equivalent concentration. The anti-bacterial activity of C. alata extracts on S. aureus was detected with only the leaves extracts using water and ethanol. The water extract exhibited higher antibacterial activity than the ethanol extract from leaves (inhibition zones of 11-14 and 9-11 mm, respectively). E. coli showed resistance to all types of extracts. Based on the current findings, it can be concluded that this plant has antimicrobial activity, which is as potent as standard antimicrobial drugs against certain microorganisms.
Dichloromethane and methanol extracts of 13 Zingiberaceae species from the Alpinia, Costus and Zingiber genera were screened for antimicrobial and antioxidant activities. The antimicrobial activity of most of the extracts was antibacterial with only the methanol extract of Costus discolor showing very potent antifungal activity against only Aspergillus ochraceous (MID, 15.6 microg per disc). All the extracts showed strong antioxidant activity comparable with or higher that of alpha-tocopherol.
Crude extracts (methanol) of various parts, viz. the leaves, fruits, roots, stem and trunk bark, of Garcinia atroviridis were screened for antimicrobial, cytotoxic, brine shrimp toxic, antitumour-promoting and antioxidant activities. The crude extracts exhibited predominantly antibacterial activity with the root extract showing the strongest inhibition against the test bacteria at a minimum inhibitory dose (MID) of 15.6 microg/disc. Although all the extracts failed to inhibit the growth of most of the test fungi, significant antifungal activity against Cladosporium herbarum was exhibited by most notably the fruit (MID: 100 microg), and the leaf (MID: 400 microg) extracts. None of the extracts were significantly cytotoxic, and lethal towards brine shrimps. The root, leaf, trunk and stem bark extracts (except for the fruits) showed strong antioxidant activity exceeding that of the standard antioxidant, alpha-tocopherol. Antitumour-promoting activity (>95% inhibition) was shown by the fruit, leaf, stem and trunk bark extracts.
Haruan, Channa striatus, is a snakehead fish consumed in many parts of the southeast Asian region. It is believed to promote wound healing, as well as reduce post-operative pain. In an attempt to establish the scientific basis for the alleged pain-relieving benefits of this fish, we studied the antinociceptive effects of whole fillet and mucus extracts from haruan in the mouse using the abdominal constriction and tail flick tests. In the abdominal constriction test, the 30 min fillet extract exhibited concentration-dependent inhibition of the writhing response in the 10-50% concentration range, with 20% as the IC50 value. This activity was not dependent on the duration of extraction, with no significant differences among the extracts obtained at durations of 10, 20, 30, 60, 90 and 120 min (range between 45-54% inhibition at 20% concentration). The mucus extract also showed concentration-dependent inhibition of the abdominal constriction response-at the highest concentration used the average inhibition was 68.9%, while IC50 value was 25%. Neither the fillet extract (30 min, 20%) nor the mucus extract (25%) had any demonstrable effect on the tail flick latency on their own, but significantly enhanced the antinociceptive activity of morphine in this assay. Similarly, low concentrations of the mucus and fillet extract enhanced the effects of morphine in the abdominal constriction test. Collectively, these results suggest a scientific basis for the folklore practice of eating haruan fish in the post-operative period for pain relief: Haruan extracts have antinociceptive activity and enhance the activity of other antinociceptive agents.
Sarawak, on the island of Borneo, is known internationally for its rich rain forests, flora and fauna. Its rain forests, occupying two-thirds of its geographical area shelters 2500 tree species, 5500 flowering plants and over 20 000 different kinds of animals and insects. Such abundance of plants, and in particular, in the variety thereof, have attracted the attention of scientists involved in the field of research into their potential medicinal value. Recent discovery that two species of Calophyllum tree in the rain forests of Sarawak produce active anti-HIV agents, has, no doubt, intensified interest in the State's plant resources for scientific research.
In October, 1993, 16 months after the United Nations approved the International Convention on Biodiversity held in Rio de Janeiro, June, 1992, the Philippine Congress ratified and adopted the Convention. This is a manifestation of the full support of the Philippines for the principles and policies adopted by the UN body on the conservation of biodiversity, sustainable development of biological resources and equitable sharing of benefits between users and owners of biodiversity resources. The Philippine scientific community has long recognized the need for and importance of a national guideline and policy with regard to the collection of plants and animals in the Philippines for scientific or commercial purposes. A series of consultative meetings were held by representatives of government agencies, non-government organizations, private organizations, academic and private persons concerned with biodiversity conservation to formulate national guidelines that regulate the collection of plant and animal specimens in the country. Guidelines were unanimously adopted by various government agencies and academia and a Memorandum of Agreement (MOA) was signed on September 28, 1990. Very recently a new document was drafted, specifically to serve as a guideline for those who desire to undertake sample collecting in the Philippines for biodiversity prospecting. The document is now being reviewed by government departments and agencies and will be presented to the President of the Philippines for signing as an Executive Order (EO). Once signed, this EO will serve as a national policy for bioprospecting in the country. The Philippines is one of the countries in Southeast Asia that has endorsed the adoption of regional guidelines on the collection of plant and animal organisms for drug development. The ASEAN Agreement on the Conservation of Nature and Natural Resources (1985). The Manila Declaration (1992) and lately, the Melaka Accord (1994), all of which were signed by various countries in Asia, are manifestations of this interest.
Ethanolic extract of Cassia alata leaves was investigated for its antimicrobial activities on several microorganisms including bacteria, yeast, dermatophytic fungi and non-dermatophytic fungi. In vitro, the extract exhibited high activity against various species of dermatophytic fungi but low activity against non-dermatophytic fungi. However, bacterial and yeast species showed resistance against in vitro treatment with the extract. The minimum inhibitory concentration (MIC) values of the extract revealed that Trichophyton mentagorphytes var. interdigitale, Trichophyton mentagrophytes var. mentagorophytes, Trichophyton rubrum and Microsporum gypseum had the MIC of 125 mg/ml, whereas Microsporum canis had the MIC of 62.5 mg/ml. The inhibition can be observed on the macroconidia of Microsporum gypseum which resulted in structural degeneration beyond repair. The mechanism of inhibition can be related to the cell leakage as observed by irregular, wrinkle shape and loss in rigidity of the macroconidia.
An investigation of nine Malaysian dart poisons has confirmed that their main active components are cardenolides from Antiaris toxicaria (Pers.) Lesch. and alkaloids probably from different forms of Strychnos ignatii P. Bergius. It is not possible to determine the ethnic origin of the poisons from the results of the analyses on their own. Two new cardiac glycosides have been isolated and their structures determined as 12 beta-hydroxycannogenin 3 beta-O-beta-D-deoxygulopyranoside and 3 beta-O-alpha-L-rhamnopyranoside, respectively.
Pharmacological studies showed that Limacia scanden Lour. extracts have sympathomimetic activities similar to noradrenaline (NA). A crude extract of Limacia scanden injected intravenously as a single bolus induced a dose-dependent increase in arterial blood pressure in anaesthetized rats and cats. Pretreatment with a non-specific alpha blocker phentolamine (10(-5) M) blocked this effect, whereas the beta blocker propanolol (10(-5) M) did not. The extract also reduced intestinal motility and this response could be blocked by pretreatment with phentolamine (10(-5) M) and specific alpha1-blocker, prazosin (10(-5) M). In superfused rabbit aorta preparations, it induced an increase in contractions. This effect was blocked by pretreatment with prazosin (10(-5) M), whereas the alpha2-blocker yohimbine (10(-5) M) had only a slight effect. The effects of NA on superfused aorta strip contraction were similar to extract. Toxic symptoms were manifested in less than 5 min when the mice were given 465 mg/kg of extract intraperitoneally. Physiological and behavioural changes observed in dying mice implicated serious malfunctioning of the autonomic nervous system and motor activity. Electrophysiological studies on the tonically autoactive neuron (TAN) of the snail Achantina fulica Férussac revealed that crude extract of Limacia scanden induced excitatory responses which were similar to those of serotonin (5-HT) stimulation. Studies with different ionic compositions of the bathing saline revealed that this excitatory effect of Limacia scanden could be attributed either to release of endogenous serotonin or inhibition of 5-HT reuptake in the CNS. This observation could tentatively be used to provide the framework towards elucidating the mechanism and rationale for the use of this plant in traditional medicine in the treatment of depression and affective disorders.
Measurement of rates of propulsion in the small intestine in control and experimental groups of male Sprague-Dawley rats (200-250 g) were carried out as a means of assessing antidiarrhoeal activity of aqueous extracts of the leaf of Psidium guajava (L.), using morphine as the standard drug of reference. Hyperpropulsion (diarrhoea) was induced by gavaging rats in a control group with Microlax, using phenol red mixed into it as a marker in the intestine, and the mean rate of the hyperpropulsion was determined. The normal rate of propulsion, defined as the percentage of the length of the ileum traversed by the front of the dye in 1 h after gavaging animals with a liquid paraffin-phenol red meal, was also determined in another control group. In experimental groups pretreated with enteral administration of either morphine or aqueous extracts, 1 h before the challenge with Microlax, the percentage inhibition to the hyperpropulsive rate (antidiarrhoeal activity) was calculated. Both morphine and the extracts produced a dose-response relationship in their antidiarrhoeal effects. A dose of 0.2 ml/kg fresh leaf extract produced 65% inhibition of propulsion. This dose is equiactive with 0.2 mg/kg of morphine sulphate. The antidiarrhoeal action of the extract may be due, in part, to the inhibition of the increased watery secretions that occur commonly in all acute diarrhoeal diseases and cholera.
Among several alkaloids, including dimeric indoles, isolated from Uncaria callophylla, gambirine which is an alkaloid unique to this plant, has been found to be another hypotensive principle from the plant. Intravenous injections of gambirine in the dose range of 0.2 to 10.0 mg/kg caused a dose-related fall in both systolic and diastolic blood pressures as well as heart rate. At all doses gambirine showed a prompt onset of action and at the higher doses (5.0-10 mg/kg), marked persistence of hypotension accompanied by severe bradycardia were observed. In addition, higher doses of gambirine produced a more marked decrease in diastolic than systolic pressure while at lower doses both decreased equally. It is suggested that the hypotensive effect of gambirine may be peripheral in origin and is associated, at least in part, with a cardiac action.